-
1
-
-
0019303558
-
Transforming growth factors: Isolation of polypeptides from virally and chemically transformed cells by acid/ethanol extraction
-
Roberts AB, Lamb LC, Newton DL, Sporn MB, De Larco JE, Todaro GJ. Transforming growth factors: isolation of polypeptides from virally and chemically transformed cells by acid/ethanol extraction. Proc Natl Acad Sci U S A. 1980;77(6):3494–3498.
-
(1980)
Proc Natl Acad Sci U S A
, vol.77
, Issue.6
, pp. 3494-3498
-
-
Roberts, A.B.1
Lamb, L.C.2
Newton, D.L.3
Sporn, M.B.4
De Larco, J.E.5
Todaro, G.J.6
-
2
-
-
0032763469
-
Specificity, diversity, and regulation in TGF-beta superfamily signaling
-
Piek E, Heldin CH, Ten Dijke P. Specificity, diversity, and regulation in TGF-beta superfamily signaling. FASEB J. 1999;13(15):2105–2124.
-
(1999)
FASEB J
, vol.13
, Issue.15
, pp. 2105-2124
-
-
Piek, E.1
Heldin, C.H.2
Ten Dijke, P.3
-
3
-
-
0020465034
-
Synergistic interaction of two classes of transforming growth factors from murine sarcoma cells
-
Anzano MA, Roberts AB, Meyers CA, et al. Synergistic interaction of two classes of transforming growth factors from murine sarcoma cells. Cancer Res. 1982;42(11):4776–4778.
-
(1982)
Cancer Res
, vol.42
, Issue.11
, pp. 4776-4778
-
-
Anzano, M.A.1
Roberts, A.B.2
Meyers, C.A.3
-
4
-
-
0346254671
-
New class of transforming growth factors potentiated by epidermal growth factor: Isolation from non-neoplastic tissues
-
Roberts AB, Anzano MA, Lamb LC, Smith JM, Sporn MB. New class of transforming growth factors potentiated by epidermal growth factor: isolation from non-neoplastic tissues. Proc Natl Acad Sci U S A. 1981;78(9):5339–5343.
-
(1981)
Proc Natl Acad Sci U S A
, vol.78
, Issue.9
, pp. 5339-5343
-
-
Roberts, A.B.1
Anzano, M.A.2
Lamb, L.C.3
Smith, J.M.4
Sporn, M.B.5
-
5
-
-
0034644472
-
TGFbeta signaling in growth control, cancer, and heritable disorders
-
Massague J, Blain SW, Lo RS. TGFbeta signaling in growth control, cancer, and heritable disorders. Cell. 2000;103(2):295–309.
-
(2000)
Cell
, vol.103
, Issue.2
, pp. 295-309
-
-
Massague, J.1
Blain, S.W.2
Lo, R.S.3
-
6
-
-
0023652332
-
The transforming growth factor-beta system, a complex pattern of cross-reactive ligands and receptors
-
Cheifetz S, Weatherbee JA, Tsang ML, et al. The transforming growth factor-beta system, a complex pattern of cross-reactive ligands and receptors. Cell. 1987;48(3):409–415.
-
(1987)
Cell
, vol.48
, Issue.3
, pp. 409-415
-
-
Cheifetz, S.1
Weatherbee, J.A.2
Tsang, M.L.3
-
7
-
-
79953792899
-
TGF-β signalling is mediated by two autonomously functioning TβRI:TβRII pairs
-
Huang T, David L, Mendoza V, et al. TGF-β signalling is mediated by two autonomously functioning TβRI:TβRII pairs. EMBO J. 2011;30(7):1263–1276.
-
(2011)
EMBO J
, vol.30
, Issue.7
, pp. 1263-1276
-
-
Huang, T.1
David, L.2
Mendoza, V.3
-
8
-
-
84866985855
-
Targeting the TGFbeta signalling pathway in disease
-
Akhurst RJ, Hata A. Targeting the TGFbeta signalling pathway in disease. Nat Rev Drug Discov. 2012;11(10):790–811.
-
(2012)
Nat Rev Drug Discov
, vol.11
, Issue.10
, pp. 790-811
-
-
Akhurst, R.J.1
Hata, A.2
-
9
-
-
40849133772
-
Role of transforming growth factor-beta superfamily signaling pathways in human disease
-
Gordon KJ, Blobe GC. Role of transforming growth factor-beta superfamily signaling pathways in human disease. Biochim Biophys Acta. 2008;1782(4):197–228.
-
(2008)
Biochim Biophys Acta
, vol.1782
, Issue.4
, pp. 197-228
-
-
Gordon, K.J.1
Blobe, G.C.2
-
10
-
-
10444261212
-
Development of TGF-beta signalling inhibitors for cancer therapy
-
Yingling, JM, Blanchard KL, Sawyer JS. Development of TGF-beta signalling inhibitors for cancer therapy. Nat Rev Drug Discov. 2004;3(12):1011–1022.
-
(2004)
Nat Rev Drug Discov
, vol.3
, Issue.12
, pp. 1011-1022
-
-
Yingling, J.M.1
Blanchard, K.L.2
Sawyer, J.S.3
-
11
-
-
0030593038
-
DPC4, a candidate tumor suppressor gene at human chromosome 18q21.1
-
Hahn SA, Schutte M, Hoque AT, et al. DPC4, a candidate tumor suppressor gene at human chromosome 18q21.1. Science. 1996;271(5247):350–353.
-
(1996)
Science
, vol.271
, Issue.5247
, pp. 350-353
-
-
Hahn, S.A.1
Schutte, M.2
Hoque, A.T.3
-
12
-
-
0033555627
-
Mutational inactivation of transforming growth factor beta receptor type II in microsatellite stable colon cancers
-
Grady WM, Myeroff LL, Swinler SE, et al. Mutational inactivation of transforming growth factor beta receptor type II in microsatellite stable colon cancers. Cancer Res. 1999;59(2):320–324.
-
(1999)
Cancer Res
, vol.59
, Issue.2
, pp. 320-324
-
-
Grady, W.M.1
Myeroff, L.L.2
Swinler, S.E.3
-
13
-
-
0032897720
-
Reduced transforming growth factor-beta type II receptor (TGF-beta RII) expression in adenocarcinoma of the lung
-
Kim WS, Park C, Jung YS, et al. Reduced transforming growth factor-beta type II receptor (TGF-beta RII) expression in adenocarcinoma of the lung. Anticancer Res. 1999;19(1A):301–306.
-
(1999)
Anticancer Res
, vol.19
, Issue.1
, pp. 301-306
-
-
Kim, W.S.1
Park, C.2
Jung, Y.S.3
-
14
-
-
30944444113
-
Alterations in components of the TGF-beta superfamily signaling pathways in human cancer
-
Levy L, Hill CS. Alterations in components of the TGF-beta superfamily signaling pathways in human cancer. Cytokine Growth Factor Rev. 2006;17(1–2):41–58.
-
(2006)
Cytokine Growth Factor Rev
, vol.17
, Issue.1-2
, pp. 41-58
-
-
Levy, L.1
Hill, C.S.2
-
15
-
-
84894593599
-
Molecular mechanisms of epithelial-mesenchymal transition
-
Lamouille S, Xu J, Derynck R. Molecular mechanisms of epithelial-mesenchymal transition. Nat Rev Mol Cell Biol. 2014;15(3):178–196.
-
(2014)
Nat Rev Mol Cell Biol
, vol.15
, Issue.3
, pp. 178-196
-
-
Lamouille, S.1
Xu, J.2
Derynck, R.3
-
16
-
-
0022465625
-
Production of transforming growth factor beta by human T lymphocytes and its potential role in the regulation of T cell growth
-
Kehrl JH, Wakefield LM, Roberts AB, et al. Production of transforming growth factor beta by human T lymphocytes and its potential role in the regulation of T cell growth. J Exp Med. 1986;163(5):1037–1050.
-
(1986)
J Exp Med
, vol.163
, Issue.5
, pp. 1037-1050
-
-
Kehrl, J.H.1
Wakefield, L.M.2
Roberts, A.B.3
-
17
-
-
77954951446
-
The polarization of immune cells in the tumour environment by TGFbeta
-
Flavell RA, Sanjabi S, Wrzesinski SH, Licona-Limon P. The polarization of immune cells in the tumour environment by TGFbeta. Nat Rev Immunol. 2010;10(8):554–567.
-
(2010)
Nat Rev Immunol
, vol.10
, Issue.8
, pp. 554-567
-
-
Flavell, R.A.1
Sanjabi, S.2
Wrzesinski, S.H.3
Licona-Limon, P.4
-
18
-
-
2142646426
-
TGF-beta signaling and the fibrotic response
-
Leask A, Abraham DJ. TGF-beta signaling and the fibrotic response. FASEB J. 2004;18(7):816–827.
-
(2004)
FASEB J
, vol.18
, Issue.7
, pp. 816-827
-
-
Leask, A.1
Abraham, D.J.2
-
19
-
-
84905863057
-
Differential knockdown of TGF-beta ligands in a three-dimensional co-culture tumor–stromal interaction model of lung cancer
-
Horie M, Saito A, Noguchi S, et al. Differential knockdown of TGF-beta ligands in a three-dimensional co-culture tumor–stromal interaction model of lung cancer. BMC Cancer. 2014;14:580.
-
(2014)
BMC Cancer
, vol.14
-
-
Horie, M.1
Saito, A.2
Noguchi, S.3
-
20
-
-
33745837774
-
Targeting tumor-associated fibroblasts improves cancer chemotherapy by increasing intratumoral drug uptake
-
Loeffler M, Kruger JA, Niethammer AG, Reisfeld RA. Targeting tumor-associated fibroblasts improves cancer chemotherapy by increasing intratumoral drug uptake. J Clin Invest. 2006;116(7):1955–1962.
-
(2006)
J Clin Invest
, vol.116
, Issue.7
, pp. 1955-1962
-
-
Loeffler, M.1
Kruger, J.A.2
Niethammer, A.G.3
Reisfeld, R.A.4
-
21
-
-
58149230979
-
TGF-beta signaling in vascular biology and dysfunction
-
Goumans MJ, Liu Z, ten Dijke P. TGF-beta signaling in vascular biology and dysfunction. Cell Res. 2009;19(1):116–127.
-
(2009)
Cell Res
, vol.19
, Issue.1
, pp. 116-127
-
-
Goumans, M.J.1
Liu, Z.2
Ten Dijke, P.3
-
22
-
-
79952284127
-
Hallmarks of cancer: The next generation
-
Hanahan D, Weinberg RA. Hallmarks of cancer: the next generation. Cell. 2011;144(5):646–674.
-
(2011)
Cell
, vol.144
, Issue.5
, pp. 646-674
-
-
Hanahan, D.1
Weinberg, R.A.2
-
23
-
-
0242499448
-
Cytostatic and apoptotic actions of TGF-beta in homeostasis and cancer
-
Siegel PM, Massague J. Cytostatic and apoptotic actions of TGF-beta in homeostasis and cancer. Nat Rev Cancer. 2003;3(11):807–821.
-
(2003)
Nat Rev Cancer
, vol.3
, Issue.11
, pp. 807-821
-
-
Siegel, P.M.1
Massague, J.2
-
24
-
-
84888639681
-
The roles of TGFbeta in the tumour microenvironment
-
Pickup M, Novitskiy S, Moses HL. The roles of TGFbeta in the tumour microenvironment. Nat Rev Cancer. 2013;13(11):788–799.
-
(2013)
Nat Rev Cancer
, vol.13
, Issue.11
, pp. 788-799
-
-
Pickup, M.1
Novitskiy, S.2
Moses, H.L.3
-
25
-
-
33751311939
-
Inhibition of transforming growth factor-beta signaling in human cancer: Targeting a tumor suppressor network as a therapeutic strategy
-
Biswas S, Criswell TL, Wang SE, Arteaga CL. Inhibition of transforming growth factor-beta signaling in human cancer: targeting a tumor suppressor network as a therapeutic strategy. Clin Cancer Res. 2006;12(14 Pt 1):4142–4146.
