Small-molecule inhibitors of the ERK signaling pathway: Towards novel anticancer therapeutics.
作者信息
Yap Jeremy L, Worlikar Shilpa, MacKerell Alexander D, Shapiro Paul, Fletcher Steven
机构信息
Department of Pharmaceutical Sciences, University of Maryland School of Pharmacy, Baltimore, 21201, USA.
出版信息
ChemMedChem. 2011 Jan 3;6(1):38-48. doi: 10.1002/cmdc.201000354.
Abstract
摘要
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PLX4032, a selective BRAF(V600E) kinase inhibitor, activates the ERK pathway and enhances cell migration and proliferation of BRAF melanoma cells.PLX4032，一种选择性 BRAF(V600E) 激酶抑制剂，激活 ERK 通路，增强 BRAF 黑色素瘤细胞的迁移和增殖。
Pigment Cell Melanoma Res. 2010 Apr;23(2):190-200. doi: 10.1111/j.1755-148X.2010.00685.x. Epub 2010 Feb 10.
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Structure-guided design of potent and selective pyrimidylpyrrole inhibitors of extracellular signal-regulated kinase (ERK) using conformational control.利用构象控制进行细胞外信号调节激酶（ERK）强效和选择性嘧啶基吡咯抑制剂的结构导向设计。
J Med Chem. 2009 Oct 22;52(20):6362-8. doi: 10.1021/jm900630q.
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Bioorg Med Chem Lett. 2009 Nov 1;19(21):6042-6. doi: 10.1016/j.bmcl.2009.09.057. Epub 2009 Sep 18.
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Clin Cancer Res. 2008 Jun 15;14(12):3651-6. doi: 10.1158/1078-0432.CCR-08-0333.
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BRAF silencing by short hairpin RNA or chemical blockade by PLX4032 leads to different responses in melanoma and thyroid carcinoma cells.通过短发夹RNA使BRAF沉默或用PLX4032进行化学阻断，在黑色素瘤和甲状腺癌细胞中会导致不同的反应。
Mol Cancer Res. 2008 May;6(5):751-9. doi: 10.1158/1541-7786.MCR-07-2001. Epub 2008 May 5.
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