-
1
-
-
30944447568
-
The extracellular signal-regulated kinase: multiple substrates regulate diverse cellular functions
-
Yoon S, Seger R, (2006) The extracellular signal-regulated kinase: multiple substrates regulate diverse cellular functions. Growth Factors 24: 21-44.
-
(2006)
Growth Factors
, vol.24
, pp. 21-44
-
-
Yoon, S.1
Seger, R.2
-
2
-
-
34248583886
-
MAP kinase signalling pathways in cancer
-
Dhillon AS, Hagan S, Rath O, Kolch W, (2007) MAP kinase signalling pathways in cancer. Oncogene 26: 3279-3290.
-
(2007)
Oncogene
, vol.26
, pp. 3279-3290
-
-
Dhillon, A.S.1
Hagan, S.2
Rath, O.3
Kolch, W.4
-
3
-
-
68949086867
-
Targeting the RAF-MEK-ERK pathway in cancer therapy
-
Montagut C, Settleman J, (2009) Targeting the RAF-MEK-ERK pathway in cancer therapy. Cancer Lett 283: 125-134.
-
(2009)
Cancer Lett
, vol.283
, pp. 125-134
-
-
Montagut, C.1
Settleman, J.2
-
4
-
-
67649770887
-
Ras signaling and therapies
-
Young A, Lyons J, Miller AL, Phan VT, Alarcon IR, et al. (2009) Ras signaling and therapies. Adv Cancer Res 102: 1-17.
-
(2009)
Adv Cancer Res
, vol.102
, pp. 1-17
-
-
Young, A.1
Lyons, J.2
Miller, A.L.3
Phan, V.T.4
Alarcon, I.R.5
-
5
-
-
80052536175
-
New drugs in melanoma: it's a whole new world
-
Eggermont AM, Robert C, (2011) New drugs in melanoma: it's a whole new world. Eur J Cancer 47: 2150-2157.
-
(2011)
Eur J Cancer
, vol.47
, pp. 2150-2157
-
-
Eggermont, A.M.1
Robert, C.2
-
6
-
-
18444374405
-
Mutations of the BRAF gene in human cancer
-
Davies H, Bignell GR, Cox C, Stephens P, Edkins S, et al. (2002) Mutations of the BRAF gene in human cancer. Nature 417: 949-954.
-
(2002)
Nature
, vol.417
, pp. 949-954
-
-
Davies, H.1
Bignell, G.R.2
Cox, C.3
Stephens, P.4
Edkins, S.5
-
8
-
-
12144289677
-
Mechanism of activation of the RAF-ERK signaling pathway by oncogenic mutations of B-RAF
-
Wan PT, Garnett MJ, Roe SM, Lee S, Niculescu-Duvaz D, et al. (2004) Mechanism of activation of the RAF-ERK signaling pathway by oncogenic mutations of B-RAF. Cell 116: 855-867.
-
(2004)
Cell
, vol.116
, pp. 855-867
-
-
Wan, P.T.1
Garnett, M.J.2
Roe, S.M.3
Lee, S.4
Niculescu-Duvaz, D.5
-
9
-
-
55749088393
-
Preclinical overview of sorafenib, a multikinase inhibitor that targets both Raf and VEGF and PDGF receptor tyrosine kinase signaling
-
Wilhelm SM, Adnane L, Newell P, Villanueva A, Llovet JM, et al. (2008) Preclinical overview of sorafenib, a multikinase inhibitor that targets both Raf and VEGF and PDGF receptor tyrosine kinase signaling. Mol Cancer Ther 7: 3129-3140.
-
(2008)
Mol Cancer Ther
, vol.7
, pp. 3129-3140
-
-
Wilhelm, S.M.1
Adnane, L.2
Newell, P.3
Villanueva, A.4
Llovet, J.M.5
-
10
-
-
77956513286
-
Clinical efficacy of a RAF inhibitor needs broad target blockade in BRAF-mutant melanoma
-
Bollag G, Hirth P, Tsai J, Zhang J, Ibrahim PN, et al. (2010) Clinical efficacy of a RAF inhibitor needs broad target blockade in BRAF-mutant melanoma. Nature 467: 596-599.