-
(2006)
Clin Cancer Res
, vol.12
, Issue.14
, pp. 4142-4146
-
-
Biswas, S.1
Criswell, T.L.2
Wang, S.E.3
Arteaga, C.L.4
-
26
-
-
40949083607
-
Cancer-associated transforming growth factor beta type II receptor gene mutant causes activation of bone morphogenic protein-Smads and invasive phenotype
-
Bharathy S, Xie W, Yingling JM, Reiss M. Cancer-associated transforming growth factor beta type II receptor gene mutant causes activation of bone morphogenic protein-Smads and invasive phenotype. Cancer Res. 2008;68(6):1656–1666.
-
(2008)
Cancer Res
, vol.68
, Issue.6
, pp. 1656-1666
-
-
Bharathy, S.1
Xie, W.2
Yingling, J.M.3
Reiss, M.4
-
28
-
-
33847635618
-
Improvement of cancer-targeting therapy, using nanocarriers for intractable solid tumors by inhibition of TGF-beta signaling
-
Kano MR, Bae Y, Iwata C, et al. Improvement of cancer-targeting therapy, using nanocarriers for intractable solid tumors by inhibition of TGF-beta signaling. Proc Natl Acad Sci U S A. 2007;104(9):3460–3465.
-
(2007)
Proc Natl Acad Sci U S A
, vol.104
, Issue.9
, pp. 3460-3465
-
-
Kano, M.R.1
Bae, Y.2
Iwata, C.3
-
29
-
-
70350418644
-
VEGF and inhibitors of TGFbeta type-I receptor kinase synergistically promote blood-vessel formation by inducing alpha5-integrin expression
-
Liu Z, Kobayashi K, van Dinther M, et al. VEGF and inhibitors of TGFbeta type-I receptor kinase synergistically promote blood-vessel formation by inducing alpha5-integrin expression. J Cell Sci. 2009;122(Pt 18):3294–3302.
-
(2009)
J Cell Sci
, vol.122
, pp. 3294-3302
-
-
Liu, Z.1
Kobayashi, K.2
Van Dinther, M.3
-
30
-
-
84897566294
-
Phase I study of GC1008 (Fresolimumab): A human anti-transforming growth factor-beta (TGFbeta) monoclonal antibody in patients with advanced malignant melanoma or renal cell carcinoma
-
Morris JC, Tan AR, Olencki TE, et al. Phase I study of GC1008 (fresolimumab): a human anti-transforming growth factor-beta (TGFbeta) monoclonal antibody in patients with advanced malignant melanoma or renal cell carcinoma. PLoS One. 2014;9(3):e90353.
-
(2014)
Plos One
, vol.9
, Issue.3
-
-
Morris, J.C.1
Tan, A.R.2
Olencki, T.E.3
-
32
-
-
79956011495
-
A phase 1, single-dose study of fresolimumab, an anti-TGF-beta antibody, in treatment-resistant primary focal segmental glomerulosclerosis
-
Trachtman H, Fervenza FC, Gipson DS, et al. A phase 1, single-dose study of fresolimumab, an anti-TGF-beta antibody, in treatment-resistant primary focal segmental glomerulosclerosis. Kidney Int. 2011;79(11):1236–1243.
-
(2011)
Kidney Int
, vol.79
, Issue.11
, pp. 1236-1243
-
-
Trachtman, H.1
Fervenza, F.C.2
Gipson, D.S.3
-
33
-
-
84885717570
-
Immunological effects of the TGFβ-blocking antibody GC1008 in malignant pleural mesothelioma patients
-
Stevenson JP, Kindler HL, Papasavvas E, et al. Immunological effects of the TGFβ-blocking antibody GC1008 in malignant pleural mesothelioma patients. Onco Immunology. 2013;2:e26218.
-
(2013)
Onco Immunology
, vol.2
-
-
Stevenson, J.P.1
Kindler, H.L.2
Papasavvas, E.3
-
34
-
-
84907710779
-
A phase I dose-escalation study to a predefined dose of a transforming growth factor-β1 monoclonal antibody (TβM1) in patients with metastatic cancer
-
Cohn A, Lahn M, Williams K, et al. A phase I dose-escalation study to a predefined dose of a transforming growth factor-β1 monoclonal antibody (TβM1) in patients with metastatic cancer. Int J Oncol. 2014;45(6):2221–2231.
-
(2014)
Int J Oncol
, vol.45
, Issue.6
, pp. 2221-2231
-
-
Cohn, A.1
Lahn, M.2
Williams, K.3
-
35
-
-
76749102053
-
Anti-transforming growth factor beta receptor II antibody has therapeutic efficacy against primary tumor growth and metastasis through multieffects on cancer, stroma, and immune cells
-
Zhong Z, Carroll KD, Policarpio D, et al. Anti-transforming growth factor beta receptor II antibody has therapeutic efficacy against primary tumor growth and metastasis through multieffects on cancer, stroma, and immune cells. Clin Cancer Res. 2010;16(4):1191–1205.
-
(2010)
Clin Cancer Res
, vol.16
, Issue.4
, pp. 1191-1205
-
-
Zhong, Z.1
Carroll, K.D.2
Policarpio, D.3
-
36
-
-
79951602633
-
Targeted therapy for high-grade glioma with the TGF-beta2 inhibitor trabedersen: Results of a randomized and controlled phase IIb study
-
Bogdahn U, Hau P, Stockhammer G, et al. Targeted therapy for high-grade glioma with the TGF-beta2 inhibitor trabedersen: results of a randomized and controlled phase IIb study. Neuro Oncol. 2011;13(1):132–142.
-
(2011)
Neuro Oncol
, vol.13
, Issue.1
, pp. 132-142
-
-
Bogdahn, U.1
Hau, P.2
Stockhammer, G.3
-
37
-
-
84939828061
-
-
[homepage on the Internet]. Antisense Pharma Unveils its Corporate Strategy for, Accessed March 3, 2015
-
Isarna-therapeutics.com [homepage on the Internet]. Antisense Pharma Unveils its Corporate Strategy for 2013. Available from: http://www.isarna-therapeutics.com/fileadmin/user_upload/documents/press-releases/2013/20130226_EN_PressRelease_CorporateStrategy_2013.pdf. Accessed March 3, 2015.
-
(2013)
-
-
-
40
-
-
43249108418
-
The TGFBeta pathway as a therapeutic target in cancer
-
Seoane J. The TGFBeta pathway as a therapeutic target in cancer. Clin Transl Oncol. 2008;10(1):14–19.
-
(2008)
Clin Transl Oncol
, vol.10
, Issue.1
, pp. 14-19
-
-
Seoane, J.1
-
41
-
-
73449089494
-
Companies waver in efforts to target transforming growth factor beta in cancer
-
Garber K. Companies waver in efforts to target transforming growth factor beta in cancer. J Natl Cancer Inst. 2009;101(24):1664–1667.
-
(2009)
J Natl Cancer Inst
, vol.101
, Issue.24
, pp. 1664-1667
-
-
Garber, K.1
-
42
-
-
72049091524
-
Targeting the transforming growth factor-beta signaling pathway in human cancer
-
Nagaraj NS, Datta PK. Targeting the transforming growth factor-beta signaling pathway in human cancer. Expert Opin Investig Drugs. 2010;19(1):77–91.
-
(2010)
Expert Opin Investig Drugs
, vol.19
, Issue.1
, pp. 77-91
-
-
Nagaraj, N.S.1
Datta, P.K.2
-
43
-
-
33751328068
-
Ki26894, a novel transforming growth factor-beta type I receptor kinase inhibitor, inhibits in vitro invasion and in vivo bone metastasis of a human breast cancer cell line
-
Ehata S, Hanyu A, Fujime M, et al. Ki26894, a novel transforming growth factor-beta type I receptor kinase inhibitor, inhibits in vitro invasion and in vivo bone metastasis of a human breast cancer cell line. Cancer Sci. 2007;98(1):127–133.
-
(2007)
Cancer Sci
, vol.98
, Issue.1
, pp. 127-133
-
-
Ehata, S.1
Hanyu, A.2
Fujime, M.3
-
44
-
-
84901270358
-
Discovery of N-((4-([1,2,4]Triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): A highly potent, selective, and orally bioavailable inhibitor of TGF-beta type I receptor kinase as cancer immunotherapeutic/antifibrotic agent
-
Jin CH, Krishnaiah M, Sreenu D, et al. Discovery of N-((4-([1,2,4]Triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-beta type I receptor kinase as cancer immunotherapeutic/antifibrotic agent. J Med Chem. 2014;57(10):4213–4238.
-
(2014)
J Med Chem
, vol.57
, Issue.10
, pp. 4213-4238
-
-
Jin, C.H.1
Krishnaiah, M.2
Sreenu, D.3
-
45
-
-
84904169349
-
EW-7197, a novel ALK-5 Kinase inhibitor, potently inhibits breast to lung metastasis
-
Son JY, Park SY, Kim SJ, et al. EW-7197, a novel ALK-5 Kinase inhibitor, potently inhibits breast to lung metastasis. Mol Cancer Ther. 2014;13(7):1704–1716.
-
(2014)
Mol Cancer Ther
, vol.13
, Issue.7
, pp. 1704-1716
-
-
Son, J.Y.1
Park, S.Y.2
Kim, S.J.3
-
46
-
-
0026496172
-
TGF beta signals through a heteromeric protein kinase receptor complex
-
Wrana JL, Attisano L, Carcamo J, et al. TGF beta signals through a heteromeric protein kinase receptor complex. Cell. 1992;71(6):1003–1014.
-
(1992)
Cell
, vol.71
, Issue.6
, pp. 1003-1014
-
-
Wrana, J.L.1
Attisano, L.2
Carcamo, J.3
-
47
-
-
0029022221
-
GS domain mutations that constitutively activate T beta R-I, the downstream signaling component in the TGF-beta receptor complex
-
Wieser R, Wrana JL, J Massague J. GS domain mutations that constitutively activate T beta R-I, the downstream signaling component in the TGF-beta receptor complex. EMBO J. 1995;14(10):2199–2208.
-
(1995)
EMBO J
, vol.14
, Issue.10
, pp. 2199-2208
-
-
Wieser, R.1
Wrana, J.L.2
J Massague, J.3
-
48
-
-
0038641688
-
Induction of c-sis mRNA and activity similar to platelet-derived growth factor by transforming growth factor beta: A proposed model for indirect mitogenesis involving autocrine activity
-
Leof EB, Proper JA, Goustin AS, Shipley GD, DiCorleto PE, MosesHL. Induction of c-sis mRNA and activity similar to platelet-derived growth factor by transforming growth factor beta: a proposed model for indirect mitogenesis involving autocrine activity. Proc Natl Acad Sci U S A. 1986;83(8):2453–2457.
-
(1986)
Proc Natl Acad Sci U S A
, vol.83
, Issue.8
, pp. 2453-2457
-
-
Leof, E.B.1
Proper, J.A.2
Goustin, A.S.3
Shipley, G.D.4
Dicorleto, P.E.5
Moses, H.L.6
-
49
-
-
2942589081
-
Synthesis and activity of new aryl- and heteroaryl-substituted 5,6-dihydro-4H-pyrrolo[1,2-b]pyrazole inhibitors of the transforming growth factor-beta type I receptor kinase domain
-
Sawyer JS, Beight DW, Britt KS, et al. Synthesis and activity of new aryl- and heteroaryl-substituted 5,6-dihydro-4H-pyrrolo[1,2-b]pyrazole inhibitors of the transforming growth factor-beta type I receptor kinase domain. Bioorg Med Chem Lett. 2004;14(13):3581–3584.
-
(2004)
Bioorg Med Chem Lett
, vol.14
, Issue.13
, pp. 3581-3584
-
-
Sawyer, J.S.1
Beight, D.W.2
Britt, K.S.3
-
50
-
-
0037620888
-
Synthesis and activity of new aryl- and heteroaryl-substituted pyrazole inhibitors of the transforming growth factor-beta type I receptor kinase domain
-
Sawyer JS, Anderson BD, Beight DW, et al. Synthesis and activity of new aryl- and heteroaryl-substituted pyrazole inhibitors of the transforming growth factor-beta type I receptor kinase domain. J Med Chem. 2003;46(19):3953–3956.
