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Volumn 4, Issue 3, 2012, Pages 315-328

Small-molecule ATP-competitive dual IGF-1R and insulin receptor inhibitors: Structural insights, chemical diversity and molecular evolution

Author keywords

[No Author keywords available]

Indexed keywords

BENZIMIDAZOLE DERIVATIVE; BMS 536924; BMS 695735; BMS 754807; GSK 1838705A; GSK 1904529A; IMIDAZOPYRAZINE DERIVATIVE; IMIDAZOPYRIDINE DERIVATIVE; INSULIN RECEPTOR; ISOQUINOLINE DERIVATIVE; LINSITINIB; PYRAZOLOPYRIMIDINE DERIVATIVE; PYRIDINE DERIVATIVE; PYRROLOPYRIMIDINE DERIVATIVE; SOMATOMEDIN B; SOMATOMEDIN C; SOMATOMEDIN RECEPTOR; UNCLASSIFIED DRUG;

EID: 84863239500     PISSN: 17568919     EISSN: 17568927     Source Type: Journal    
DOI: 10.4155/fmc.11.180     Document Type: Review
Times cited : (11)

References (64)
  • 1
    • 56749184290 scopus 로고    scopus 로고
    • Insulin and insulin-like growth factor signalling in neoplasia
    • Provides an overview of insulin and insulin-like growth factor signaling in neoplasia with a focus on recent findings relevant to cancer biology
    • Pollak M. Insulin and insulin-like growth factor signalling in neoplasia. Nat. Rev. Cancer 8, 915-928 (2008). Provides an overview of insulin and insulin-like growth factor signaling in neoplasia with a focus on recent findings relevant to cancer biology.
    • (2008) Nat. Rev. Cancer , vol.8 , pp. 915-928
    • Pollak, M.1
  • 2
    • 0038398622 scopus 로고    scopus 로고
    • The insulin-like growth factor system and cancer
    • LeRoith D, Roberts CT Jr. The insulin-like growth factor system and cancer. Cancer Lett. 195, 127-137 (2003).
    • (2003) Cancer Lett. , vol.195 , pp. 127-137
    • LeRoith, D.1    Roberts Jr., C.T.2
  • 3
    • 0027496895 scopus 로고
    • Mice carrying null mutations of the genes encoding insulin-like growth factor I (IGF-1) and type 1 IGF receptor (IGF1r)
    • Liu JP, Baker J, Perkins AS, Robertson EJ, Efstratiadis A. Mice carrying null mutations of the genes encoding insulin-like growth factor I (IGF-1) and type 1 IGF receptor (IGF1r). Cell 75, 59-72 (1993).
    • (1993) Cell , vol.75 , pp. 59-72
    • Liu, J.P.1    Baker, J.2    Perkins, A.S.3    Robertson, E.J.4    Efstratiadis, A.5
  • 4
    • 0027366338 scopus 로고
    • Simian virus 40 large tumor antigen is unable to transform mouse embryonic fibroblasts lacking type 1 insulin-like growth factor receptor
    • Sell C, Rubini M, Rubin R, Liu JP, Efstratiadis A, Baserga R. Simian virus 40 large tumor antigen is unable to transform mouse embryonic fibroblasts lacking type 1 insulin-like growth factor receptor. Proc. Natl Acad. Sci. USA 90, 11217-11221 (1993).
    • (1993) Proc. Natl Acad. Sci. USA , vol.90 , pp. 11217-11221
    • Sell, C.1    Rubini, M.2    Rubin, R.3    Liu, J.P.4    Efstratiadis, A.5    Baserga, R.6
  • 5
    • 0042515293 scopus 로고    scopus 로고
    • An anti-insulin-like growth factor I receptor antibody that is a potent inhibitor of cancer cell proliferation
    • Maloney EK, McLaughlin JL, Dagdigian NE et al. An anti-insulin-like growth factor I receptor antibody that is a potent inhibitor of cancer cell proliferation. Cancer Res. 63, 5073-5083 (2003).
    • (2003) Cancer Res. , vol.63 , pp. 5073-5083
    • Maloney, E.K.1    McLaughlin, J.L.2    Dagdigian, N.E.3
  • 6
    • 12144285705 scopus 로고    scopus 로고
    • In vivo antitumor activity of NVP-AEW541 - A novel, potent, and selective inhibitor of the IGF-IR kinase
    • Garcia-Echeverria C, Pearson MA, Marti A et al. In vivo antitumor activity of NVP-AEW541 - a novel, potent, and selective inhibitor of the IGF-IR kinase. Cancer Cell 5, 231-239 (2004).
    • (2004) Cancer Cell , vol.5 , pp. 231-239
    • Garcia-Echeverria, C.1    Pearson, M.A.2    Marti, A.3
  • 7
    • 20144386856 scopus 로고    scopus 로고
    • Combination therapy enhances the inhibition of tumor growth with the fully human anti-type 1 insulin-like growth factor receptor monoclonal antibody CP-751,871
    • Cohen BD, Baker DA, Soderstrom C et al. Combination therapy enhances the inhibition of tumor growth with the fully human anti-type 1 insulin-like growth factor receptor monoclonal antibody CP-751,871. Clin. Cancer Res. 11, 2063-2073 (2005).