-
(2010)
Nature
, vol.467
, pp. 596-599
-
-
Bollag, G.1
Hirth, P.2
Tsai, J.3
Zhang, J.4
Ibrahim, P.N.5
-
11
-
-
77957350123
-
Phase I/II study of GSK2118436, a selective inhibitor of oncogenic mutant BRAF kinase, in patients with metastatic melanoma and other solid tumors
-
abstr 8503
-
Kefford R, Arkenau H, Brown MP, Millward M, Infante JR, et al. (2010) Phase I/II study of GSK2118436, a selective inhibitor of oncogenic mutant BRAF kinase, in patients with metastatic melanoma and other solid tumors. J Clin Oncol 28(15 suppl): abstr 8503.
-
(2010)
J Clin Oncol
, vol.28
, Issue.15 SUPPL.
-
-
Kefford, R.1
Arkenau, H.2
Brown, M.P.3
Millward, M.4
Infante, J.R.5
-
12
-
-
84978034236
-
Prognostic and clinicopathologic associations of oncogenic BRAF in metastatic melanoma
-
Long GV, Menzies AM, Nagrial AM, Haydu LE, Hamilton AL, et al. (2011) Prognostic and clinicopathologic associations of oncogenic BRAF in metastatic melanoma. J Clin Oncol 29: 1239-1246.
-
(2011)
J Clin Oncol
, vol.29
, pp. 1239-1246
-
-
Long, G.V.1
Menzies, A.M.2
Nagrial, A.M.3
Haydu, L.E.4
Hamilton, A.L.5
-
13
-
-
80052539696
-
Results from the first-in-human (FIH) phase I study of the oral RAF inhibitor RAF265 administered daily to patients with advanced cutaneous melanoma
-
abstr 8508
-
Sharfman WH, Hodi FS, Lawrence DP, Flaherty KT, Amaravadi RK, et al. (2011) Results from the first-in-human (FIH) phase I study of the oral RAF inhibitor RAF265 administered daily to patients with advanced cutaneous melanoma. J Clin Oncol 29(15 suppl): abstr 8508.
-
(2011)
J Clin Oncol
, vol.29
, Issue.15 SUPPL.
-
-
Sharfman, W.H.1
Hodi, F.S.2
Lawrence, D.P.3
Flaherty, K.T.4
Amaravadi, R.K.5
-
14
-
-
45349101568
-
Multiple squamous cell carcinomas of the skin after therapy with sorafenib combined with tipifarnib
-
Hong DS, Reddy SB, Prieto VG, Wright JJ, Tannir NM, et al. (2008) Multiple squamous cell carcinomas of the skin after therapy with sorafenib combined with tipifarnib. Arch Dermatol 144: 779-782.
-
(2008)
Arch Dermatol
, vol.144
, pp. 779-782
-
-
Hong, D.S.1
Reddy, S.B.2
Prieto, V.G.3
Wright, J.J.4
Tannir, N.M.5
-
15
-
-
45349100306
-
Sorafenib-induced eruptive melanocytic lesions
-
Kong HH, Sibaud V, Chanco Turner ML, Foto J, Hornyak TJ, et al. (2008) Sorafenib-induced eruptive melanocytic lesions. Arch Dermatol 144: 820-822.
-
(2008)
Arch Dermatol
, vol.144
, pp. 820-822
-
-
Kong, H.H.1
Sibaud, V.2
Chanco Turner, M.L.3
Foto, J.4
Hornyak, T.J.5
-
16
-
-
65249127575
-
Cutaneous squamous cell carcinoma and inflammation of actinic keratoses associated with sorafenib
-
Dubauskas Z, Kunishige J, Prieto VG, Jonasch E, Hwu P, et al. (2009) Cutaneous squamous cell carcinoma and inflammation of actinic keratoses associated with sorafenib. Clin Genitourin Cancer 7: 20-23.
-
(2009)
Clin Genitourin Cancer
, vol.7
, pp. 20-23
-
-
Dubauskas, Z.1
Kunishige, J.2
Prieto, V.G.3
Jonasch, E.4
Hwu, P.5
-
17
-
-
68949094219
-
Keratoacanthomas and squamous cell carcinomas in patients receiving sorafenib
-
Arnault JP, Wechsler J, Escudier B, Spatz A, Tomasic G, et al. (2009) Keratoacanthomas and squamous cell carcinomas in patients receiving sorafenib. J Clin Oncol 27: e59-e61.