-
(2003)
J Med Chem
, vol.46
, Issue.19
, pp. 3953-3956
-
-
Sawyer, J.S.1
Erson, B.D.2
Beight, D.W.3
-
51
-
-
41849147494
-
Optimization of a dihydropyrrolopyrazole series of transforming growth factor-beta type I receptor kinase domain inhibitors: Discovery of an orally bioavailable transforming growth factor-beta receptor type I inhibitor as antitumor agent
-
Li HY, McMillen WT, Heap CR, et al. Optimization of a dihydropyrrolopyrazole series of transforming growth factor-beta type I receptor kinase domain inhibitors: discovery of an orally bioavailable transforming growth factor-beta receptor type I inhibitor as antitumor agent. J Med Chem. 2008;51(7):2302–2306.
-
(2008)
J Med Chem
, vol.51
, Issue.7
, pp. 2302-2306
-
-
Li, H.Y.1
McMillen, W.T.2
Heap, C.R.3
-
53
-
-
20044375562
-
Kinetic characterization of novel pyrazole TGF-beta receptor I kinase inhibitors and their blockade of the epithelial-mesenchymal transition
-
Peng SB, Yan L, Xia X, et al. Kinetic characterization of novel pyrazole TGF-beta receptor I kinase inhibitors and their blockade of the epithelial-mesenchymal transition. Biochemistry. 2005;44(7):2293–2304.
-
(2005)
Biochemistry
, vol.44
, Issue.7
, pp. 2293-2304
-
-
Peng, S.B.1
Yan, L.2
Xia, X.3
-
54
-
-
33745050200
-
Activated type I TGFbeta receptor kinase enhances the survival of mammary epithelial cells and accelerates tumor progression
-
Muraoka-Cook RS, Shin I, Yi JY, et al. Activated type I TGFbeta receptor kinase enhances the survival of mammary epithelial cells and accelerates tumor progression. Oncogene. 2006;25(24):3408–3423.
-
(2006)
Oncogene
, vol.25
, Issue.24
, pp. 3408-3423
-
-
Muraoka-Cook, R.S.1
Shin, I.2
Yi, J.Y.3
-
55
-
-
2942559053
-
Novel and potent transforming growth factor beta type I receptor kinase domain inhibitor: 7-amino 4-(2-pyridin-2-yl-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazol-3-yl)-quinolines
-
Li HY, Wang Y, Yan L, et al. Novel and potent transforming growth factor beta type I receptor kinase domain inhibitor: 7-amino 4-(2-pyridin-2-yl-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazol-3-yl)-quinolines. Bioorg Med Chem Lett. 2004;14(13):3585–3588.
-
(2004)
Bioorg Med Chem Lett
, vol.14
, Issue.13
, pp. 3585-3588
-
-
Li, H.Y.1
Wang, Y.2
Yan, L.3
-
56
-
-
84939828064
-
Transforming growth factor beta (TGF-beta) inhibitors and their development in the treatment of cancer
-
San Francisco, CA
-
Lahn M. Transforming growth factor beta (TGF-beta) inhibitors and their development in the treatment of cancer. In: 3rd Cancer Drug Research and Development GTCbio, 2006, San Francisco, CA.
-
(2006)
3Rd Cancer Drug Research and Development Gtcbio
-
-
Lahn, M.1
-
57
-
-
84922201803
-
Nonclinical safety evaluation of a transforming growth factor β receptor I kinase inhibitor in fischer 344 rats and beagle dogs
-
Stauber AJ, Credille KM, Truex LL, Ehlhardt WJ, Young JK. Nonclinical safety evaluation of a transforming growth factor β receptor I kinase inhibitor in fischer 344 rats and beagle dogs. J Clin Pract. 2014;4:196.
-
(2014)
J Clin Pract
, vol.4
-
-
Stauber, A.J.1
Credille, K.M.2
Truex, L.L.3
Ehlhardt, W.J.4
Young, J.K.5
-
60
-
-
80053585761
-
Induction of heart valve lesions by small-molecule ALK5 inhibitors
-
Anderton MJ, Mellor HR, Bell A, et al. Induction of heart valve lesions by small-molecule ALK5 inhibitors. Toxicol Pathol. 2011;39(6):916–924.
-
(2011)
Toxicol Pathol
, vol.39
, Issue.6
, pp. 916-924
-
-
Anderton, M.J.1
Mellor, H.R.2
Bell, A.3
-
61
-
-
4644243836
-
Transforming the TGFbeta pathway: Convergence of distinct lead generation strategies on a novel kinase pharmacophore for TbetaRI (ALK5)
-
Singh J, Ling LE, Sawyer JS, Lee WC, Zhang F, Yingling JM. Transforming the TGFbeta pathway: convergence of distinct lead generation strategies on a novel kinase pharmacophore for TbetaRI (ALK5). Curr Opin Drug Discov Devel. 2004;7(4):437–445.
-
(2004)
Curr Opin Drug Discov Devel
, vol.7
, Issue.4
, pp. 437-445
-
-
Singh, J.1
Ling, L.E.2
Sawyer, J.S.3
Lee, W.C.4
Zhang, F.5
Yingling, J.M.6
-
62
-
-
84939828065
-
Pathobiology of a valvulopathy in fischer 344 rats given a transforming growth factor-b RI kinase inhibitor
-
2006. San Diego (CA): Oxford University Press. Abstract 290
-
Stauber AJ, Zimmermann JL, Berridge BR. Pathobiology of a valvulopathy in fischer 344 rats given a transforming growth factor-b RI kinase inhibitor. In: SOT 45th Annual Meeting and Tox Expo™; 2006. San Diego (CA): Oxford University Press. Abstract 290.
-
SOT 45Th Annual Meeting and Tox Expo™
-
-
Stauber, A.J.1
Zimmermann, J.L.2
Berridge, B.R.3
-
63
-
-
0030955330
-
Shear stress as an inhibitor of vascular smooth muscle cell proliferation. Role of transforming growth factor-beta 1 and tissue-type plasminogen activator
-
Ueba H, Kawakami M, Yaginuma T. Shear stress as an inhibitor of vascular smooth muscle cell proliferation. Role of transforming growth factor-beta 1 and tissue-type plasminogen activator. Arterioscler Thromb Vasc Biol. 1997;17(8):1512–1516.
-
(1997)
Arterioscler Thromb Vasc Biol
, vol.17
, Issue.8
, pp. 1512-1516
-
-
Ueba, H.1
Kawakami, M.2
Yaginuma, T.3
-
64
-
-
84887071743
-
The role of shear-induced transforming growth factor-beta signaling in the endothelium
-
Walshe TE, dela Paz NG, D’Amore PA. The role of shear-induced transforming growth factor-beta signaling in the endothelium. Arterioscler Thromb Vasc Biol. 2013;33(11):2608–2617.
-
(2013)
Arterioscler Thromb Vasc Biol
, vol.33
, Issue.11
, pp. 2608-2617
-
-
Walshe, T.E.1
Dela Paz, N.G.2
D’Amore, P.A.3
-
65
-
-
33747812887
-
Aneurysm syndromes caused by mutations in the TGF-beta receptor
-
Loeys BL, Schwarze U, Holm T, et al. Aneurysm syndromes caused by mutations in the TGF-beta receptor. N Engl J Med. 2006;355(8):788–798.
-
(2006)
N Engl J Med
, vol.355
, Issue.8
, pp. 788-798
-
-
Loeys, B.L.1
Schwarze, U.2
Holm, T.3
-
66
-
-
84864415173
-
Loss-of-function mutations in TGFB2 cause a syndromic presentation of thoracic aortic aneurysm
-
Lindsay ME, Schepers D, Bolar NA, et al. Loss-of-function mutations in TGFB2 cause a syndromic presentation of thoracic aortic aneurysm. Nat Genet. 2012;44(8):922–927.
-
(2012)
Nat Genet
, vol.44
, Issue.8
, pp. 922-927
-
-
Lindsay, M.E.1
Schepers, D.2
Bolar, N.A.3
-
67
-
-
79954625123
-
Noncanonical TGFbeta signaling contributes to aortic aneurysm progression in Marfan syndrome mice
-
Holm TM, Habashi JP, Doyle JJ, et al. Noncanonical TGFbeta signaling contributes to aortic aneurysm progression in Marfan syndrome mice. Science. 2011;332(6027):358–361.
-
(2011)
Science
, vol.332
, Issue.6027
, pp. 358-361
-
-
Holm, T.M.1
Habashi, J.P.2
Doyle, J.J.3
-
68
-
-
33645754505
-
Signal processing in the TGF-beta superfamily ligand-receptor network
-
Vilar JM, Jansen R, Sander C. Signal processing in the TGF-beta superfamily ligand-receptor network. PLoS Comput Biol. 2006;2(1):e3.
-
(2006)
Plos Comput Biol
, vol.2
, Issue.1
-
-
Vilar, J.M.1
Jansen, R.2
Sander, C.3
-
69
-
-
84891864342
-
Controlling long-term signaling: Receptor dynamics determine attenuation and refractory behavior of the TGF-beta pathway
-
Vizan P, Miller DS, Gori I, Das D, Schmierer B, Hill CS. Controlling long-term signaling: receptor dynamics determine attenuation and refractory behavior of the TGF-beta pathway. Sci Signal. 2013;6(305):ra106.
-
(2013)
Sci Signal
, vol.6
, Issue.305
-
-
Vizan, P.1
Miller, D.S.2
Gori, I.3
Das, D.4
Schmierer, B.5
Hill, C.S.6
-
70
-
-
78249231410
-
Role of transforming growth factor-beta in inflammatory bowel disease and colitis-associated colon cancer
-
Feagins LA. Role of transforming growth factor-beta in inflammatory bowel disease and colitis-associated colon cancer. Inflamm Bowel Dis. 2010;16(11):1963–1968.
-
(2010)
Inflamm Bowel Dis
, vol.16
, Issue.11
, pp. 1963-1968
-
-
Feagins, L.A.1
-
71
-
-
77952524907
-
Connection between inflammation and carcinogenesis in gastrointestinal tract: Focus on TGF-beta signaling
-
Hong S, Lee HJ, Kim SJ, Hahm KB. Connection between inflammation and carcinogenesis in gastrointestinal tract: focus on TGF-beta signaling. World J Gastroenterol. 2010;16(17):2080–2093.
-
(2010)
World J Gastroenterol
, vol.16
, Issue.17
, pp. 2080-2093
-
-
Hong, S.1
Lee, H.J.2
Kim, S.J.3
Hahm, K.B.4
-
73
-
-
37149042061
-
Semi-mechanistic modelling of the tumour growth inhibitory effects of LY2157299, a new type I receptor TGF-beta kinase antagonist, in mice
-
Bueno L, de Alwis DP, Pitou C, et al. Semi-mechanistic modelling of the tumour growth inhibitory effects of LY2157299, a new type I receptor TGF-beta kinase antagonist, in mice. Eur J Cancer. 2008;44(1):142–150.
-
(2008)
Eur J Cancer
, vol.44
, Issue.1
, pp. 142-150
-
-
Bueno, L.1
De Alwis, D.P.2
Pitou, C.3
-
74
-
-
84882362186
-
A small molecule inhibitor of TGFβ RI kinase potentiates VEGF dependent angiogenesis in vitro
-
Abstract 250
-
Yingling JM, Shou J, Xia X, et al. A small molecule inhibitor of TGFβ RI kinase potentiates VEGF dependent angiogenesis in vitro. Proc Am Assoc Cancer Res. 2006. Abstract 250.
-
(2006)
Proc am Assoc Cancer Res
-
-
Yingling, J.M.1
Shou, J.2
Xia, X.3
-
75
-
-
84939960795
-
Anti-tumor activity of the TGF-beta receptor kinase inhibitor galunisertib (LY2157299 monohydrate) in patient-derived tumor xenografts
-
Epub, Jan 9
-
Maier A, Peille AL, Vuaroqueaux V, Lahn M. Anti-tumor activity of the TGF-beta receptor kinase inhibitor galunisertib (LY2157299 monohydrate) in patient-derived tumor xenografts. Cell Oncol (Dordr). Epub 2015 Jan 9
-
(2015)
Cell Oncol (Dordr)
-
-
Maier, A.1
Peille, A.L.2
Vuaroqueaux, V.3
Lahn, M.4
-
76
-
-
0035501062
-
TGF-beta signaling in cancer–a double-edged sword
-
Akhurst RJ, Derynck R. TGF-beta signaling in cancer–a double-edged sword. Trends Cell Biol. 2001;11(11):S44–S51.