    • (2005) Clin. Cancer Res. , vol.11 , pp. 2063-2073
    • Cohen, B.D.1    Baker, D.A.2    Soderstrom, C.3
  • 8
    • 51549115215 scopus 로고    scopus 로고
    • Targeting insulin and insulin-like growth factor signalling in oncology
    • Pollak M. Targeting insulin and insulin-like growth factor signalling in oncology. Curr. Opin. Pharmacol. 8, 384-392 (2008).
    • (2008) Curr. Opin. Pharmacol. , vol.8 , pp. 384-392
    • Pollak, M.1
  • 9
    • 0033906634 scopus 로고    scopus 로고
    • Structure and function of the type 1 insulin-like growth factor receptor
    • Adams TE, Epa VC, Garrett TP, Ward CW. Structure and function of the type 1 insulin-like growth factor receptor. Cell. Mol. Life Sci. 57, 1050-1093 (2000).
    • (2000) Cell. Mol. Life Sci. , vol.57 , pp. 1050-1093
    • Adams, T.E.1    Epa, V.C.2    Garrett, T.P.3    Ward, C.W.4
  • 10
    • 0037436509 scopus 로고    scopus 로고
    • Loss of IGF2 imprinting: A potential marker of colorectal cancer risk
    • Cui H, Cruz-Correa M, Giardiello FM et al. Loss of IGF2 imprinting: a potential marker of colorectal cancer risk. Science 299, 1753-1755 (2003).
    • (2003) Science , vol.299 , pp. 1753-1755
    • Cui, H.1    Cruz-Correa, M.2    Giardiello, F.M.3
  • 12
    • 0028356544 scopus 로고
    • Loss of imprinting of IGF2 is linked to reduced expression and abnormal methylation of H19 in Wilms' tumour
    • Steenman MJ, Rainier S, Dobry CJ, Grundy P, Horon IL, Feinberg AP. Loss of imprinting of IGF2 is linked to reduced expression and abnormal methylation of H19 in Wilms' tumour. Nat. Genet. 7, 433-439 (1994).
    • (1994) Nat. Genet. , vol.7 , pp. 433-439
    • Steenman, M.J.1    Rainier, S.2    Dobry, C.J.3    Grundy, P.4    Horon, I.L.5    Feinberg, A.P.6
  • 13
    • 59449098488 scopus 로고    scopus 로고
    • Molecular classification and prognostication of adrenocortical tumors by transcriptome profiling
    • Giordano TJ, Kuick R, Else T et al. Molecular classification and prognostication of adrenocortical tumors by transcriptome profiling. Clin. Cancer Res. 15, 668-676 (2009).
    • (2009) Clin. Cancer Res. , vol.15 , pp. 668-676
    • Giordano, T.J.1    Kuick, R.2    Else, T.3
  • 14
    • 0028906841 scopus 로고
    • Insulin receptor overexpression in 184B5 human mammary epithelial cells induces a ligand-dependent transformed phenotype
    • Frittitta L, Vigneri R, Stampfer MR, Goldfine ID. Insulin receptor overexpression in 184B5 human mammary epithelial cells induces a ligand-dependent transformed phenotype. J. Cell Biochem. 57, 666-669 (1995).
    • (1995) J. Cell Biochem. , vol.57 , pp. 666-669
    • Frittitta, L.1    Vigneri, R.2    Stampfer, M.R.3    Goldfine, I.D.4
  • 15
    • 0025865344 scopus 로고
    • Overexpression of insulin receptors in fibroblast and ovary cells induces a ligand- Mediated transformed phenotype
    • Giorgino F, Belfiore A, Milazzo G et al. Overexpression of insulin receptors in fibroblast and ovary cells induces a ligand- mediated transformed phenotype. Mol. Endocrinol. 5, 452-459 (1991).
    • (1991) Mol. Endocrinol. , vol.5 , pp. 452-459
    • Giorgino, F.1    Belfiore, A.2    Milazzo, G.3
  • 16
    • 0031238774 scopus 로고    scopus 로고
    • Growth-promoting interaction of IGF-II with the insulin receptor during mouse embryonic development
    • Louvi A, Accili D, Efstratiadis A. Growth-promoting interaction of IGF-II with the insulin receptor during mouse embryonic development. Dev. Biol. 189, 33-48 (1997).
    • (1997) Dev. Biol. , vol.189 , pp. 33-48
    • Louvi, A.1    Accili, D.2    Efstratiadis, A.3
  • 17
    • 0033561728 scopus 로고    scopus 로고
    • Insulin receptor activation by IGF-II in breast cancers: Evidence for a new autocrine/paracrine mechanism
    • Sciacca L, Costantino A, Pandini G et al. Insulin receptor activation by IGF-II in breast cancers: evidence for a new autocrine/paracrine mechanism. Oncogene 18, 2471-2479 (1999).