-
(2009)
J Clin Oncol
, vol.27
-
-
Arnault, J.P.1
Wechsler, J.2
Escudier, B.3
Spatz, A.4
Tomasic, G.5
-
18
-
-
67651246671
-
Phase I study of PLX4032: proof of concept for V600E BRAF mutation as a therapeutic target in human cancer
-
abstr 9000
-
Flaherty K, Puzanov I, Sosman J, Kim K, Ribas A, et al. (2009) Phase I study of PLX4032: proof of concept for V600E BRAF mutation as a therapeutic target in human cancer. J Clin Oncol 27(15 suppl): abstr 9000.
-
(2009)
J Clin Oncol
, vol.27
, Issue.15 SUPPL.
-
-
Flaherty, K.1
Puzanov, I.2
Sosman, J.3
Kim, K.4
Ribas, A.5
-
19
-
-
77949678177
-
Drug discovery: inhibitors that activate
-
Cichowski K, Jänne PA, (2010) Drug discovery: inhibitors that activate. Nature 464: 358-359.
-
(2010)
Nature
, vol.464
, pp. 358-359
-
-
Cichowski, K.1
Jänne, P.A.2
-
20
-
-
77949685981
-
RAF inhibitors prime wild-type RAF to activate the MAPK pathway and enhance growth
-
Hatzivassiliou G, Song K, Yen I, Brandhuber BJ, Anderson DJ, et al. (2010) RAF inhibitors prime wild-type RAF to activate the MAPK pathway and enhance growth. Nature 464: 431-435.
-
(2010)
Nature
, vol.464
, pp. 431-435
-
-
Hatzivassiliou, G.1
Song, K.2
Yen, I.3
Brandhuber, B.J.4
Anderson, D.J.5
-
21
-
-
74849109743
-
Kinase-dead BRAF and oncogenic RAS cooperate to drive tumor progression through CRAF
-
Heidorn SJ, Milagre C, Whittaker S, Nourry A, Niculescu-Duvas I, et al. (2010) Kinase-dead BRAF and oncogenic RAS cooperate to drive tumor progression through CRAF. Cell 140: 209-221.
-
(2010)
Cell
, vol.140
, pp. 209-221
-
-
Heidorn, S.J.1
Milagre, C.2
Whittaker, S.3
Nourry, A.4
Niculescu-Duvas, I.5
-
22
-
-
77949732073
-
RAF inhibitors transactivate RAF dimers and ERK signalling in cells with wild-type BRAF
-
Poulikakos PI, Zhang C, Bollag G, Shokat KM, Rosen N, (2010) RAF inhibitors transactivate RAF dimers and ERK signalling in cells with wild-type BRAF. Nature 464: 427-430.
-
(2010)
Nature
, vol.464
, pp. 427-430
-
-
Poulikakos, P.I.1
Zhang, C.2
Bollag, G.3
Shokat, K.M.4
Rosen, N.5
-
23
-
-
84875186930
-
Discovery of dabrafenib: A selective inhibitor of Raf kinases with anti-tumor activity against B-Raf-driven tumors
-
Rheault TR, Stellwagen JC, Adjabeng GM, Hornberger KR, Petrov KG, et al. (2013) Discovery of dabrafenib: A selective inhibitor of Raf kinases with anti-tumor activity against B-Raf-driven tumors. ACS Med Chem Lett 4: 358-362.
-
(2013)
ACS Med Chem Lett
, vol.4
, pp. 358-362
-
-
Rheault, T.R.1
Stellwagen, J.C.2
Adjabeng, G.M.3
Hornberger, K.R.4
Petrov, K.G.5
-
24
-
-
34447617694
-
An intrinsic ATPase activity of phospho-MEK-1 uncoupled from downstream ERK phosphorylation
-
Rominger CM, Schaber MD, Yang J, Gontarek RR, Weaver KL, et al. (2007) An intrinsic ATPase activity of phospho-MEK-1 uncoupled from downstream ERK phosphorylation. Arch Biochem Biophys 464: 130-137.