-
(2001)
Trends Cell Biol
, vol.11
, Issue.11
, pp. S44-S51
-
-
Akhurst, R.J.1
Derynck, R.2
-
77
-
-
0034785348
-
TGF-beta signaling in tumor suppression and cancer progression
-
Derynck R, Akhurst RJ, Balmain A. TGF-beta signaling in tumor suppression and cancer progression. Nat Genet. 2001;29(2):117–129.
-
(2001)
Nat Genet
, vol.29
, Issue.2
, pp. 117-129
-
-
Derynck, R.1
Akhurst, R.J.2
Balmain, A.3
-
78
-
-
0036087521
-
Lifetime exposure to a soluble TGF-beta antagonist protects mice against metastasis without adverse side effects
-
Yang YA, Dukhanina O, Tang B, et al. Lifetime exposure to a soluble TGF-beta antagonist protects mice against metastasis without adverse side effects. J Clin Invest. 2002;109(12):1607–1615.
-
(2002)
J Clin Invest
, vol.109
, Issue.12
, pp. 1607-1615
-
-
Yang, Y.A.1
Dukhanina, O.2
Tang, B.3
-
79
-
-
84876931434
-
Flow-based pipeline for systematic modulation and analysis of 3D tumor microenvironments
-
Li CY, Wood DK, Huang JH, Bhatia SN. Flow-based pipeline for systematic modulation and analysis of 3D tumor microenvironments. Lab Chip. 2013;13(10):1969–1978.
-
(2013)
Lab Chip
, vol.13
, Issue.10
, pp. 1969-1978
-
-
Li, C.Y.1
Wood, D.K.2
Huang, J.H.3
Bhatia, S.N.4
-
80
-
-
84870020040
-
MED12 controls the response to multiple cancer drugs through regulation of TGF-beta receptor signaling
-
Huang S, Holzel M, Knijnenburg T, et al. MED12 controls the response to multiple cancer drugs through regulation of TGF-beta receptor signaling. Cell. 2012;151(5):937–950.
-
(2012)
Cell
, vol.151
, Issue.5
, pp. 937-950
-
-
Huang, S.1
Holzel, M.2
Knijnenburg, T.3
-
81
-
-
84874607100
-
TGF-beta inhibition enhances chemotherapy action against triple-negative breast cancer
-
Bhola NE, Balko JM, Dugger TC, et al. TGF-beta inhibition enhances chemotherapy action against triple-negative breast cancer. J Clin Invest. 2013;123(3):1348–1358.
-
(2013)
J Clin Invest
, vol.123
, Issue.3
, pp. 1348-1358
-
-
Bhola, N.E.1
Balko, J.M.2
Dugger, T.C.3
-
82
-
-
0842282616
-
Predictive pharmacokinetic-pharmacodynamic modeling of tumor growth kinetics in xenograft models after administration of anticancer agents
-
Simeoni M, Magni P, Cammia C, et al. Predictive pharmacokinetic-pharmacodynamic modeling of tumor growth kinetics in xenograft models after administration of anticancer agents. Cancer Res. 2004;64(3):1094–1101.
-
(2004)
Cancer Res
, vol.64
, Issue.3
, pp. 1094-1101
-
-
Simeoni, M.1
Magni, P.2
Cammia, C.3
-
83
-
-
15244351351
-
A pharmacokinetic-pharmacodynamic model for predicting tumour growth inhibition in mice: A useful tool in oncology drug development
-
Rocchetti M, Poggesi I, Germani M, et al. A pharmacokinetic-pharmacodynamic model for predicting tumour growth inhibition in mice: a useful tool in oncology drug development. Basic Clin Pharmacol Toxicol. 2005;96(3):265–268.
-
(2005)
Basic Clin Pharmacol Toxicol
, vol.96
, Issue.3
, pp. 265-268
-
-
Rocchetti, M.1
Poggesi, I.2
Germani, M.3
-
84
-
-
80053221530
-
Effect of gastric pH on the pharmacokinetics of a BCS class II compound in dogs: Utilization of an artificial stomach and duodenum dissolution model and GastroPlus, simulations to predict absorption
-
Bhattachar SN, Perkins EJ, Tan JS, Burns LJ. Effect of gastric pH on the pharmacokinetics of a BCS class II compound in dogs: utilization of an artificial stomach and duodenum dissolution model and GastroPlus, simulations to predict absorption. J Pharm Sci. 2011;100(11):4756–4765.
-
(2011)
J Pharm Sci
, vol.100
, Issue.11
, pp. 4756-4765
-
-
Bhattachar, S.N.1
Perkins, E.J.2
Tan, J.S.3
Burns, L.J.4
-
85
-
-
84899071195
-
Defining a therapeutic window for the novel TGF-β inhibitor LY2157299 monohydrate based on a pharmacokinetic/pharmacodynamic model
-
Gueorguieva I, Cleverly AL, Stauber A, et al. Defining a therapeutic window for the novel TGF-β inhibitor LY2157299 monohydrate based on a pharmacokinetic/pharmacodynamic model. Br J Clin Pharmacol. 2014;77(5):796–807.
-
(2014)
Br J Clin Pharmacol
, vol.77
, Issue.5
, pp. 796-807
-
-
Gueorguieva, I.1
Cleverly, A.L.2
Stauber, A.3
-
86
-
-
0030843284
-
Comparison of cytogenetics, cytokine secretion, and oncogene expression in primary cultures of renal carcinoma cells
-
Lahn M, Kunzmann R, Kohler G, et al. Comparison of cytogenetics, cytokine secretion, and oncogene expression in primary cultures of renal carcinoma cells. Oncology. 1997;54(5):429–437.
-
(1997)
Oncology
, vol.54
, Issue.5
, pp. 429-437
-
-
Lahn, M.1
Kunzmann, R.2
Kohler, G.3
-
87
-
-
0035367931
-
Preoperative plasma levels of transforming growth factor beta(1) (TGF-beta(1)) strongly predict progression in patients undergoing radical prostatectomy
-
Shariat SF, Shalev M, Menesses-Diaz A, et al. Preoperative plasma levels of transforming growth factor beta(1) (TGF-beta(1)) strongly predict progression in patients undergoing radical prostatectomy. J Clin Oncol. 2001;19(11):2856–2864.
-
(2001)
J Clin Oncol
, vol.19
, Issue.11
, pp. 2856-2864
-
-
Shariat, S.F.1
Shalev, M.2
Menesses-Diaz, A.3
-
88
-
-
33746145265
-
Inhibition of pulmonary and skeletal metastasis by a transforming growth factor-beta type I receptor kinase inhibitor
-
Bandyopadhyay A, Agyin JK, Wang L, et al. Inhibition of pulmonary and skeletal metastasis by a transforming growth factor-beta type I receptor kinase inhibitor. Cancer Res. 2006;66(13):6714–6721.
-
(2006)
Cancer Res
, vol.66
, Issue.13
, pp. 6714-6721
-
-
Bandyopadhyay, A.1
Agyin, J.K.2
Wang, L.3
-
89
-
-
34247617701
-
Development and validation of a phosphorylated SMAD ex vivo stimulation assay
-
Farrington DL, Yingling JM, Fill JA, et al. Development and validation of a phosphorylated SMAD ex vivo stimulation assay. Biomarkers. 2007;12(3):313–330.
-
(2007)
Biomarkers
, vol.12
, Issue.3
, pp. 313-330
-
-
Farrington, D.L.1
Yingling, J.M.2
Fill, J.A.3
-
90
-
-
39149139338
-
TGF-beta signalling-related markers in cancer patients with bone metastasis
-
Baselga J, Rothenberg ML, Tabernero J, et al. TGF-beta signalling-related markers in cancer patients with bone metastasis. Biomarkers. 2008;13(2):217–236.
-
(2008)
Biomarkers
, vol.13
, Issue.2
, pp. 217-236
-
-
Baselga, J.1
Rothenberg, M.L.2
Tabernero, J.3
-
91
-
-
77954176730
-
Analysis and variability of TGFbeta measurements in cancer patients with skeletal metastases
-
O’Brien PJ, Ramanathan R, Yingling JM, et al. Analysis and variability of TGFbeta measurements in cancer patients with skeletal metastases. Biologics. 2008;2(3):563–569.
-
(2008)
Biologics
, vol.2
, Issue.3
, pp. 563-569
-
-
O’Brien, P.J.1
Ramanathan, R.2
Yingling, J.M.3
-
92
-
-
76749138062
-
Application of T cell-based transcriptomics to identify three candidate biomarkers for monitoring anti-TGFbetaR therapy
-
Classen S, Muth C, Debey-Pascher S, et al. Application of T cell-based transcriptomics to identify three candidate biomarkers for monitoring anti-TGFbetaR therapy. Pharmacogenet Genomics. 2010;20(3):147–156.
-
(2010)
Pharmacogenet Genomics
, vol.20
, Issue.3
, pp. 147-156
-
-
Classen, S.1
Muth, C.2
Debey-Pascher, S.3
-
93
-
-
84907700942
-
A canonical transforming growth factor beta-dependent signaling pathway is present in peripheral blood cells of cancer patients with skeletal metastasis
-
Kadam S, Cleverly AL, Farmen M, Grondin J, Cox YI, Lahn M. A canonical transforming growth factor beta-dependent signaling pathway is present in peripheral blood cells of cancer patients with skeletal metastasis. J Mol Biomark Diagn. 2013;4(3):153–161.
-
(2013)
J Mol Biomark Diagn
, vol.4
, Issue.3
, pp. 153-161
-
-
Kadam, S.1
Cleverly, A.L.2
Farmen, M.3
Grondin, J.4
Cox, Y.I.5
Lahn, M.6
-
94
-
-
84939828068
-
Integrative analysis of genomic RNA expression data from in vitro and in vivo models of TGF-beta receptor kinase inhibitors to identify novel informative biomarkers of TGF-beta signaling
-
Kanjilal V, Yingling JM, Yan L, et al. Integrative analysis of genomic RNA expression data from in vitro and in vivo models of TGF-beta receptor kinase inhibitors to identify novel informative biomarkers of TGF-beta signaling. Cancer Res. 2006;(1):204.
-
(2006)
Cancer Res
, vol.1
-
-
Kanjilal, V.1
Yingling, J.M.2
Yan, L.3
-
95
-
-
84939828069
-
-
Presented at: First AACR Centennial Conference on Translational Cancer Medicine; Nov 4–8; 2007; Singapore. Abstract B57
-
Duan K, Kanjilal V, Yan L, Yingling J, Patel K, Shou J. Genomic analysis of TGFβ treated cell lines with phenotypically distinct outcomes to identify transcriptional signatures for assessment in stratification of cancers. Presented at: First AACR Centennial Conference on Translational Cancer Medicine; Nov 4–8; 2007; Singapore. Abstract B57.
-
Genomic Analysis of TGFβ Treated Cell Lines with Phenotypically Distinct Outcomes to Identify Transcriptional Signatures for Assessment in Stratification of Cancers
-
-
Duan, K.1
Kanjilal, V.2
Yan, L.3
Yingling, J.4
Patel, K.5
Shou, J.6
-
96
-
-
84939828070
-
First human dose escalation study in patients with metastatic malignancies to determine safety and pharmacokinetics of LY2157299, a small molecule inhibitor of the transforming growth factor-beta receptor I kinase. Poster presented at: ASCO Annual Meeting; 2008; Chicago, IL
-
Abstract 14554
-
Calvo-Aller E, Baselga J, Glatt S, et al. First human dose escalation study in patients with metastatic malignancies to determine safety and pharmacokinetics of LY2157299, a small molecule inhibitor of the transforming growth factor-beta receptor I kinase. Poster presented at: ASCO Annual Meeting; 2008; Chicago, IL. J Clin Oncol. Abstract 14554.
