Small molecule inhibitors of BRAF in clinical trials

被引：54

作者：

Zambon, Alfonso ^{[2
]}

Niculescu-Duvaz, Ion ^{[2
]}

Niculescu-Duvaz, Dan ^{[2
]}

Marais, Richard ^{[1
]}

Springer, Caroline J. ^{[2
]}

机构：

[1] Inst Canc Res, Signal Transduct Team, Div Canc Biol, London SW3 6JB, England

[2] Inst Canc Res, Canc Res UK Canc Therapeut Unit, Div Canc Therapeut, Sutton SM2 5NG, Surrey, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2012年 / 22卷 / 02期

基金：

英国惠康基金;

关键词：

Kinase inhibitor; BRAF protein; Clinical candidate; B-RAF; COMBINATION THERAPY; RAF/MEK/ERK PATHWAY; ANTITUMOR-ACTIVITY; TUMOR PROGRESSION; KINASE; SORAFENIB; MELANOMA; POTENT; VEMURAFENIB;

D O I：

10.1016/j.bmcl.2011.11.060

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Over the last few years, BRAF has emerged as a validated target in melanoma. This review summarises recent advances in the development of BRAF inhibitors, focussing on agents that have been assessed clinically. (C) 2011 Elsevier Ltd. All rights reserved.

引用

页码：789 / 792

页数：4

共 52 条

[1]

Amiri P., 2006, AACR M, P1140

[2]

[Anonymous], 2008, CANCER RES

[3] Targeting BRAF for patients with melanoma [J].

Arkenau, H-T ;

Kefford, R. ;

Long, G. V. .

BRITISH JOURNAL OF CANCER, 2011, 104 (03) :392-398

[4] Clinical efficacy of a RAF inhibitor needs broad target blockade in BRAF-mutant melanoma [J].

Bollag, Gideon ;

Hirth, Peter ;

Tsai, James ;

Zhang, Jiazhong ;

Ibrahim, Prabha N. ;

Cho, Hanna ;

Spevak, Wayne ;

Zhang, Chao ;

Zhang, Ying ;

Habets, Gaston ;

Burton, ElizabethA. ;

Wong, Bernice ;

Tsang, Garson ;

West, Brian L. ;

Powell, Ben ;

Shellooe, Rafe ;

Marimuthu, Adhirai ;

Nguyen, Hoa ;

Zhang, Kam Y. J. ;

Artis, Dean R. ;

Schlessinger, Joseph ;

Su, Fei ;

Higgins, Brian ;

Iyer, Raman ;

D'Andrea, Kurt ;

Koehler, Astrid ;

Stumm, Michael ;

Lin, Paul S. ;

Lee, Richard J. ;

Grippo, Joseph ;

Puzanov, Igor ;

Kim, Kevin B. ;

Ribas, Antoni ;

McArthur, Grant A. ;

Sosman, Jeffrey A. ;

Chapman, Paul B. ;

Flaherty, Keith T. ;

Xu, Xiaowei ;

Nathanson, Katherine L. ;

Nolop, Keith .

NATURE, 2010, 467 (7315) :596-599

[5] Improved Survival with Vemurafenib in Melanoma with BRAF V600E Mutation [J].

Chapman, Paul B. ;

Hauschild, Axel ;

Robert, Caroline ;

Haanen, John B. ;

Ascierto, Paolo ;

Larkin, James ;

Dummer, Reinhard ;

Garbe, Claus ;

Testori, Alessandro ;

Maio, Michele ;

Hogg, David ;

Lorigan, Paul ;

Lebbe, Celeste ;

Jouary, Thomas ;

Schadendorf, Dirk ;

Ribas, Antoni ;

O'Day, Steven J. ;

Sosman, Jeffrey A. ;

Kirkwood, John M. ;

Eggermont, Alexander M. M. ;

Dreno, Brigitte ;

Nolop, Keith ;

Li, Jiang ;

Nelson, Betty ;

Hou, Jeannie ;

Lee, Richard J. ;

Flaherty, Keith T. ;

McArthur, Grant A. .

NEW ENGLAND JOURNAL OF MEDICINE, 2011, 364 (26) :2507-2516

[6] Mutations of the BRAF gene in human cancer [J].

Davies, H ;

Bignell, GR ;

Cox, C ;

Stephens, P ;

Edkins, S ;

Clegg, S ;

Teague, J ;

Woffendin, H ;

Garnett, MJ ;

Bottomley, W ;

Davis, N ;

Dicks, N ;

Ewing, R ;

Floyd, Y ;

Gray, K ;

Hall, S ;

Hawes, R ;

Hughes, J ;

Kosmidou, V ;

Menzies, A ;

Mould, C ;

Parker, A ;

Stevens, C ;

Watt, S ;

Hooper, S ;

Wilson, R ;

Jayatilake, H ;

Gusterson, BA ;

Cooper, C ;

Shipley, J ;

Hargrave, D ;

Pritchard-Jones, K ;

Maitland, N ;

Chenevix-Trench, G ;

Riggins, GJ ;

Bigner, DD ;

Palmieri, G ;

Cossu, A ;

Flanagan, A ;

Nicholson, A ;

Ho, JWC ;

Leung, SY ;

Yuen, ST ;

Weber, BL ;

Siegler, HF ;

Darrow, TL ;

Paterson, H ;

Marais, R ;

Marshall, CJ ;

Wooster, R .

NATURE, 2002, 417 (6892) :949-954

[7] Sorafenib in advanced melanoma: a Phase II randomised discontinuation trial analysis [J].

Eisen, T. ;

Ahmad, T. ;

Flaherty, K. T. ;

Gore, M. ;

Kaye, S. ;

Marais, R. ;

Gibbens, I. ;

Hackett, S. ;

James, M. ;

Schuchter, L. M. ;

Nathanson, K. L. ;

Xia, C. ;

Simantov, R. ;

Schwartz, B. ;

Poulin-Costello, M. ;

O'Dwyer, P. J. ;

Ratain, M. J. .

BRITISH JOURNAL OF CANCER, 2006, 95 (05) :581-586

[8]

Flaherty KT, N ENGL J MED, V363, P809

[9] Guilty as charged: B-RAF is a human oncogene [J].

Garnett, MJ ;

Marais, R .

CANCER CELL, 2004, 6 (04) :313-319

[10]

Garraway LA., 2010, NATURE, V468, P968

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