-
(2007)
Arch Biochem Biophys
, vol.464
, pp. 130-137
-
-
Rominger, C.M.1
Schaber, M.D.2
Yang, J.3
Gontarek, R.R.4
Weaver, K.L.5
-
25
-
-
0017714532
-
Flow microfluorometric analysis of nuclear DNA in cells from solid tumors and cell suspensions. A new method for rapid isolation and staining of nuclei
-
Vindeløv LL, (1977) Flow microfluorometric analysis of nuclear DNA in cells from solid tumors and cell suspensions. A new method for rapid isolation and staining of nuclei. Virchows Arch B Cell Pathol 24: 227-242.
-
(1977)
Virchows Arch B Cell Pathol
, vol.24
, pp. 227-242
-
-
Vindeløv, L.L.1
-
26
-
-
0141816881
-
Suppression of BRAF(V599E) in human melanoma abrogates transformation
-
Hingorani SR, Jacobetz MA, Robertson GP, Herlyn M, Tuveson DA, (2003) Suppression of BRAF(V599E) in human melanoma abrogates transformation. Cancer Res 63: 5198-5202.
-
(2003)
Cancer Res
, vol.63
, pp. 5198-5202
-
-
Hingorani, S.R.1
Jacobetz, M.A.2
Robertson, G.P.3
Herlyn, M.4
Tuveson, D.A.5
-
27
-
-
1942506706
-
V599EB-RAF is an oncogene in melanocytes
-
Wellbrock C, Ogilvie L, Hedley D, Karasarides M, Martin J, et al. (2004) V599EB-RAF is an oncogene in melanocytes. Cancer Res 64: 2338-2342.
-
(2004)
Cancer Res
, vol.64
, pp. 2338-2342
-
-
Wellbrock, C.1
Ogilvie, L.2
Hedley, D.3
Karasarides, M.4
Martin, J.5
-
28
-
-
84856217925
-
Concurrent loss of the PTEN and RB1 tumor suppressors attenuates RAF dependence in melanomas harboring (V600E)BRAF
-
Xing F, Persaud Y, Pratilas CA, Taylor BS, Janakiraman M, et al. (2012) Concurrent loss of the PTEN and RB1 tumor suppressors attenuates RAF dependence in melanomas harboring (V600E)BRAF. Oncogene 31: 446-457.
-
(2012)
Oncogene
, vol.31
, pp. 446-457
-
-
Xing, F.1
Persaud, Y.2
Pratilas, C.A.3
Taylor, B.S.4
Janakiraman, M.5
-
29
-
-
79952261716
-
GSK1120212 (JTP-74057) is an inhibitor of MEK activity and activation with favorable pharmacokinetic properties for sustained in vivo pathway inhibition
-
Gilmartin AG, Bleam MR, Groy A, Moss KG, Minthorn EA, et al. (2011) GSK1120212 (JTP-74057) is an inhibitor of MEK activity and activation with favorable pharmacokinetic properties for sustained in vivo pathway inhibition. Clin Cancer Res 17: 989-1000.
-
(2011)
Clin Cancer Res
, vol.17
, pp. 989-1000
-
-
Gilmartin, A.G.1
Bleam, M.R.2
Groy, A.3
Moss, K.G.4
Minthorn, E.A.5
-
30
-
-
84862908097
-
RAS mutations in cutaneous squamous-cell carcinomas in patients treated with BRAF inhibitors
-
Su F, Viros A, Milagre C, Trunzer K, Bollag G, et al. (2012) RAS mutations in cutaneous squamous-cell carcinomas in patients treated with BRAF inhibitors. New Engl J Med 366: 207-215.
-
(2012)
New Engl J Med
, vol.366
, pp. 207-215
-
-
Su, F.1
Viros, A.2
Milagre, C.3
Trunzer, K.4
Bollag, G.5
-
31
-
-
84879747901
-
Evaluation of N-acyl sulfonamide prodrug inhibitors of MEK kinase
-
2nd ACS National Meeting: abstr. MEDI 34
-
Ralph JM, Adams JL, Silva DJ, Feng Y, Martin PJ, et al. (2011) Evaluation of N-acyl sulfonamide prodrug inhibitors of MEK kinase. American Chemical Society; Division of Medicinal Chemistry, 242nd ACS National Meeting: abstr. MEDI 34.