-
J Clin Oncol
-
-
Calvo-Aller, E.1
Baselga, J.2
Glatt, S.3
-
99
-
-
84939828072
-
-
Presented at: ASCO Annual Meeting; 2013; Chicago, IL. Abstract
-
Rodon J, Carducci MA, Sepúlveda JM, et al. Integrated data review of the first-in-human dose (FHD) study evaluating safety, pharmacokinetics (PK), and pharmacodynamics (PD) of the oral transforming growth factor-beta (TGF-β) receptor I kinase inhibitor, LY2157299 monohydrate (LY). Presented at: ASCO Annual Meeting; 2013; Chicago, IL. Abstract 2016.
-
(2016)
Integrated Data Review of the First-In-Human Dose (FHD) Study Evaluating Safety, Pharmacokinetics (PK), and Pharmacodynamics (PD) of the Oral Transforming Growth Factor-Beta (TGF-β) Receptor I Kinase Inhibitor, LY2157299 Monohydrate (LY)
-
-
Rodon, J.1
Carducci, M.A.2
Sepúlveda, J.M.3
-
100
-
-
84942370577
-
Cardiac safety of TGF-beta receptor I kinase inhibitor LY2157299 monohydrate in cancer patients in a first-in-human dose study
-
Epub 2014 Dec 9
-
Kovacs RJ, Maldonado G, Azaro A, et al. Cardiac safety of TGF-beta receptor I kinase inhibitor LY2157299 monohydrate in cancer patients in a first-in-human dose study. Cardiovasc Toxicol. Epub 2014 Dec 9; DOI: 10.1007/s12012-014-9297-4.
-
Cardiovasc Toxicol
-
-
Kovacs, R.J.1
Maldonado, G.2
Azaro, A.3
-
101
-
-
84939804573
-
Case series of cancer patients treated with galunisertib, a transforming growth factor-beta receptor I kinase inhibitor in a first-in-human dose study
-
Azaro A, Rodon J, Carducci M, et al. Case series of cancer patients treated with galunisertib, a transforming growth factor-beta receptor I kinase inhibitor in a first-in-human dose study. J Med Cases. 2014;5(11):603–609.
-
(2014)
J Med Cases
, vol.5
, Issue.11
, pp. 603-609
-
-
Azaro, A.1
Rodon, J.2
Carducci, M.3
-
102
-
-
84939789948
-
Pharmacokinetic, pharmacodynamic and biomarker evaluation of transforming growth factor-beta receptor I kinase inhibitor, galunisertib, in phase 1 study in patients with advanced cancer
-
Rodon J, Carducci M, Sepulveda-Sanchez JM, et al. Pharmacokinetic, pharmacodynamic and biomarker evaluation of transforming growth factor-beta receptor I kinase inhibitor, galunisertib, in phase 1 study in patients with advanced cancer. Invest New Drugs. 2015;33(2):357–370.
-
(2015)
Invest New Drugs
, vol.33
, Issue.2
, pp. 357-370
-
-
Rodon, J.1
Carducci, M.2
Sepulveda-Sanchez, J.M.3
-
103
-
-
84961288435
-
First-in-human dose study of the novel transforming growth factor-beta receptor I kinase inhibitor LY2157299 monohydrate in patients with advanced cancer and glioma
-
Rodon J, Carducci MA, Sepulveda-Sanchez JM, et al. First-in-human dose study of the novel transforming growth factor-beta receptor I kinase inhibitor LY2157299 monohydrate in patients with advanced cancer and glioma. Clin Cancer Res. 2015;21(3):553–560.
-
(2015)
Clin Cancer Res
, vol.21
, Issue.3
, pp. 553-560
-
-
Rodon, J.1
Carducci, M.A.2
Sepulveda-Sanchez, J.M.3
-
104
-
-
84930005881
-
Assessment of changes in brain perfusion and permeability in patients with advanced, refractory glioblastoma treated with the combination of lomustine and the oral transforming growth factor-beta (TGF-β) receptor I kinase inhibitor LY2157299 monohydrate
-
Sepulveda-Sanchez J, Ramos A, Hilario A, et al. Assessment of changes in brain perfusion and permeability in patients with advanced, refractory glioblastoma treated with the combination of lomustine and the oral transforming growth factor-beta (TGF-β) receptor I kinase inhibitor LY2157299 monohydrate. Oncology Lett. 2015;9(6):2442–2448.
-
(2015)
Oncology Lett
, vol.9
, Issue.6
, pp. 2442-2448
-
-
Sepulveda-Sanchez, J.1
Ramos, A.2
Hilario, A.3
-
105
-
-
84870677094
-
Isocitrate dehydrogenase (IDH) mutations promote a reversible ZEB1/microRNA (miR)-200-dependent epithelial-mesenchymal transition (EMT)
-
Grassian AR, Lin F, Barrett R, et al. Isocitrate dehydrogenase (IDH) mutations promote a reversible ZEB1/microRNA (miR)-200-dependent epithelial-mesenchymal transition (EMT). J Biol Chem. 2012;287(50):42180–42194.
-
(2012)
J Biol Chem
, vol.287
, Issue.50
, pp. 42180-42194
-
-
Grassian, A.R.1
Lin, F.2
Barrett, R.3
-
106
-
-
73649123907
-
Integrated genomic analysis identifies clinically relevant subtypes of glioblastoma characterized by abnormalities in PDGFRA, IDH1, EGFR, and NF1
-
Verhaak RG, Hoadley KA, Purdom E, et al. Integrated genomic analysis identifies clinically relevant subtypes of glioblastoma characterized by abnormalities in PDGFRA, IDH1, EGFR, and NF1. Cancer Cell. 2010;17(1):98–110.
-
(2010)
Cancer Cell
, vol.17
, Issue.1
, pp. 98-110
-
-
Verhaak, R.G.1
Hoadley, K.A.2
Purdom, E.3
-
107
-
-
78649986150
-
TGF-beta receptor inhibitors target the CD44 (High)/Id1 (high) glioma-initiating cell population in human glioblastoma
-
Anido J, Saez-Borderias A, Gonzalez-Junca A, et al. TGF-beta receptor inhibitors target the CD44 (high)/Id1 (high) glioma-initiating cell population in human glioblastoma. Cancer Cell. 2010;18(6):655–668.
-
(2010)
Cancer Cell
, vol.18
, Issue.6
, pp. 655-668
-
-
Anido, J.1
Saez-Borderias, A.2
Gonzalez-Junca, A.3
-
108
-
-
33846821916
-
High TGFbeta-Smad activity confers poor prognosis in glioma patients and promotes cell proliferation depending on the methylation of the PDGF-B gene
-
Bruna A, Darken RS, Rojo F, et al. High TGFbeta-Smad activity confers poor prognosis in glioma patients and promotes cell proliferation depending on the methylation of the PDGF-B gene. Cancer Cell. 2007;11(2):147–160.
-
(2007)
Cancer Cell
, vol.11
, Issue.2
, pp. 147-160
-
-
Bruna, A.1
Darken, R.S.2
Rojo, F.3
-
110
-
-
80053502219
-
VEGFR2 expression and TGF-beta signaling in initial and recurrent high-grade human glioma
-
Kuczynski EA, Patten SG, Coomber BL. VEGFR2 expression and TGF-beta signaling in initial and recurrent high-grade human glioma. Oncology. 2011;81(2):126–134.
-
(2011)
Oncology
, vol.81
, Issue.2
, pp. 126-134
-
-
Kuczynski, E.A.1
Patten, S.G.2
Coomber, B.L.3
-
111
-
-
84873143684
-
Plasma levels of transforming growth factor-beta 1 before and after removal of low- and high-grade astrocytomas
-
Loh JK, Lieu AS, Su YF, et al. Plasma levels of transforming growth factor-beta 1 before and after removal of low- and high-grade astrocytomas. Cytokine. 2013;61(2):413–418.
-
(2013)
Cytokine
, vol.61
, Issue.2
, pp. 413-418
-
-
Loh, J.K.1
Lieu, A.S.2
Su, Y.F.3
-
112
-
-
63249123273
-
TGF-beta increases glioma-initiating cell self-renewal through the induction of LIF in human glioblastoma
-
Penuelas S, Anido J, Prieto-Sanchez RM, et al. TGF-beta increases glioma-initiating cell self-renewal through the induction of LIF in human glioblastoma. Cancer Cell. 2009;15(4):315–327.
-
(2009)
Cancer Cell
, vol.15
, Issue.4
, pp. 315-327
-
-
Penuelas, S.1
Anido, J.2
Prieto-Sanchez, R.M.3
-
113
-
-
84865140762
-
Resistance of glioblastoma-initiating cells to radiation mediated by the tumor microenvironment can be abolished by inhibiting transforming growth factor-beta
-
Hardee ME, Marciscano AE, Medina-Ramirez CM, et al. Resistance of glioblastoma-initiating cells to radiation mediated by the tumor microenvironment can be abolished by inhibiting transforming growth factor-beta. Cancer Res. 2012;72(16):4119–4129.
-
(2012)
Cancer Res
, vol.72
, Issue.16
, pp. 4119-4129
-
-
Hardee, M.E.1
Marciscano, A.E.2
Medina-Ramirez, C.M.3
-
114
-
-
79958082880
-
Trimodal glioblastoma treatment consisting of concurrent radiotherapy, temozolomide, and the novel TGF-beta receptor I kinase inhibitor LY2109761
-
Zhang M, Herion TW, Timke C, et al. Trimodal glioblastoma treatment consisting of concurrent radiotherapy, temozolomide, and the novel TGF-beta receptor I kinase inhibitor LY2109761. Neoplasia. 2011;13(6):537–549.
-
(2011)
Neoplasia
, vol.13
, Issue.6
, pp. 537-549
-
-
Zhang, M.1
Herion, T.W.2
Timke, C.3
-
115
-
-
82655181475
-
Blockade of TGF-beta signaling by the TGFbetaR-I kinase inhibitor LY2109761 enhances radiation response and prolongs survival in glioblastoma
-
Zhang M, Kleber S, Rohrich M, et al. Blockade of TGF-beta signaling by the TGFbetaR-I kinase inhibitor LY2109761 enhances radiation response and prolongs survival in glioblastoma. Cancer Res. 2011;71(23):7155–7167.
-
(2011)
Cancer Res
, vol.71
, Issue.23
, pp. 7155-7167
-
-
Zhang, M.1
Kleber, S.2
Rohrich, M.3
-
116
-
-
84939828074
-
-
Parsons S, Sawyer S, Yan L, et al. The combination of the small molecule TGFβR1 inhibitor, LY2157299 monohydrate, with CCNU substantially blocks SMAD phosphorylation and significantly suppresses human glioblastoma xenograft growth. Presented at: Proceedings of the 2011 AACR-NCI-EORTC International Conference on Molecular Targets and Cancer Therapeutics; November 12–16; 2011; San Francisco, CA. Mol Cancer Ther. Abstract C201.
-
The Combination of the Small Molecule TGFβR1 Inhibitor, LY2157299 Monohydrate, with CCNU Substantially Blocks SMAD Phosphorylation and Significantly Suppresses Human Glioblastoma Xenograft Growth
-
-
Parsons, S.1
Sawyer, S.2
Yan, L.3
-
117
-
-
84872660761
-
-
Silver Spring (MD): US Food and Drug Administration; 2013 [updated April 1, 2013], Accessed March 3, 2015
-
US Food and Drug Administration. Search Orphan Drug Designations and Approvals. Silver Spring (MD): US Food and Drug Administration; 2013 [updated April 1, 2013]. Available from: http://www.accessdata.fda.gov/scripts/opdlisting/oopd/OOPD_Results_2.cfm?Index_Number=378712. Accessed March 3, 2015.
-
Search Orphan Drug Designations and Approvals
-
-
-
120
-
-
84939828076
-
Safety interim data from a three-arm phase II study evaluating safety and pharmacokinetics of the oral transforming growth factor-beta (TGF-β) receptor I kinase inhibitor LY2157299 monohydrate in patients with glioblastoma at first progression
-
Chicago, IL. Abstract Number 2061
-
Carpentier AF, Brandes AA, Kesari S, et al. Safety interim data from a three-arm phase II study evaluating safety and pharmacokinetics of the oral transforming growth factor-beta (TGF-β) receptor I kinase inhibitor LY2157299 monohydrate in patients with glioblastoma at first progression. In: Annual Meeting of the American Society of Clinical Oncology; 2013; Chicago, IL. Abstract Number 2061.