    • (1999) Oncogene , vol.18 , pp. 2471-2479
    • Sciacca, L.1    Costantino, A.2    Pandini, G.3
  • 18
    • 0030976615 scopus 로고    scopus 로고
    • Insulin-like growth factor II stimulates cell proliferation through the insulin receptor
    • Morrione A, Valentinis B, Xu SQ et al. Insulin-like growth factor II stimulates cell proliferation through the insulin receptor. Proc. Natl Acad. Sci. USA 94, 3777-3782 (1997).
    • (1997) Proc. Natl Acad. Sci. USA , vol.94 , pp. 3777-3782
    • Morrione, A.1    Valentinis, B.2    Xu, S.Q.3
  • 19
    • 0036721496 scopus 로고    scopus 로고
    • Functional insulin receptors on human epithelial ovarian carcinoma cells: Implications for IGF-II mitogenic signaling
    • Kalli KR, Falowo OI, Bale LK, Zschunke MA, Roche PC, Conover CA. Functional insulin receptors on human epithelial ovarian carcinoma cells: implications for IGF-II mitogenic signaling. Endocrinology 143, 3259-3267 (2002).
    • (2002) Endocrinology , vol.143 , pp. 3259-3267
    • Kalli, K.R.1    Falowo, O.I.2    Bale, L.K.3    Zschunke, M.A.4    Roche, P.C.5    Conover, C.A.6
  • 20
    • 0036148531 scopus 로고    scopus 로고
    • A novel autocrine loop involving IGF-II and the insulin receptor isoform-A stimulates growth of thyroid cancer
    • Studies compensatory crosstalk between IGF-1R and insulin receptor (IR) and provides rationale for co-targeting IGF-1R and IR in cancer treatment
    • Vella V, Pandini G, Sciacca L et al. A novel autocrine loop involving IGF-II and the insulin receptor isoform-A stimulates growth of thyroid cancer. J. Clin. Endocrinol. Metab. 87, 245-254 (2002). Studies compensatory crosstalk between IGF-1R and insulin receptor (IR) and provides rationale for co-targeting IGF-1R and IR in cancer treatment.
    • (2002) J. Clin. Endocrinol. Metab. , vol.87 , pp. 245-254
    • Vella, V.1    Pandini, G.2    Sciacca, L.3
  • 21
    • 77958067823 scopus 로고    scopus 로고
    • Compensatory insulin receptor (IR) activation on inhibition of insulin-like growth factor-1 receptor (IGF-1R): Rationale for cotargeting IGF-1R and IR in cancer
    • Buck E, Gokhale PC, Koujak S et al. Compensatory insulin receptor (IR) activation on inhibition of insulin-like growth factor-1 receptor (IGF-1R): rationale for cotargeting IGF-1R and IR in cancer. Mol. Cancer Ther. 9, 2652-2664 (2010).
    • (2010) Mol. Cancer Ther. , vol.9 , pp. 2652-2664
    • Buck, E.1    Gokhale, P.C.2    Koujak, S.3
  • 22
    • 35348815620 scopus 로고    scopus 로고
    • Phase I dose escalation study of the anti insulin-like growth factor-I receptor monoclonal antibody CP-751,871 in patients with refractory solid tumors
    • Haluska P, Shaw HM, Batzel GN et al. Phase I dose escalation study of the anti insulin-like growth factor-I receptor monoclonal antibody CP-751,871 in patients with refractory solid tumors. Clin. Cancer Res. 13, 5834-5840 (2007).
    • (2007) Clin. Cancer Res. , vol.13 , pp. 5834-5840
    • Haluska, P.1    Shaw, H.M.2    Batzel, G.N.3
  • 23
    • 69349103706 scopus 로고    scopus 로고
    • Inhibition of insulin-like growth factor 1 receptor by CP-751,871 radiosensitizes non-small cell lung cancer cells
    • Iwasa T, Okamoto I, Suzuki M et al. Inhibition of insulin-like growth factor 1 receptor by CP-751,871 radiosensitizes non-small cell lung cancer cells. Clin. Cancer Res. 15, 5117-5125 (2009).
    • (2009) Clin. Cancer Res. , vol.15 , pp. 5117-5125
    • Iwasa, T.1    Okamoto, I.2    Suzuki, M.3
  • 24
    • 34247140280 scopus 로고    scopus 로고
    • Ionizing radiation activates IGF-1R triggering a cytoprotective signaling by interfering with Ku-DNA binding and by modulating Ku86 expression via a p38 kinase-dependent mechanism
    • Cosaceanu D, Budiu RA, Carapancea M, Castro J, Lewensohn R, Dricu A. Ionizing radiation activates IGF-1R triggering a cytoprotective signaling by interfering with Ku-DNA binding and by modulating Ku86 expression via a p38 kinase-dependent mechanism. Oncogene 26, 2423-2434 (2007).
