A strategy for the design of multiplex inhibitors for kinase-mediated signalling in angiogenesis

Current Opinion in Chemical Biology - Tập 6 - Trang 486-492 - 2002
Jerry Adams1, Pearl Huang1, Denis Patrick1
1GlaxoSmithKline MMPD CEDD Departments Oncology and Medicinal Chemistry, Upper Merion, King of Prussia, Philadelphia 19406, USA

Tài liệu tham khảo

Hasan, 2001, VEGF antagonists, Expert Opin Biol Ther, 1, 703, 10.1517/14712598.1.4.703 Sun, 2000, Identification of substituted 3-[(4,5,6, 7-tetrahydro-1H-indol-2-yl)methylene]-1,3-dihydroindol-2-ones as growth factor receptor inhibitors for VEGF-R2 (Flk-1/KDR), FGF-R1, and PDGF-Rbeta tyrosine kinases, J Med Chem, 43, 2655, 10.1021/jm9906116 Hamby, 1999, Small molecule inhibitors of tumor-promoted angiogenesis, including protein tyrosine kinase inhibitors, Pharmacol Ther, 82, 169, 10.1016/S0163-7258(98)00053-9 Relf, 1997, Cancer Res, 57, 963 Taylor, 2002, Tumor-specific regulation of angiogenic growth factors and their receptors during recovery from cytotoxic therapy, Clin Cancer Res, 8, 1213 Cherrington, 2000, New paradigms for the treatment of cancer: the role of anti- angiogenesis agents, Adv Cancer Res, 79, 1, 10.1016/S0065-230X(00)79001-4 Mohammadi, 1998, Crystal structure of an angiogenesis inhibitor bound to the FGF receptor tyrosine kinase domain, EMBO J, 17, 5896, 10.1093/emboj/17.20.5896 Wishart N, Arnold LD, Barlozzari T, Burchat AF, Calderwood DJ, Qian X-D, Choquette DM, Deng B, Friedman MM, Hirst GC et al.: Structure activity relationships for a novel series of pyrrolo[2,3-d]pyrimidine tie-2 Inhibitors. Abstract # 4205 at the 93rd National Meeting of the American Association Cancer Research, 2002 April: San Francisco, California, USA 2002. http://aacr02.agora.com/planner/default.asp. Ciardiello F, Caputo R, Damiano V, Vitagliano D, Carlomagno F, Santoro M, Fontanini G, Bianco AR, Tortora G, Antitumor effects of ZD6474, a small molecule VEGF receptor tyrosine kinase inhibitor that is also active against EGF receptor tyrosine kinase. Abstract #5348 at the 93rd National Meeting of the American Association Cancer Research, 2002 April: San Francisco, CA, USA 2002. http://aacr02.agora.com/planner/default.asp. Hennequin, 2002, Novel 4-anilinoquinazolines with C-7 basic side chains: design and structure activity relationship of a series of potent, orally active, VEGF receptor tyrosine kinase inhibitors, J Med Chem, 45, 1300, 10.1021/jm011022e Laird, 2000, Cherrington: SU6668 is a potent antiangiogenic and antitumor agent that induces regression of established tumors, Cancer Res, 60, 4152 Blume-Jensen, 2001, Oncogenic kinase signalling, Nature, 411, 355, 10.1038/35077225 Hubbard, 2002, Autoinhibitory mechanisms in receptor tyrosine kinases, Front Biosci, 7, d330, 10.2741/A778 Huse, 2002, The conformational plasticity of protein kinases, Cell, 109, 275, 10.1016/S0092-8674(02)00741-9 Davies, 2000, Specificity and mechanism of action of some commonly used protein kinase inhibitors, Biochem J, 351, 95, 10.1042/bj3510095 Cohen, 1999, The development and therapeutic potential of protein kinase inhibitors, Curr Opin Chem Biol, 3, 459, 10.1016/S1367-5931(99)80067-2 Adams, 1999, Recent progress towards the identification of selective inhibitors of serine/threonine protein kinase, Curr Opin Drug Discov Dev, 2, 96 Toledo, 1999, The structure-based design of ATP-site directed protein kinase