-
(2013)
Annual Meeting of the American Society of Clinical Oncology
-
-
Carpentier, A.F.1
Brandes, A.A.2
Kesari, S.3
-
121
-
-
84939828077
-
-
Poster presented at: 18th Annual SNO Scientific Meeting and Education Day; November 22; 2013;2013; Society of Neurooncology: San Francisco, CA
-
Wick W, Suarez C, Rodon J, et al. Phase 1b/2a study evaluating safety, pharmacokinetics (PK) and preliminary pharmacodynamics responses of the oral transforming growth factor-beta (TGF-β) receptor I kinase inhibitor LY2157299 monohydrate (LY) when combined with chemoradiotherapy in newly diagnosed malignant gliomas. Poster presented at: 18th Annual SNO Scientific Meeting and Education Day; November 22; 2013;2013; Society of Neurooncology: San Francisco, CA.
-
Phase 1B/2A Study Evaluating Safety, Pharmacokinetics (PK) and Preliminary Pharmacodynamics Responses of the Oral Transforming Growth Factor-Beta (TGF-β) Receptor I Kinase Inhibitor LY2157299 Monohydrate (LY) When Combined with Chemoradiotherapy in Newly Diagnosed Malignant Gliomas
-
-
Wick, W.1
Suarez, C.2
Rodon, J.3
-
122
-
-
0032964644
-
Transforming growth factor betas and their signaling receptors in human hepatocellular carcinoma
-
Abou-Shady M, Baer HU, Friess H, et al. Transforming growth factor betas and their signaling receptors in human hepatocellular carcinoma. Am J Surg. 1999;177(3):209–215.
-
(1999)
Am J Surg
, vol.177
, Issue.3
, pp. 209-215
-
-
Abou-Shady, M.1
Baer, H.U.2
Friess, H.3
-
123
-
-
0033865273
-
Regulatory mechanisms for transforming growth factor beta as an autocrine inhibitor in human hepatocellular carcinoma: Implications for roles of smads in its growth
-
Matsuzaki K, Date M, Furukawa F, et al. Regulatory mechanisms for transforming growth factor beta as an autocrine inhibitor in human hepatocellular carcinoma: implications for roles of smads in its growth. Hepatology. 2000;32(2):218–227.
-
(2000)
Hepatology
, vol.32
, Issue.2
, pp. 218-227
-
-
Matsuzaki, K.1
Date, M.2
Furukawa, F.3
-
124
-
-
0033948531
-
Transforming growth factor beta1 and soluble Fas serum levels in hepatocellular carcinoma
-
Sacco R, Leuci D, Tortorella C, et al. Transforming growth factor beta1 and soluble Fas serum levels in hepatocellular carcinoma. Cytokine. 2000;12(6):811–814.
-
(2000)
Cytokine
, vol.12
, Issue.6
, pp. 811-814
-
-
Sacco, R.1
Leuci, D.2
Tortorella, C.3
-
125
-
-
27744527762
-
Laminin-5 with transforming growth factor-beta1 induces epithelial to mesenchymal transition in hepatocellular carcinoma
-
Giannelli G, Bergamini C, Fransvea E, Sgarra C, Antonaci S. Laminin-5 with transforming growth factor-beta1 induces epithelial to mesenchymal transition in hepatocellular carcinoma. Gastroenterology. 2005;129(5):1375–1383.
-
(2005)
Gastroenterology
, vol.129
, Issue.5
, pp. 1375-1383
-
-
Giannelli, G.1
Bergamini, C.2
Fransvea, E.3
Sgarra, C.4
Antonaci, S.5
-
126
-
-
84897450600
-
Transforming growth factor-beta as a therapeutic target in hepatocellular carcinoma
-
Giannelli G, Villa E, Lahn M. Transforming growth factor-beta as a therapeutic target in hepatocellular carcinoma. Cancer Res. 2014;74(7):1890–1894.
-
(2014)
Cancer Res
, vol.74
, Issue.7
, pp. 1890-1894
-
-
Giannelli, G.1
Villa, E.2
Lahn, M.3
-
127
-
-
43949140575
-
Blocking transforming growth factor-beta up-regulates E-cadherin and reduces migration and invasion of hepatocellular carcinoma cells
-
Fransvea E, Angelotti U, Antonaci S, Giannelli G. Blocking transforming growth factor-beta up-regulates E-cadherin and reduces migration and invasion of hepatocellular carcinoma cells. Hepatology. 2008;47(5):1557–1566.
-
(2008)
Hepatology
, vol.47
, Issue.5
, pp. 1557-1566
-
-
Fransvea, E.1
Angelotti, U.2
Antonaci, S.3
Giannelli, G.4
-
128
-
-
63349088695
-
Targeting transforming growth factor (TGF)-betaRI inhibits activation of beta1 integrin and blocks vascular invasion in hepatocellular carcinoma
-
Fransvea E, Mazzocca A, Antonaci S, Giannelli G. Targeting transforming growth factor (TGF)-betaRI inhibits activation of beta1 integrin and blocks vascular invasion in hepatocellular carcinoma. Hepatology. 2009;49(3):839–850.
-
(2009)
Hepatology
, vol.49
, Issue.3
, pp. 839-850
-
-
Fransvea, E.1
Mazzocca, A.2
Antonaci, S.3
Giannelli, G.4
-
129
-
-
70350059078
-
Inhibition of transforming growth factor beta receptor I kinase blocks hepatocellular carcinoma growth through neo-angiogenesis regulation
-
Mazzocca A, Fransvea E, Lavezzari G, Antonaci S, Giannelli G. Inhibition of transforming growth factor beta receptor I kinase blocks hepatocellular carcinoma growth through neo-angiogenesis regulation. Hepatology. 2009;50(4):1140–1151.
-
(2009)
Hepatology
, vol.50
, Issue.4
, pp. 1140-1151
-
-
Mazzocca, A.1
Fransvea, E.2
Lavezzari, G.3
Antonaci, S.4
Giannelli, G.5
-
130
-
-
84939828078
-
-
Presented at: 22nd EORTC-NCI-AACR Symposium on Molecular Targets and Cancer Therapeutics, Berlin, Germany
-
Garbay D, Serova M, Serrate C, et al. Specific TGF-beta receptor-I inhibition using LY364947 impairs signaling, motility and invasion in parental and multikinase inhibitor-resistant hepatocarcinoma cells. Presented at: 22nd EORTC-NCI-AACR Symposium on Molecular Targets and Cancer Therapeutics; 2010; Berlin, Germany.
-
(2010)
Specific Tgf-Beta Receptor-I Inhibition Using LY364947 Impairs Signaling, Motility and Invasion in Parental and Multikinase Inhibitor-Resistant Hepatocarcinoma Cells
-
-
Garbay, D.1
Serova, M.2
Serrate, C.3
-
131
-
-
75449092617
-
Down-regulation of connective tissue growth factor by inhibition of transforming growth factor beta blocks the tumor-stroma cross-talk and tumor progression in hepatocellular carcinoma
-
Mazzocca A, Fransvea E, Dituri F, Lupo L, Antonaci S, Giannelli G. Down-regulation of connective tissue growth factor by inhibition of transforming growth factor beta blocks the tumor-stroma cross-talk and tumor progression in hepatocellular carcinoma. Hepatology. 2010;51(2):523–534.
-
(2010)
Hepatology
, vol.51
, Issue.2
, pp. 523-534
-
-
Mazzocca, A.1
Fransvea, E.2
Dituri, F.3
Lupo, L.4
Antonaci, S.5
Giannelli, G.6
-
132
-
-
79959599396
-
Kinase activation profile associated with TGF-beta-dependent migration of HCC cells: A preclinical study
-
Fransvea E, Mazzocca A, Santamato A, Azzariti A, Antonaci S, Giannelli G. Kinase activation profile associated with TGF-beta-dependent migration of HCC cells: a preclinical study. Cancer Chemother Pharmacol. 2011;68(1):79–86.
-
(2011)
Cancer Chemother Pharmacol
, vol.68
, Issue.1
, pp. 79-86
-
-
Fransvea, E.1
Mazzocca, A.2
Santamato, A.3
Azzariti, A.4
Antonaci, S.5
Giannelli, G.6
-
133
-
-
79251633236
-
Inhibiting TGF-beta signaling in hepatocellular carcinoma
-
Giannelli G, Mazzocca A, Fransvea E, Lahn M, Antonaci S. Inhibiting TGF-beta signaling in hepatocellular carcinoma. Biochim Biophys Acta. 2011;1815(2):214–223.
-
(2011)
Biochim Biophys Acta
, vol.1815
, Issue.2
, pp. 214-223
-
-
Giannelli, G.1
Mazzocca, A.2
Fransvea, E.3
Lahn, M.4
Antonaci, S.5
-
134
-
-
84939828079
-
-
Presented at: 104th annual meeting of the American Association for Cancer Research; April 6–10, Washington, DC, Philadelphia (PA). Abstract
-
Serova M, Tijeras-Raballand A, Dos Santos C, et al. Effects of TGF-beta signaling inhibition with LY2157299 in hepatocarcinoma models and in ex vivo whole tumor tissue samples from patient specimen. Presented at: 104th annual meeting of the American Association for Cancer Research; April 6–10; 2013; Washington, DC, Philadelphia (PA). Abstract 2094.
-
(2013)
Effects of Tgf-Beta Signaling Inhibition with LY2157299 in Hepatocarcinoma Models and in Ex Vivo Whole Tumor Tissue Samples from Patient Specimen
-
-
Serova, M.1
Tijeras-Raballand, A.2
Dos Santos, C.3
-
135
-
-
84939828080
-
-
Presented at: International Liver Cancer Association (ILCA) Annual Conference, 2014; Kyoto; Japan. Abstract P-005
-
Tijeras-Raballand A, Serova M, Neuzillet C, et al. LY2157299 w/wo sorafenib in hepatocarcinomas yields antitumor effects in transgenic mice and xenografts, also inhibiting Tgf-Β signalling in freshly-grown sliced tumor specimens. Presented at: International Liver Cancer Association (ILCA) Annual Conference, 2014; Kyoto; Japan. Abstract P-005.
-
LY2157299 W/Wo Sorafenib in Hepatocarcinomas Yields Antitumor Effects in Transgenic Mice and Xenografts, also Inhibiting Tgf-Β Signalling in Freshly-Grown Sliced Tumor Specimens
-
-
Tijeras-Raballand, A.1
Serova, M.2
Neuzillet, C.3
-
136
-
-
84874251938
-
Sorafenib reduces hepatic infiltrated regulatory T cells in hepatocellular carcinoma patients by suppressing TGF-beta signal
-
Wang Q, Yu T, Yuan Y, et al. Sorafenib reduces hepatic infiltrated regulatory T cells in hepatocellular carcinoma patients by suppressing TGF-beta signal. J Surg Oncol. 2013;107(4):422–427.
-
(2013)
J Surg Oncol
, vol.107
, Issue.4
, pp. 422-427
-
-
Wang, Q.1
Yu, T.2
Yuan, Y.3
-
138
-
-
84939828082
-
-
Presented at: AACR-NCI-EORTC International Conference on Molecular Targets and Cancer Therapeutics; November 12–16; 2011; San Francisco, CA.Mol Cancer Ther. Abstract Number B175
-
Serova M, Riveiro ME, de Gramont A, et al. TGF-β-RI kinase inhibitors, LY2157299 and LY364947, decrease motility and invasion in hepatocarcinoma (HCC) cells developing resistance to VEGFR/PDGFR kinase inhibitors. Presented at: AACR-NCI-EORTC International Conference on Molecular Targets and Cancer Therapeutics; November 12–16; 2011; San Francisco, CA. Mol Cancer Ther. Abstract Number B175.