    • (2007) Oncogene , vol.26 , pp. 2423-2434
    • Cosaceanu, D.1    Budiu, R.A.2    Carapancea, M.3    Castro, J.4    Lewensohn, R.5    Dricu, A.6
  • 25
    • 33847041527 scopus 로고    scopus 로고
    • Insulin-like growth factor-I receptor signaling blockade combined with radiation
    • Allen GW, Saba C, Armstrong EA et al. Insulin-like growth factor-I receptor signaling blockade combined with radiation. Cancer Res. 67, 1155-1162 (2007).
    • (2007) Cancer Res. , vol.67 , pp. 1155-1162
    • Allen, G.W.1    Saba, C.2    Armstrong, E.A.3
  • 27
    • 33745212417 scopus 로고    scopus 로고
    • Insulin-like growth factor I receptor pathway inhibition by ADW742, alone or in combination with imatinib, doxorubicin, or vincristine, is a novel therapeutic approach in Ewing tumor
    • Martins AS, Mackintosh C, Martin DH et al. Insulin-like growth factor I receptor pathway inhibition by ADW742, alone or in combination with imatinib, doxorubicin, or vincristine, is a novel therapeutic approach in Ewing tumor. Clin. Cancer Res. 12, 3532-3540 (2006).
    • (2006) Clin. Cancer Res. , vol.12 , pp. 3532-3540
    • Martins, A.S.1    Mackintosh, C.2    Martin, D.H.3
  • 28
    • 65249162840 scopus 로고    scopus 로고
    • Sequencing of type I insulin-like growth factor receptor inhibition affects chemotherapy response in vitro and in vivo
    • Zeng X, Sachdev D, Zhang H, Gaillard-Kelly M, Yee D. Sequencing of type I insulin-like growth factor receptor inhibition affects chemotherapy response in vitro and in vivo. Clin. Cancer Res. 15, 2840-2849 (2009).
    • (2009) Clin. Cancer Res. , vol.15 , pp. 2840-2849
    • Zeng, X.1    Sachdev, D.2    Zhang, H.3    Gaillard-Kelly, M.4    Yee, D.5
  • 29
    • 77953088280 scopus 로고    scopus 로고
    • Insulin-like growth factor 2 expression modulates Taxol resistance and is a candidate biomarker for reduced disease-free survival in ovarian cancer
    • Huang GS, Brouwer-Visser J, Ramirez MJ et al. Insulin-like growth factor 2 expression modulates Taxol resistance and is a candidate biomarker for reduced disease-free survival in ovarian cancer. Clin. Cancer. Res. 16, 2999-3010 (2010).
    • (2010) Clin. Cancer. Res. , vol.16 , pp. 2999-3010
    • Huang, G.S.1    Brouwer-Visser, J.2    Ramirez, M.J.3
  • 30
    • 46749156706 scopus 로고    scopus 로고
    • Acquired resistance to EGFR tyrosine kinase inhibitors in cancer cells is mediated by loss of IGF-binding proteins
    • Guix M, Faber AC, Wang SE et al. Acquired resistance to EGFR tyrosine kinase inhibitors in cancer cells is mediated by loss of IGF-binding proteins. J. Clin. Invest. 118, 2609-2619 (2008).
    • (2008) J. Clin. Invest. , vol.118 , pp. 2609-2619
    • Guix, M.1    Faber, A.C.2    Wang, S.E.3
  • 31
    • 54249117292 scopus 로고    scopus 로고
    • Feedback mechanisms promote cooperativity for small molecule inhibitors of epidermal and insulin-like growth factor receptors
    • Buck E, Eyzaguirre A, Rosenfeld-Franklin M et al. Feedback mechanisms promote cooperativity for small molecule inhibitors of epidermal and insulin-like growth factor receptors. Cancer Res. 68, 8322-8332 (2008).
    • (2008) Cancer Res. , vol.68 , pp. 8322-8332
    • Buck, E.1    Eyzaguirre, A.2    Rosenfeld-Franklin, M.3
  • 32
    • 0036141447 scopus 로고    scopus 로고
    • Insulin-like growth factor receptor I mediates resistance to anti-epidermal growth factor receptor therapy in primary human glioblastoma cells through continued activation of phosphoinositide 3-kinase signaling
    • Chakravarti A, Loeffler JS, Dyson NJ. Insulin-like growth factor receptor I mediates resistance to anti-epidermal growth factor receptor therapy in primary human glioblastoma cells through continued activation of phosphoinositide 3-kinase signaling. Cancer Res. 62, 200-207 (2002).
    • (2002) Cancer Res. , vol.62 , pp. 200-207
    • Chakravarti, A.1    Loeffler, J.S.2    Dyson, N.J.3
  • 33
    • 33750605628 scopus 로고    scopus 로고
    • Impact of IGF-1R/EGFR cross-talks on hepatoma cell sensitivity to gefitinib
    • Desbois-Mouthon C, Cacheux W, Blivet-Van Eggelpoel MJ et al. Impact of IGF-1R/EGFR cross-talks on hepatoma cell sensitivity to gefitinib. Int. J. Cancer 119, 2557-2566 (2006).