-
(2011)
American Chemical Society; Division of Medicinal Chemistry
, pp. 24
-
-
Ralph, J.M.1
Adams, J.L.2
Silva, D.J.3
Feng, Y.4
Martin, P.J.5
-
32
-
-
77955475709
-
Selective and potent Raf inhibitors paradoxically stimulate normal cell proliferation and tumor growth
-
Carnahan J, Beltran PJ, Babij C, Le Q, Rose MJ, et al. (2010) Selective and potent Raf inhibitors paradoxically stimulate normal cell proliferation and tumor growth. Mol Cancer Ther 9: 2399-2410.
-
(2010)
Mol Cancer Ther
, vol.9
, pp. 2399-2410
-
-
Carnahan, J.1
Beltran, P.J.2
Babij, C.3
Le, Q.4
Rose, M.J.5
-
33
-
-
5444227865
-
Guilty as charged: B-RAF is a human oncogene
-
Garnett MJ, Marais R, (2004) Guilty as charged: B-RAF is a human oncogene. Cancer Cell 6: 313-319.
-
(2004)
Cancer Cell
, vol.6
, pp. 313-319
-
-
Garnett, M.J.1
Marais, R.2
-
34
-
-
4344584872
-
B-RAF is a therapeutic target in melanoma
-
Karasarides M, Chiloeches A, Hayward R, Niculescu-Duvaz D, Scanlon I, et al. (2004) B-RAF is a therapeutic target in melanoma. Oncogene 23: 6292-6298.
-
(2004)
Oncogene
, vol.23
, pp. 6292-6298
-
-
Karasarides, M.1
Chiloeches, A.2
Hayward, R.3
Niculescu-Duvaz, D.4
Scanlon, I.5
-
35
-
-
16844362816
-
Mutant V599EB-Raf regulates growth and vascular development of malignant melanoma tumors
-
Sharma A, Trivedi NR, Zimmerman MA, Tuveson DA, Smith CD, et al. (2005) Mutant V599EB-Raf regulates growth and vascular development of malignant melanoma tumors. Cancer Res 65: 2412-2421.
-
(2005)
Cancer Res
, vol.65
, pp. 2412-2421
-
-
Sharma, A.1
Trivedi, N.R.2
Zimmerman, M.A.3
Tuveson, D.A.4
Smith, C.D.5
-
36
-
-
33845730781
-
Demonstration of a genetic therapeutic index for tumors expressing oncogenic BRAF by the kinase inhibitor SB-590885
-
King AJ, Patrick DR, Batorsky RS, Ho ML, Do HT, et al. (2006) Demonstration of a genetic therapeutic index for tumors expressing oncogenic BRAF by the kinase inhibitor SB-590885. Cancer Res 66: 11100-11105.
-
(2006)
Cancer Res
, vol.66
, pp. 11100-11105
-
-
King, A.J.1
Patrick, D.R.2
Batorsky, R.S.3
Ho, M.L.4
Do, H.T.5
-
37
-
-
42949149240
-
Discovery of a selective inhibitor of oncogenic B-Raf kinase with potent antimelanoma activity
-
Tsai J, Lee JT, Wang W, Zhang J, Cho H, et al. (2008) Discovery of a selective inhibitor of oncogenic B-Raf kinase with potent antimelanoma activity. Proc Natl Acad Sci USA 105: 3041-3046.
-
(2008)
Proc Natl Acad Sci USA
, vol.105
, pp. 3041-3046
-
-
Tsai, J.1
Lee, J.T.2
Wang, W.3
Zhang, J.4
Cho, H.5
-
38
-
-
79953899480
-
Selective inhibition of oncogenic BRAF V600E/K/D by GSK2118436: evidence of clinical activity in subjects with metastatic melanoma
-
Kefford R, Long G, Arkenau HT, Brown MP, Millward M, et al. (2010) Selective inhibition of oncogenic BRAF V600E/K/D by GSK2118436: evidence of clinical activity in subjects with metastatic melanoma. Pigment Cell Melanoma Res 23: 874-1004.
-
(2010)
Pigment Cell Melanoma Res
, vol.23
, pp. 874-1004
-
-
Kefford, R.1
Long, G.2
Arkenau, H.T.3
Brown, M.P.4
Millward, M.5
-
39
-
-
79959795786
-
Improved survival with vemurafenib in melanoma with BRAF V600E mutation
-
Chapman PB, Hauschild A, Robert C, Haanen JB, Ascierto P, et al. (2011) Improved survival with vemurafenib in melanoma with BRAF V600E mutation. N Engl J Med 364: 2507-2516.