-
TGF-β-RI Kinase Inhibitors, LY2157299 and LY364947, Decrease Motility and Invasion in Hepatocarcinoma (HCC) Cells Developing Resistance to VEGFR/PDGFR Kinase Inhibitors
-
-
Serova, M.1
Riveiro, M.E.2
De Gramont, A.3
-
139
-
-
84939795587
-
-
NLM identifier: NCT01246986. Accessed March 3, 2015
-
Eli Lilly and Company. Phase 2 study of LY2157299 in patients with hepatocellular carcinoma. Available from: https://clinicaltrials.gov/ct2/show/NCT01246986?term=NCT01246986&rank=1. NLM identifier: NCT01246986. Accessed March 3, 2015.
-
Phase 2 Study of LY2157299 in Patients with Hepatocellular Carcinoma
-
-
-
140
-
-
84939828083
-
-
International Liver Cancer Association) Annual Conference, Washington, DC, USA
-
Giannelli G, Santoro A, Kelley RK, et al. Phase 2 study of the oral transforming growth factor-beta (TGF-beta) receptor I kinase inhibitor LY2157299. Presented at: 7th ILCA (International Liver Cancer Association) Annual Conference; 2013; Washington, DC, USA.
-
(2013)
Phase 2 Study of the Oral Transforming Growth Factor-Beta (Tgf-Beta) Receptor I Kinase Inhibitor LY2157299. Presented At: 7Th ILCA
-
-
Giannelli, G.1
Santoro, A.2
Kelley, R.K.3
-
141
-
-
84939828084
-
-
Presented at: Gastrointestinal Cancers Symposium, San Francisco, CA
-
Faivre S, Santoro A, Kelley RK, et al. A Phase 2 study of a novel transforming growth factor-beta (TGF-β) receptor I kinase inhibitor, LY2157299 monohydrate, in patients with advanced hepatocellular carcinoma (HCC). Presented at: Gastrointestinal Cancers Symposium; 2014; San Francisco, CA.
-
(2014)
A Phase 2 Study of a Novel Transforming Growth Factor-Beta (TGF-β) Receptor I Kinase Inhibitor, LY2157299 Monohydrate, in Patients with Advanced Hepatocellular Carcinoma (HCC)
-
-
Faivre, S.1
Santoro, A.2
Kelley, R.K.3
-
142
-
-
35348901453
-
Basics of TGF-beta and pancreatic cancer
-
Truty MJ, Urrutia R. Basics of TGF-beta and pancreatic cancer. Pancreatology. 2007;7(5–6):423–435.
-
(2007)
Pancreatology
, vol.7
, Issue.5-6
, pp. 423-435
-
-
Truty, M.J.1
Urrutia, R.2
-
143
-
-
42249099019
-
LY2109761, a novel transforming growth factor beta receptor type I and type II dual inhibitor, as a therapeutic approach to suppressing pancreatic cancer metastasis
-
Melisi D, Ishiyama S, Sclabas GM, et al. LY2109761, a novel transforming growth factor beta receptor type I and type II dual inhibitor, as a therapeutic approach to suppressing pancreatic cancer metastasis. Mol Cancer Ther. 2008;7(4):829–840.
-
(2008)
Mol Cancer Ther
, vol.7
, Issue.4
, pp. 829-840
-
-
Melisi, D.1
Ishiyama, S.2
Sclabas, G.M.3
-
144
-
-
70350218798
-
TrkBT1 induces liver metastasis of pancreatic cancer cells by sequestering Rho GDP dissociation inhibitor and promoting RhoA activation
-
Li Z, Chang Z, Chiao LJ, et al. TrkBT1 induces liver metastasis of pancreatic cancer cells by sequestering Rho GDP dissociation inhibitor and promoting RhoA activation. Cancer Res. 2009;69(19):7851–7859.
-
(2009)
Cancer Res
, vol.69
, Issue.19
, pp. 7851-7859
-
-
Li, Z.1
Chang, Z.2
Chiao, L.J.3
-
145
-
-
80755141299
-
Nodal/Activin signaling drives self-renewal and tumorigenicity of pancreatic cancer stem cells and provides a target for combined drug therapy
-
Lonardo E, Hermann PC, Mueller MT, et al. Nodal/Activin signaling drives self-renewal and tumorigenicity of pancreatic cancer stem cells and provides a target for combined drug therapy. Cell Stem Cell. 2011;9(5):433–446.
-
(2011)
Cell Stem Cell
, vol.9
, Issue.5
, pp. 433-446
-
-
Lonardo, E.1
Hermann, P.C.2
Mueller, M.T.3
-
146
-
-
84907494552
-
Neutralizing murine TGFbetaR2 promotes a differentiated tumor cell phenotype and inhibits pancreatic cancer metastasis
-
Ostapoff KT, Cenik BK, Wang M, et al. Neutralizing murine TGFbetaR2 promotes a differentiated tumor cell phenotype and inhibits pancreatic cancer metastasis. Cancer Res. 2014;74(18):4996–5007.
-
(2014)
Cancer Res
, vol.74
, Issue.18
, pp. 4996-5007
-
-
Ostapoff, K.T.1
Cenik, B.K.2
Wang, M.3
-
148
-
-
54049149411
-
Inhibition of the TGF-beta receptor I kinase promotes hematopoiesis in MDS
-
Zhou L, Nguyen AN, Sohal D, et al. Inhibition of the TGF-beta receptor I kinase promotes hematopoiesis in MDS. Blood. 2008;112(8):3434–3443.
-
(2008)
Blood
, vol.112
, Issue.8
, pp. 3434-3443
-
-
Zhou, L.1
Nguyen, A.N.2
Sohal, D.3
-
149
-
-
79551518231
-
Reduced SMAD7 leads to overactivation of TGF-beta signaling in MDS that can be reversed by a specific inhibitor of TGF-beta receptor I kinase
-
Zhou L, McMahon C, Bhagat T, et al. Reduced SMAD7 leads to overactivation of TGF-beta signaling in MDS that can be reversed by a specific inhibitor of TGF-beta receptor I kinase. Cancer Res. 2011;71(3):955–963.
-
(2011)
Cancer Res
, vol.71
, Issue.3
, pp. 955-963
-
-
Zhou, L.1
McMahon, C.2
Bhagat, T.3
-
151
-
-
47249119717
-
TGF-beta receptor kinase inhibitor LY2109761 reverses the anti-apoptotic effects of TGF-beta1 in myelo-monocytic leukaemic cells co-cultured with stromal cells
-
Xu Y, Tabe Y, Jin L, Watt J, et al. TGF-beta receptor kinase inhibitor LY2109761 reverses the anti-apoptotic effects of TGF-beta1 in myelo-monocytic leukaemic cells co-cultured with stromal cells. Br J Haematol. 2008;142(2):192–201.
-
(2008)
Br J Haematol
, vol.142
, Issue.2
, pp. 192-201
-
-
Xu, Y.1
Tabe, Y.2
Jin, L.3
Watt, J.4
-
152
-
-
84877607466
-
TGFbeta restores hematopoietic homeostasis after myelosuppressive chemotherapy
-
Brenet F, Kermani P, Spektor R, Rafii S, Scandura JM. TGFbeta restores hematopoietic homeostasis after myelosuppressive chemotherapy. J Exp Med. 2013;210(3):623–639.
-
(2013)
J Exp Med
, vol.210
, Issue.3
, pp. 623-639
-
-
Brenet, F.1
Kermani, P.2
Spektor, R.3
Rafii, S.4
Scandura, J.M.5
-
153
-
-
84939815403
-
-
Presented at: AACR Meeting, Los Angeles, CA. Abstract
-
Ge R, Kang Y, McPherson J, Yingling J, Reiss M. Transforming growth factor β pathway antagonists inhibit human breast cancer metastases to lung and bone. Presented at: AACR Meeting; 2007; Los Angeles, CA. Abstract 2231.
-
(2007)
Transforming Growth Factor β Pathway Antagonists Inhibit Human Breast Cancer Metastases to Lung and Bone
-
-
Ge, R.1
Kang, Y.2
McPherson, J.3
Yingling, J.4
Reiss, M.5
-
154
-
-
84874106140
-
Combined treatment with erlotinib and a transforming growth factor-beta type I receptor inhibitor effectively suppresses the enhanced motility of erlotinib-resistant non-small-cell lung cancer cells
-
Serizawa M, Takahashi T, Yamamoto N, Koh Y. Combined treatment with erlotinib and a transforming growth factor-beta type I receptor inhibitor effectively suppresses the enhanced motility of erlotinib-resistant non-small-cell lung cancer cells. J Thorac Oncol. 2013;8(3):259–269.
-
(2013)
J Thorac Oncol
, vol.8
, Issue.3
, pp. 259-269
-
-
Serizawa, M.1
Takahashi, T.2
Yamamoto, N.3
Koh, Y.4
-
155
-
-
84890435497
-
TGF-beta specifically enhances the metastatic attributes of murine lung adenocarcinoma: Implications for human non-small cell lung cancer
-
Vazquez PF, Carlini MJ, Daroqui MC, et al. TGF-beta specifically enhances the metastatic attributes of murine lung adenocarcinoma: implications for human non-small cell lung cancer. Clin Exp Metastasis. 2013;30(8):993–1007.
-
(2013)
Clin Exp Metastasis
, vol.30
, Issue.8
, pp. 993-1007
-
-
Vazquez, P.F.1
Carlini, M.J.2
Daroqui, M.C.3
-
156
-
-
84887989710
-
Colorectal cancer intrinsic subtypes predict chemotherapy benefit, deficient mismatch repair and epithelial-to-mesenchymal transition
-
Roepman P, Schlicker A, Tabernero J, et al. Colorectal cancer intrinsic subtypes predict chemotherapy benefit, deficient mismatch repair and epithelial-to-mesenchymal transition. Int J Cancer. 2014;134(3):552–562.
-
(2014)
Int J Cancer
, vol.134
, Issue.3
, pp. 552-562
-
-
Roepman, P.1
Schlicker, A.2
Tabernero, J.3
-
157
-
-
84869021181
-
Dependency of colorectal cancer on a TGF-beta-driven program in stromal cells for metastasis initiation
-
Calon A, Espinet E, Palomo-Ponce S, et al. Dependency of colorectal cancer on a TGF-beta-driven program in stromal cells for metastasis initiation. Cancer Cell. 2012;22(5):571–584.
-
(2012)
Cancer Cell
, vol.22
, Issue.5
, pp. 571-584
-
-
Calon, A.1
Espinet, E.2
Palomo-Ponce, S.3
-
158
-
-
0023676353
-
Transforming growth factor beta: Potential autocrine growth inhibitor of estrogen receptor-negative human breast cancer cells
-
Arteaga CL, Tandon AK, Von Hoff DD, Osborne CK. Transforming growth factor beta: potential autocrine growth inhibitor of estrogen receptor-negative human breast cancer cells. Cancer Res. 1988;48(14):3898–3904.
-
(1988)
Cancer Res
, vol.48
, Issue.14
, pp. 3898-3904
-
-
Arteaga, C.L.1
Tandon, A.K.2
Von Hoff, D.D.3
Osborne, C.K.4
-
159
-
-
0027137485
-
Anti-transforming growth factor (TGF)-beta antibodies inhibit breast cancer cell tumorigenicity and increase mouse spleen natural killer cell activity. Implications for a possible role of tumor cell/host TGF-beta interactions in human breast cancer progression
-
Arteaga CL, Hurd SD, Winnier AR, Johnson MD, Fendly BM, Forbes JT. Anti-transforming growth factor (TGF)-beta antibodies inhibit breast cancer cell tumorigenicity and increase mouse spleen natural killer cell activity. Implications for a possible role of tumor cell/host TGF-beta interactions in human breast cancer progression. J Clin Invest. 1993;92(6):2569–2576.
-
(1993)
J Clin Invest
, vol.92
, Issue.6
, pp. 2569-2576
-
-
Arteaga, C.L.1
Hurd, S.D.2
Winnier, A.R.3
Johnson, M.D.4
Fendly, B.M.5
Forbes, J.T.6
-
160
-
-
0030793645
-
Transforming growth factor-beta in breast cancer: A working hypothesis
-
Reiss M, Barcellos-Hoff MH. Transforming growth factor-beta in breast cancer: a working hypothesis. Breast Cancer Res Treat. 1997;45(1):81–95.