    • (2006) Int. J. Cancer , vol.119 , pp. 2557-2566
    • Desbois-Mouthon, C.1    Cacheux, W.2    Blivet-Van Eggelpoel, M.J.3
  • 34
    • 33750571170 scopus 로고    scopus 로고
    • Heterodimerization of insulin-like growth factor receptor/epidermal growth factor receptor and induction of survivin expression counteract the antitumor action of erlotinib
    • Morgillo F, Woo JK, Kim ES, Hong WK, Lee HY. Heterodimerization of insulin-like growth factor receptor/epidermal growth factor receptor and induction of survivin expression counteract the antitumor action of erlotinib. Cancer Res. 66, 10100-10111 (2006).
    • (2006) Cancer Res. , vol.66 , pp. 10100-10111
    • Morgillo, F.1    Woo, J.K.2    Kim, E.S.3    Hong, W.K.4    Lee, H.Y.5
  • 35
    • 32944457518 scopus 로고    scopus 로고
    • MTOR inhibition induces upstream receptor tyrosine kinase signaling and activates Akt
    • O'Reilly KE, Rojo F, She QB et al. mTOR inhibition induces upstream receptor tyrosine kinase signaling and activates Akt. Cancer Res. 66, 1500-1508 (2006).
    • (2006) Cancer Res. , vol.66 , pp. 1500-1508
    • O'Reilly, K.E.1    Rojo, F.2    She, Q.B.3
  • 36
    • 53249138207 scopus 로고    scopus 로고
    • Recombinant human insulin-like growth factor-binding protein 3 inhibits tumor growth and targets the Akt pathway in lung and colon cancer models
    • Alami N, Page V, Yu Q et al. Recombinant human insulin-like growth factor-binding protein 3 inhibits tumor growth and targets the Akt pathway in lung and colon cancer models. Growth Horm. IGF Res. 18, 487-496 (2008).
    • (2008) Growth Horm. IGF Res. , vol.18 , pp. 487-496
    • Alami, N.1    Page, V.2    Yu, Q.3
  • 37
    • 33746867442 scopus 로고    scopus 로고
    • Recombinant human insulin-like growth factor binding protein 3 inhibits growth of human epidermal growth factor receptor-2-overexpressing breast tumors and potentiates herceptin activity in vivo
    • Jerome L, Alami N, Belanger S et al. Recombinant human insulin-like growth factor binding protein 3 inhibits growth of human epidermal growth factor receptor-2-overexpressing breast tumors and potentiates herceptin activity in vivo. Cancer Res. 66, 7245-7252 (2006).
    • (2006) Cancer Res. , vol.66 , pp. 7245-7252
    • Jerome, L.1    Alami, N.2    Belanger, S.3
  • 38
    • 77949448133 scopus 로고    scopus 로고
    • Figitumumab (CP-751,871) for cancer therapy
    • Gualberto A. Figitumumab (CP-751,871) for cancer therapy. Expert Opin. Biol. Ther. 10, 575-585 (2010).
    • (2010) Expert Opin. Biol. Ther. , vol.10 , pp. 575-585
    • Gualberto, A.1
  • 39
    • 69449097339 scopus 로고    scopus 로고
    • Emerging role of insulin-like growth factor receptor inhibitors in oncology: Early clinical trial results and future directions
    • Gualberto A, Pollak M. Emerging role of insulin-like growth factor receptor inhibitors in oncology: early clinical trial results and future directions. Oncogene 28, 3009-3021 (2009).
    • (2009) Oncogene , vol.28 , pp. 3009-3021
    • Gualberto, A.1    Pollak, M.2
  • 42
    • 84863144911 scopus 로고    scopus 로고
    • The discovery of OSI-906, a small-molecule inhibitor of the insulin-like growth factor-1 and insulin receptors
    • In press Describes the discovery of OSI-906, the most advanced dual IGF-1R and IR inhibitor currently in clinical evaluation (Phase III)
    • Mulvihill MJ, Buck E. The discovery of OSI-906, a small-molecule inhibitor of the insulin-like growth factor-1 and insulin receptors. Royal Soc. Chem. Drug Discov. Series No. 2 (In press) (2011). Describes the discovery of OSI-906, the most advanced dual IGF-1R and IR inhibitor currently in clinical evaluation (Phase III).
    • (2011) Royal Soc. Chem. Drug Discov. Series No. 2
    • Mulvihill, M.J.1    Buck, E.2
  • 43
    • 77952060250 scopus 로고    scopus 로고
    • Discovery of OSI-906: A selective and orally efficacious dual inhibitor of the IGF-1 receptor and insulin receptor
    • Mulvihill MJ, Cooke A, Rosenfeld-Franklin M et al. Discovery of OSI-906: a selective and orally efficacious dual inhibitor of the IGF-1 receptor and insulin receptor. Future Med. Chem. 1, 1153-1171 (2009).