-
(2011)
N Engl J Med
, vol.364
, pp. 2507-2516
-
-
Chapman, P.B.1
Hauschild, A.2
Robert, C.3
Haanen, J.B.4
Ascierto, P.5
-
40
-
-
78650309875
-
COT drives resistance to RAF inhibition through MAP kinase pathway reactivation
-
Johannessen CM, Boehm JS, Kim SY, Thomas SR, Wardwell L, et al. (2010) COT drives resistance to RAF inhibition through MAP kinase pathway reactivation. Nature 468: 968-972.
-
(2010)
Nature
, vol.468
, pp. 968-972
-
-
Johannessen, C.M.1
Boehm, J.S.2
Kim, S.Y.3
Thomas, S.R.4
Wardwell, L.5
-
41
-
-
78650303507
-
Melanomas acquire resistance to B-RAF(V600E) inhibition by RTK or N-RAS upregulation
-
Nazarian R, Shi H, Wang Q, Kong X, Koya RC, et al. (2010) Melanomas acquire resistance to B-RAF(V600E) inhibition by RTK or N-RAS upregulation. Nature 468: 973-977.
-
(2010)
Nature
, vol.468
, pp. 973-977
-
-
Nazarian, R.1
Shi, H.2
Wang, Q.3
Kong, X.4
Koya, R.C.5
-
42
-
-
80053307869
-
Potential therapeutic strategies to overcome acquired resistance to BRAF or MEK inhibitors in BRAF mutant cancers
-
Corcoran RB, Settleman J, Engelman JA, (2011) Potential therapeutic strategies to overcome acquired resistance to BRAF or MEK inhibitors in BRAF mutant cancers. Oncotarget 2: 336-346.
-
(2011)
Oncotarget
, vol.2
, pp. 336-346
-
-
Corcoran, R.B.1
Settleman, J.2
Engelman, J.A.3
-
43
-
-
80051625929
-
Dissecting therapeutic resistance to RAF inhibition in melanoma by tumor genomic profiling
-
Wagle N, Emery C, Berger MF, Davis MJ, Sawyer A, et al. (2011) Dissecting therapeutic resistance to RAF inhibition in melanoma by tumor genomic profiling. J Clin Oncol 29: 3085-3096.
-
(2011)
J Clin Oncol
, vol.29
, pp. 3085-3096
-
-
Wagle, N.1
Emery, C.2
Berger, M.F.3
Davis, M.J.4
Sawyer, A.5
-
44
-
-
83455254767
-
RAF inhibitor resistance is mediated by dimerization of aberrantly spliced BRAF (V600E)
-
Poulikakos PI, Persaud Y, Janakiraman M, Kong X, Ng C, et al. (2011) RAF inhibitor resistance is mediated by dimerization of aberrantly spliced BRAF (V600E). Nature 480: 387-390.
-
(2011)
Nature
, vol.480
, pp. 387-390
-
-
Poulikakos, P.I.1
Persaud, Y.2
Janakiraman, M.3
Kong, X.4
Ng, C.5
-
45
-
-
84862908526
-
RAS mutations are associated with the development of cutaneous squamous cell tumors in patients treated with RAF inhibitors
-
Oberholzer PA, Kee D, Dziunycz P, Sucker A, Kamsukom N, et al. (2012) RAS mutations are associated with the development of cutaneous squamous cell tumors in patients treated with RAF inhibitors. J Clin Oncol 30: 316-321.
-
(2012)
J Clin Oncol
, vol.30
, pp. 316-321
-
-
Oberholzer, P.A.1
Kee, D.2
Dziunycz, P.3
Sucker, A.4
Kamsukom, N.5
-
46
-
-
84868224906
-
Combined BRAF and MEK inhibition in melanoma with BRAF V600 mutations
-
Flaherty KT, Infante JR, Daud A, Gonzalez R, Kefford RF, et al. (2012) Combined BRAF and MEK inhibition in melanoma with BRAF V600 mutations. N Engl J Med 367: 1694-1703.
-
(2012)
N Engl J Med
, vol.367
, pp. 1694-1703
-
-
Flaherty, K.T.1
Infante, J.R.2
Daud, A.3
Gonzalez, R.4
Kefford, R.F.5
|