inhibitors, Curr Med Chem, 6, 775, 10.2174/092986730609220401150028 Hanks, 1988, The protein kinase family: conserved features and deduced phylogeny of the catalytic domains, Science, 241, 42, 10.1126/science.3291115 Eyers, 1998, Conversion of SB 203580-insensitive MAP kinase family members to drug-sensitive forms by a single amino-acid substitution, Chem Biol, 5, 321, 10.1016/S1074-5521(98)90170-3 Trumpp-Kallmeyer, 1998, Development of a binding model to protein tyrosine kinases for substituted pyrido[2,3-d]pyrimidine inhibitors, J Med Chem, 41, 1752, 10.1021/jm970634p Adams, 2001, p38 MAP kinase: molecular target for the inhibition of pro-inflammatory cytokines, Prog Med Chem, 38, 1, 10.1016/S0079-6468(08)70091-2 Bishop, 2000, Unnatural ligands for engineered proteins: new tools for chemical genetics, Annu Rev Biophys Biomol Struct, 29, 577, 10.1146/annurev.biophys.29.1.577 Plowman, 1999, The protein kinases of Caenorhabditis elegans: a model for signal transduction in multicellular organisms, Proc Natl Acad Sci USA, 96, 13603, 10.1073/pnas.96.24.13603 Panek, 1997, In vitro pharmacological characterization of PD 166285, a new nanomolar potent and broadly active protein tyrosine kinase inhibitor, J Pharmacol Exp Ther, 283, 1433 Schindler, 2000, Structural mechanism for STI-571 inhibition of Abelson tyrosine kinase, Science, 289, 1938, 10.1126/science.289.5486.1938 Druker, 1996, Effects of a selective inhibitor of the Abl tyrosine kinase on the growth of Bcr-Abl positive cells, Nat Med, 2, 561, 10.1038/nm0596-561 Griffin, 2002, Simultaneous inhibition of the receptor kinase activity of vascular endothelial, fibroblast, and platelet-derived growth factors suppresses tumor growth and enhances tumor radiation response, Cancer Res, 62, 1702 Shaheen, 1999, Antiangiogenic therapy targeting the tyrosine kinase receptor for vascular endothelial growth factor receptor inhibits the growth of colon cancer liver metastasis and induces tumor and endothelial cell apoptosis, Cancer Res, 59, 5412 Shaheen, 2001, Tyrosine kinase inhibition of multiple angiogenic growth factor receptors improves survival in mice bearing colon cancer liver metastases by inhibition of endothelial cell survival mechanisms, Cancer Res, 61, 1464 Laird, 2002, SU6668 inhibits Flk-1/KDR and PDGFRbeta in vivo, resulting in rapid apoptosis of tumor vasculature and tumor regression in mice, FASEB J, 16, 681, 10.1096/fj.01-0700com Drevs J, Esser N, Konerding MA, Wolloscheck T, Wedge SR, Ryan A, Ogilvie DJ, Unger C, Marme D: Effect of ZD6474, a VEGF receptor tyrosine kinase inhibitor, on primary tumor growth, metastasis, vessel density and microvascular architecture in murine renal cell carcinoma. Abstract # 5358 at the 93rd National Meeting of the American Association Cancer Research, 2002 April: San Francisco, California, USA 2002. http://aacr02.agora.com/planner/default.asp. Weismann M, Lee SH, Wernette-Hammond M-E, Lapointe G, Javandel M, Chreyl G, Nordahl L, Heise C, Amiri P, Renhowe P et al.: Characterization of potent tyrosine kinase inhibitors that modulate angiogenesis and proliferation of selected cancer cell lines. Abstract # 4208 at the 93rd National Meeting of the American Association Cancer Research, 2002 April: San Francisco, California, USA 2002. http://aacr02.agora.com/planner/default.asp. Heise C, Nordahl L, Watson C, Ye H, Aardalen K, Lee SH, Goldbeck C, Renhowe P, Tesconi