    • (2009) Future Med. Chem. , vol.1 , pp. 1153-1171
    • Mulvihill, M.J.1    Cooke, A.2    Rosenfeld-Franklin, M.3
  • 44
    • 73149120253 scopus 로고    scopus 로고
    • BMS-754807, a small molecule inhibitor of insulin-like growth factor-1R/IR
    • Carboni JM, Wittman M, Yang Z et al. BMS-754807, a small molecule inhibitor of insulin-like growth factor-1R/IR. Mol. Cancer Ther. 8, 3341-3349 (2009).
    • (2009) Mol. Cancer Ther. , vol.8 , pp. 3341-3349
    • Carboni, J.M.1    Wittman, M.2    Yang, Z.3
  • 45
    • 34548058890 scopus 로고    scopus 로고
    • A novel, potent and selective insulin-like growth factor-I receptor kinase inhibitor blocks insulin-like growth factor-I receptor signaling in vitro and inhibits insulin-like growth factor-I receptor dependent tumor growth in vivo
    • Ji Q, Mulvihill MJ, Rosenfeld-Franklin M et al. A novel, potent and selective insulin-like growth factor-I receptor kinase inhibitor blocks insulin-like growth factor-I receptor signaling in vitro and inhibits insulin-like growth factor-I receptor dependent tumor growth in vivo. Mol. Cancer Ther. 6, 2158-2167 (2007).
    • (2007) Mol. Cancer Ther. , vol.6 , pp. 2158-2167
    • Ji, Q.1    Mulvihill, M.J.2    Rosenfeld-Franklin, M.3
  • 46
    • 77952109477 scopus 로고    scopus 로고
    • Recent progress in the development of small molecule inhibitors of insulin-like growth factor-I receptor kinase
    • Wittman M, Velaparthi U, Vyas D. Recent progress in the development of small molecule inhibitors of insulin-like growth factor-I receptor kinase. Ann. Reports Med. Chem. 44, 281-299 (2009).
    • (2009) Ann. Reports Med. Chem. , vol.44 , pp. 281-299
    • Wittman, M.1    Velaparthi, U.2    Vyas, D.3
  • 47
    • 69049108757 scopus 로고    scopus 로고
    • Inhibition of the insulin-like growth factor-1 receptor (IGF1R) tyrosine kinase as a novel cancer therapy approach
    • Li R, Pourpak A, Morris SW. Inhibition of the insulin-like growth factor-1 receptor (IGF1R) tyrosine kinase as a novel cancer therapy approach. J. Med. Chem. 52, 4981-5004 (2009).
    • (2009) J. Med. Chem. , vol.52 , pp. 4981-5004
    • Li, R.1    Pourpak, A.2    Morris, S.W.3
  • 48
    • 24744437999 scopus 로고    scopus 로고
    • Discovery of a 1H-benzoimidazol-2-yl-1H-pyridin-2-one (BMS-536924) inhibitor of insulin-like growth factor I receptor kinase with in vivo antitumor activity
    • Wittman D, Carboni J, Attar R et al. Discovery of a 1H-benzoimidazol-2- yl)-1H-pyridin-2-one (BMS-536924) inhibitor of insulin-like growth factor I receptor kinase with in vivo antitumor activity, J. Med. Chem. 48, 5639-5643 (2005).
    • (2005) J. Med. Chem. , vol.48 , pp. 5639-5643
    • Wittman, D.1    Carboni, J.2    Attar, R.3
  • 49
    • 53549109444 scopus 로고    scopus 로고
    • Discovery and evaluation of 4-(2-(4-chloro-1H-pyrazol-1-yl)ethylamino)-3- (6-(1-(3-fluoropropyl)piperidin-4-yl)-4-methyl-1Hbenzo[d]imidazol-2-yl) pyridin-2(1H)-one (BMS-695735), an orally efficacious inhibitor of insulin-like growth factor-1 receptor kinase with broad spectrum in vivo antitumor activity
    • Describes the discovery of BMS-754807, a dual IGF-1R and IR inhibitor currently in Phase I clinical evaluation
    • Velaparthi U, Wittman M, Liu P et al. Discovery and evaluation of 4-(2-(4-chloro-1H-pyrazol-1-yl)ethylamino)-3-(6-(1-(3-fluoropropyl) piperidin-4-yl)-4-methyl-1Hbenzo[d]imidazol-2-yl)pyridin-2(1H)-one (BMS-695735), an orally efficacious inhibitor of insulin-like growth factor-1 receptor kinase with broad spectrum in vivo antitumor activity. J. Med. Chem. 51, 5897-5900 (2008). Describes the discovery of BMS-754807, a dual IGF-1R and IR inhibitor currently in Phase I clinical evaluation.
    • (2008) J. Med. Chem. , vol.51 , pp. 5897-5900
    • Velaparthi, U.1    Wittman, M.2    Liu, P.3
  • 50
    • 72249089981 scopus 로고    scopus 로고
    • Discovery of a 2,4-disubstituted pyrrolo-[1,2-f][1,2,4]triazine inhibitor (BMS-754807) of insulin-like growth factor receptor (IGF-1R) kinase in clinical development
    • Wittman D, Carboni J, Yang Z et al. Discovery of a 2,4-disubstituted pyrrolo-[1,2-f][1,2,4]triazine inhibitor (BMS-754807) of insulin-like growth factor receptor (IGF-1R) kinase in clinical development, J. Med. Chem. 52, 7360-7363 (2009).