-
(1997)
Breast Cancer Res Treat
, vol.45
, Issue.1
, pp. 81-95
-
-
Reiss, M.1
Barcellos-Hoff, M.H.2
-
161
-
-
68349160814
-
Imaging transforming growth factor-beta signaling dynamics and therapeutic response in breast cancer bone metastasis
-
Korpal M, Yan J, Lu X, Xu S, Lerit DA, Kang Y. Imaging transforming growth factor-beta signaling dynamics and therapeutic response in breast cancer bone metastasis. Nat Med. 2009;15(8):960–966.
-
(2009)
Nat Med
, vol.15
, Issue.8
, pp. 960-966
-
-
Korpal, M.1
Yan, J.2
Lu, X.3
Xu, S.4
Lerit, D.A.5
Kang, Y.6
-
162
-
-
32944460413
-
Transforming growth factor-beta receptor inhibition enhances adenoviral infectability of carcinoma cells via up-regulation of coxsackie and adenovirus receptor in conjunction with reversal of epithelial-mesenchymal transition
-
Lacher MD, Tiirikainen MI, Saunier EF, et al. Transforming growth factor-beta receptor inhibition enhances adenoviral infectability of carcinoma cells via up-regulation of coxsackie and adenovirus receptor in conjunction with reversal of epithelial-mesenchymal transition. Cancer Res. 2006;66(3):1648–1657.
-
(2006)
Cancer Res
, vol.66
, Issue.3
, pp. 1648-1657
-
-
Lacher, M.D.1
Tiirikainen, M.I.2
Saunier, E.F.3
-
163
-
-
67349091089
-
Transforming growth factor-beta signaling: Emerging stem cell target in metastatic breast cancer?
-
Tan AR, Alexe G, Reiss M. Transforming growth factor-beta signaling: emerging stem cell target in metastatic breast cancer? Breast Cancer Res Treat. 2009;115(3):453–495.
-
(2009)
Breast Cancer Res Treat
, vol.115
, Issue.3
, pp. 453-495
-
-
Tan, A.R.1
Alexe, G.2
Reiss, M.3
-
164
-
-
77952609184
-
Targeting the transforming growth factor-beta pathway inhibits human basal-like breast cancer metastasis
-
Ganapathy V, Ge R, Grazioli A, et al. Targeting the transforming growth factor-beta pathway inhibits human basal-like breast cancer metastasis. Mol Cancer. 2010;9:122.
-
(2010)
Mol Cancer
, vol.9
-
-
Ganapathy, V.1
Ge, R.2
Grazioli, A.3
-
165
-
-
84939806801
-
Transforming growth factor beta engages TACE/ADAM17 and ErbB3 to activate PI3K/Akt in HER2-overexpressing breast cancer and desensitizes cells to trastuzumab. Presented at: CTRC-AACR San Antonio Breast Cancer Symposium; San Antonio, CA
-
Wang E, Xiang B, Olivares M, Chung C, Arteaga C. Transforming growth factor beta engages TACE/ADAM17 and ErbB3 to activate PI3K/Akt in HER2-overexpressing breast cancer and desensitizes cells to trastuzumab. Presented at: CTRC-AACR San Antonio Breast Cancer Symposium; San Antonio, CA. Cancer Res. 2008
-
(2008)
Cancer Res
-
-
Wang, E.1
Xiang, B.2
Olivares, M.3
Chung, C.4
Arteaga, C.5
-
166
-
-
77953479867
-
Oncogenic mutations regulate tumor microenvironment through induction of growth factors and angiogenic mediators
-
Wang SE, Yu Y, Criswell TL, et al. Oncogenic mutations regulate tumor microenvironment through induction of growth factors and angiogenic mediators. Oncogene. 2010;29(23):3335–3348.
-
(2010)
Oncogene
, vol.29
, Issue.23
, pp. 3335-3348
-
-
Wang, S.E.1
Yu, Y.2
Criswell, T.L.3
-
167
-
-
80054723100
-
BMP9 inhibits the proliferation and invasiveness of breast cancer cells MDA-MB-231
-
Wang K, Feng H, Ren W, et al. BMP9 inhibits the proliferation and invasiveness of breast cancer cells MDA-MB-231. J Cancer Res Clin Oncol. 2011;137(11):1687–1696.
-
(2011)
J Cancer Res Clin Oncol
, vol.137
, Issue.11
, pp. 1687-1696
-
-
Wang, K.1
Feng, H.2
Ren, W.3
-
169
-
-
79952771133
-
Outgrowth of drug-resistant carcinomas expressing markers of tumor aggression after long-term TβRI/II kinase inhibition with LY2109761
-
Connolly EC, Saunier EF, Quigley D, et al. Outgrowth of drug-resistant carcinomas expressing markers of tumor aggression after long-term TβRI/II kinase inhibition with LY2109761. Cancer Res. 2011;71(6):2339–2349.
-
(2011)
Cancer Res
, vol.71
, Issue.6
, pp. 2339-2349
-
-
Connolly, E.C.1
Saunier, E.F.2
Quigley, D.3
-
170
-
-
0035667565
-
Plasma levels of interleukin-6 and its soluble receptor are associated with prostate cancer progression and metastasis
-
Shariat SF, Andrews B, Kattan MW, Kim J, Wheeler TM, Slawin KM. Plasma levels of interleukin-6 and its soluble receptor are associated with prostate cancer progression and metastasis. Urology. 2001;58(6):1008–1015.
-
(2001)
Urology
, vol.58
, Issue.6
, pp. 1008-1015
-
-
Shariat, S.F.1
Rews, B.2
Kattan, M.W.3
Kim, J.4
Wheeler, T.M.5
Slawin, K.M.6
-
171
-
-
1642392553
-
Association of pre- and postoperative plasma levels of transforming growth factor beta(1) and interleukin 6 and its soluble receptor with prostate cancer progression
-
Shariat SF, Kattan MW, Traxel E, et al. Association of pre- and postoperative plasma levels of transforming growth factor beta(1) and interleukin 6 and its soluble receptor with prostate cancer progression. Clin Cancer Res. 2004;10(6):1992–1999.
-
(2004)
Clin Cancer Res
, vol.10
, Issue.6
, pp. 1992-1999
-
-
Shariat, S.F.1
Kattan, M.W.2
Traxel, E.3
-
172
-
-
79957461212
-
Tumor markers in prostate cancer I: Blood-based markers
-
Shariat SF, Semjonow A, Lilja H, Savage C, Vickers AJ, Bjartell A. Tumor markers in prostate cancer I: blood-based markers. Acta Oncol. 2011;50 Suppl 1:61–75.
-
(2011)
Acta Oncol
, vol.50
, pp. 61-75
-
-
Shariat, S.F.1
Semjonow, A.2
Lilja, H.3
Savage, C.4
Vickers, A.J.5
Bjartell, A.6
-
173
-
-
84856977508
-
Effect of transforming growth factor beta (TGF-beta) receptor I kinase inhibitor on prostate cancer bone growth
-
Wan X, Li ZG, Yingling JM, Yang J, et al. Effect of transforming growth factor beta (TGF-beta) receptor I kinase inhibitor on prostate cancer bone growth. Bone. 2012;50(3):695–703.
-
(2012)
Bone
, vol.50
, Issue.3
, pp. 695-703
-
-
Wan, X.1
Li, Z.G.2
Yingling, J.M.3
Yang, J.4
-
174
-
-
84939828086
-
Role of cytokine-induced plasticity in melanoma on invasive, therapy-resistant cells that express EMT-related genes and pathways. Poster presented at ASCO Annual Meeting; 2012; Chicago. IL
-
Abstract 8542
-
Cebon JS, Anaka M, Hudson C, et al. Role of cytokine-induced plasticity in melanoma on invasive, therapy-resistant cells that express EMT-related genes and pathways. Poster presented at ASCO Annual Meeting; 2012; Chicago. IL. J Clin Oncol. Abstract 8542.
-
J Clin Oncol
-
-
Cebon, J.S.1
Anaka, M.2
Hudson, C.3
-
175
-
-
84897531613
-
Reversible and adaptive resistance to BRAF(V600E) inhibition in melanoma
-
Sun C, Wang L, Huang S, et al. Reversible and adaptive resistance to BRAF(V600E) inhibition in melanoma. Nature. 2014;508(7494):118–122.
-
(2014)
Nature
, vol.508
, Issue.7494
, pp. 118-122
-
-
Sun, C.1
Wang, L.2
Huang, S.3
-
176
-
-
84939828087
-
Combinatorial TGF-beta signaling blockade and anti-CTLA4 antibody immunotherapy in a murine BRAFV600E-PTEN-/- transgenic model of melanoma. Presented at: ASCO Annual Meeting; 2014; Chicago, IL
-
Abstract 3011
-
Hanks BA, Holtzhausen A, Evans K, Heid M, Blobe GC. Combinatorial TGF-beta signaling blockade and anti-CTLA4 antibody immunotherapy in a murine BRAFV600E-PTEN-/- transgenic model of melanoma. Presented at: ASCO Annual Meeting; 2014; Chicago, IL. J Clin Oncol. Abstract 3011.
-
J Clin Oncol
-
-
Hanks, B.A.1
Holtzhausen, A.2
Evans, K.3
Heid, M.4
Blobe, G.C.5
-
177
-
-
24944580634
-
Regulatory T cells and cytokines in malignant pleural effusions secondary to mesothelioma and carcinoma
-
DeLong P, Carroll RG, Henry AC, et al. Regulatory T cells and cytokines in malignant pleural effusions secondary to mesothelioma and carcinoma. Cancer Biol Ther. 2005;4(3):342–346.
-
(2005)
Cancer Biol Ther
, vol.4
, Issue.3
, pp. 342-346
-
-
Delong, P.1
Carroll, R.G.2
Henry, A.C.3
-
178
-
-
34248185926
-
Inhibition of TGF-beta with neutralizing antibodies prevents radiation-induced acceleration of metastatic cancer progression
-
Biswas S, Guix M, Rinehart C, et al. Inhibition of TGF-beta with neutralizing antibodies prevents radiation-induced acceleration of metastatic cancer progression. J Clin Invest. 2007;117(5):1305–1313.
-
(2007)
J Clin Invest
, vol.117
, Issue.5
, pp. 1305-1313
-
-
Biswas, S.1
Guix, M.2
Rinehart, C.3
-
179
-
-
0032527651
-
Plasma transforming growth factor beta1 as a predictor of radiation pneumonitis
-
Anscher MS, Kong FM, Andrews K, et al. Plasma transforming growth factor beta1 as a predictor of radiation pneumonitis. Int J Radiat Oncol Biol Phys. 1998;41(5):1029–1035.
-
(1998)
Int J Radiat Oncol Biol Phys
, vol.41
, Issue.5
, pp. 1029-1035
-
-
Anscher, M.S.1
Kong, F.M.2
Rews, K.3
-
180
-
-
77956489582
-
TGF-β receptor kinase inhibitors for the treatment of fibrosis
-
Dijke P, Heldin C-H, editors
-
Laping N, Huet S. TGF-β receptor kinase inhibitors for the treatment of fibrosis. In: Dijke P, Heldin C-H, editors. Smad Signal Transduction: Smads in Proliferation, Differentiation and Disease. the Netherlands: Springer Verlag; 2006:443–459.
-
(2006)
Smad Signal Transduction: Smads in Proliferation, Differentiation and Disease. The Netherlands: Springer Verlag
, pp. 443-459
-
-
Laping, N.1
Huet, S.2
-
181
-
-
84863325122
-
LY2109761 attenuates radiation-induced pulmonary murine fibrosis via reversal of TGF-beta and BMP-associated proinflammatory and proangiogenic signals
-
Flechsig P, Dadrich M, Bickelhaupt S, et al. LY2109761 attenuates radiation-induced pulmonary murine fibrosis via reversal of TGF-beta and BMP-associated proinflammatory and proangiogenic signals. Clin Cancer Res. 2012;18(13):3616–3627.
-
(2012)
Clin Cancer Res
, vol.18
, Issue.13
, pp. 3616-3627
-
-
Flechsig, P.1
Dadrich, M.2
Bickelhaupt, S.3
|