M, Harris A et al.: In vivo preclinical evaluation of tyrosine kinase inhibitors with potent effects on tumor angiogenesis, growth and metastasis. Abstract # 3675 at the 93rd National Meeting of the American Association Cancer Research, 2002 April: San Francisco, California, USA 2002. http://aacr02.agora.com/planner/default.asp. Gorre, 2001, Clinical resistance to STI-571 cancer therapy caused by BCR-ABL gene mutation or amplification, Science, 293, 876, 10.1126/science.1062538 Hofmann, 2002, Ph(+) acute lymphoblastic leukemia resistant to the tyrosine kinase inhibitor STI571 has a unique BCR-ABL gene mutation, Blood, 99, 1860, 10.1182/blood.V99.5.1860 Wood, 2000, PTK787/ZK 222584, a novel and potent inhibitor of vascular endothelial growth factor receptor tyrosine kinases, impairs vascular endothelial growth factor-induced responses and tumor growth after oral administration, Cancer Res, 60, 2178 Mendel, 2000, Development of SU5416, a selective small molecule inhibitor of VEGF receptor tyrosine kinase activity, as an anti-angiogenesis agent, Anticancer Drug Des, 15, 29 Mendel DB, Laird AD, Xin X, Abrams GT, Li J, Schreck RE, Carver J, Louie SG, Ngai TJ, Lee LB et al.: In vivo anti-tumor and mechanism of action studies of SU11248, a potent and selective inhibitor of the VEGF and PDGF receptors. Abstract # 5349 at the 93rd National Meeting of the American Association Cancer Research, 2002 April: San Francisco, California, USA 2002. http://aacr02.agora.com/planner/default.asp. Karp DD, Tolcher A, Healey D, O'Leary JJ, Debono J, Huberman M, Caulkins J, Molpus K, Sutula K, Noe DA: Preliminary pharmacokinetic (PK) characteristics of an oral vascular endothelial growth factor receptor-2 (VEFGR-2) tyrosine kinase inhibitor (TKI), Cp-547,632 in patients (Pts) with advanced solid tumors. Abstract # 2753 at the 93rd National Meeting of the American Association Cancer Research, 2002 April: San Francisco, California, USA 2002. http://aacr02.agora.com/planner/default.asp. Ruggeri BA, Singh J, Hudkins R, Gingrich D, Angeles T, Robinsin C, Chang H, Hunter K, Dobranski P, Pritchard S et al.: CEP-7055: an orally-active VEGF-R kinase inhibitor with potent anti-angiogenic activity and anti-tumor efficacy against human tumor xenograft growth. Abstract # 5347 at the 93rd National Meeting of the American Association Cancer Research, 2002 April: San Francisco, California, USA 2002. http://aacr02.agora.com/planner/default.asp. Hu-Lowe D, Hallin M, Feeley R, Zou H, Rewolinski D, Wickman G, Chen E, Kim Y, Riney S, Reed J et al.: Characterization of potency and activity of the VEGF/PDGF receptor tyrosine kinase inhibitor AG013736. Abstract # 5356 at the 93rd National Meeting of the American Association Cancer Research, 2002 April: San Francisco, California, USA 2002. http://aacr02.agora.com/planner/default.asp. Kubo K, Fujiwara Y, Iwakubo M, Murooka H, Iwai A, Nakamura K, Hasegawa K, Kobayashi Y, Takahashi N, Takahashi K et al.: Synthesis and structure-activity relationship of quinazoline-urea derivatives as novel orally active VEGF receptor tyrosine kinase selective inhibitors. Abstract # 913 at the 93rd National Meeting of the American Association Cancer Research, 2002 April: San Francisco, California, USA 2002. http://aacr02.agora.com/planner/default.asp. Robinson, 2000, The protein tyrosine kinase family of the human genome, Oncogene, 19, 5548, 10.1038/sj.onc.1203957