    • (2009) J. Med. Chem. , vol.52 , pp. 7360-7363
    • Wittman, D.1    Carboni, J.2    Yang, Z.3
  • 51
    • 57749094579 scopus 로고    scopus 로고
    • Optimization of 4,6-bis-anilino-1H-pyrrolo[2,3-d]pyrimidine IGF-1R tyrosine kinase inhibitors towards JNK selectivity
    • Chamberlain SD, Redman AM, Wilson JW et al. Optimization of 4,6-bis-anilino-1H-pyrrolo[2,3-d]pyrimidine IGF-1R tyrosine kinase inhibitors towards JNK selectivity. Bioorg. Med. Chem. Lett. 19, 360-364 (2009).
    • (2009) Bioorg. Med. Chem. Lett. , vol.19 , pp. 360-364
    • Chamberlain, S.D.1    Redman, A.M.2    Wilson, J.W.3
  • 52
    • 57749086732 scopus 로고    scopus 로고
    • Discovery of 4,6-bis-anilino-1Hpyrrolo[2,3-d]pyrimidines: Potent inhibitors of the IGF-1R receptor tyrosine kinase
    • Chamberlain SD, Wilson JW, Deanda F et al. Discovery of 4,6-bis-anilino-1Hpyrrolo[2,3-d]pyrimidines: potent inhibitors of the IGF-1R receptor tyrosine kinase. Bioorg. Med. Chem. Lett. 19, 469-473 (2009).
    • (2009) Bioorg. Med. Chem. Lett. , vol.19 , pp. 469-473
    • Chamberlain, S.D.1    Wilson, J.W.2    Deanda, F.3
  • 53
    • 70350228629 scopus 로고    scopus 로고
    • GSK1838705A inhibits the insulin-like growth factor-1 receptor and anaplastic lymphoma kinase and shows antitumor activity in experimental models of human cancers
    • Sabbatini P, Korenchuk S, Rowand J et al. GSK1838705A inhibits the insulin-like growth factor-1 receptor and anaplastic lymphoma kinase and shows antitumor activity in experimental models of human cancers. Mol. Cancer Ther. 8, 2811-2820 (2009).
    • (2009) Mol. Cancer Ther. , vol.8 , pp. 2811-2820
    • Sabbatini, P.1    Korenchuk, S.2    Rowand, J.3
  • 54
    • 57749093097 scopus 로고    scopus 로고
    • Optimization of a series of 4,6-bis-anilino-1H-pyrrolo[2,3-d]pyrimidine inhibitors of IGF-1R: Elimination of an acid-mediated decomposition pathway
    • Chamberlain SD, Redman AM, Patnaik S et al. Optimization of a series of 4,6-bis-anilino-1H-pyrrolo[2,3-d]pyrimidine inhibitors of IGF-1R: elimination of an acid-mediated decomposition pathway. Bioorg. Med. Chem. Lett. 19, 373-377 (2009).
    • (2009) Bioorg. Med. Chem. Lett. , vol.19 , pp. 373-377
    • Chamberlain, S.D.1    Redman, A.M.2    Patnaik, S.3
  • 55
    • 65149102076 scopus 로고    scopus 로고
    • Discovery of 3,5-disubstituted-1H-pyrrolo[2,3-b]pyridines as potent inhibitors of the insulin-like growth factor-1 receptor (IGF-1R) tyrosine kinase
    • Patnaik S, Stevens K, Gerding R et al. Discovery of 3,5-disubstituted-1H- pyrrolo[2,3-b]pyridines as potent inhibitors of the insulin-like growth factor-1 receptor (IGF-1R) tyrosine kinase. Bioorg. Med. Chem. Lett. 19, 3136-3140 (2009).
    • (2009) Bioorg. Med. Chem. Lett. , vol.19 , pp. 3136-3140
    • Patnaik, S.1    Stevens, K.2    Gerding, R.3
  • 56
    • 33745298429 scopus 로고    scopus 로고
    • Rational design of inhibitors that bind to inactive kinase conformations
    • Liu Y, Gray N. Rational design of inhibitors that bind to inactive kinase conformations. Nat. Chem. Biol. 2, 358 (2006).
    • (2006) Nat. Chem. Biol. , vol.2 , pp. 358
    • Liu, Y.1    Gray, N.2
  • 57
    • 58549088976 scopus 로고    scopus 로고
    • Discovery and optimization of imidazo[1,2-a]pyridine inhibitors of insulin-like growth factor-1 receptor (IGF-1R)
    • Emmitte K, Wilson B, Baum E et al. Discovery and optimization of imidazo[1,2-a]pyridine inhibitors of insulin-like growth factor-1 receptor (IGF-1R). Bioorg. Med. Chem. Lett. 19, 1004-1008 (2009).
    • (2009) Bioorg. Med. Chem. Lett. , vol.19 , pp. 1004-1008
    • Emmitte, K.1    Wilson, B.2    Baum, E.3
  • 58
    • 65649122657 scopus 로고    scopus 로고
    • Antitumor activity of GSK1904529A, a small-molecule inhibitor of the insulin-like growth factor-I receptor tyrosine kinase
    • Sabbatini P, Rowand J, Groy A et al. Antitumor activity of GSK1904529A, a small-molecule inhibitor of the insulin-like growth factor-I receptor tyrosine kinase. Clin. Cancer Res. 15, 3058-3067 (2009).
    • (2009) Clin. Cancer Res. , vol.15 , pp. 3058-3067
    • Sabbatini, P.1    Rowand, J.2    Groy, A.3
  • 59
    • 44949188302 scopus 로고    scopus 로고
    • Lead identification to generate isoquinolinedione inhibitors of insulin like growth factor receptor (IGF-1R) for potential use in cancer treatment
    • Mayer C, Banker L, Boschelli F et al. Lead identification to generate isoquinolinedione inhibitors of insulin like growth factor receptor (IGF-1R) for potential use in cancer treatment. Bioorg. Med. Chem. Lett. 18, 3641-3645 (2008).
    • (2008) Bioorg. Med. Chem. Lett. , vol.18 , pp. 3641-3645
    • Mayer, C.1    Banker, L.2    Boschelli, F.3
  • 60
    • 57949114351 scopus 로고    scopus 로고
    • Lead identification to generate 3-cyanoquinoline inhibitors of insulin-like growth factor receptor (IGF-1R) for potential use in cancer treatment
    • Miller L, Mayer S, Berger D et al. Lead identification to generate 3-cyanoquinoline inhibitors of insulin-like growth factor receptor (IGF-1R) for potential use in cancer treatment. Bioorg. Med. Chem. Lett. 19, 62-66 (2009).
    • (2009) Bioorg. Med. Chem. Lett. , vol.19 , pp. 62-66
    • Miller, L.1    Mayer, S.2    Berger, D.3
  • 61
    • 38849133610 scopus 로고    scopus 로고
    • Novel 2-phenylquinolin-7-yl-derived imidazo[1,5-a]pyrazines as potent insulin-like growth factor-I receptor (IGF-IR) inhibitors
    • Mulvihill M, Ji Q, Coate H et al. Novel 2-phenylquinolin-7-yl-derived imidazo[1,5-a]pyrazines as potent insulin-like growth factor-I receptor (IGF-IR) inhibitors. Bioorg. Med. Chem. 16, 1359-1375 (2008).
    • (2008) Bioorg. Med. Chem. , vol.16 , pp. 1359-1375
    • Mulvihill, M.1    Ji, Q.2    Coate, H.3
  • 62
    • 38049018155 scopus 로고    scopus 로고
    • A quantitative analysis of kinase inhibitor selectivity
    • Karaman W, Herrgard S, Treiber K et al. A quantitative analysis of kinase inhibitor selectivity. Nat. Biotechnol. 26, 127-132 (2008).
    • (2008) Nat. Biotechnol. , vol.26 , pp. 127-132
    • Karaman, W.1    Herrgard, S.2    Treiber, K.3
  • 63
    • 78650220850 scopus 로고    scopus 로고
    • Discovery of an orally efficacious imidazo[5,1-f][1,2,4]triazine dual inhibitor of IGF-1R and IR. ACS Med
    • Compound 9 in this manuscript is referred to as FQIT (cis-3-[4-amino-5- (8-fluoro-2-phenyl-quinolin-7-yl)-imidazo[5,1-f][1,2,4]triazin-7-yl] -1-methyl-cyclobutanol)
    • Jin M, Gokhale P, Cooke A et al. Discovery of an orally efficacious imidazo[5,1-f][1,2,4]triazine dual inhibitor of IGF-1R and IR. ACS Med. Chem. Lett. 1, 510-515 (2010). Compound 9 in this manuscript is referred to as FQIT (cis-3-[4-amino-5-(8-fluoro-2-phenyl-quinolin-7-yl)-imidazo[5,1-f][1,2,4] triazin-7-yl]-1-methyl-cyclobutanol).
    • (2010) Chem. Lett. , vol.1 , pp. 510-515
    • Jin, M.1    Gokhale, P.2    Cooke, A.3
  • 64
    • 79851513257 scopus 로고    scopus 로고
    • Potent and selective cyclohexyl-derived imidazopyrazine insulin-like growth factor 1 receptor inhibitors with in vivo efficacy
    • Jin M, Kleinberg A, Cooke A et al. Potent and selective cyclohexyl-derived imidazopyrazine insulin-like growth factor 1 receptor inhibitors with in vivo efficacy. Bioorg. Med. Chem. Lett. 21, 1176-1180 (2011).
    • (2011) Bioorg. Med. Chem. Lett. , vol.21 , pp. 1176-1180
    • Jin, M.1    Kleinberg, A.2    Cooke, A.3


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