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重视基于片段的药物发现技术 被引量:1

Emphasizing on the fragment-based drug discovery
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摘要 基于片段的药物发现(FBDD)是将结构生物学、药物筛选、药物化学和分子模拟相整合的创制小分子药物的综合技术。本文简要介绍了FBDD的基本原理,并讨论了国外应用此技术推动新药研发的实例,旨在呼吁我国的众多药物研发大平台重视FBDD技术并加以应用。 The fragment-based drug discovery(FBDD) is a comprehensive technology, consisting of struc- tural biology, drug screening, medicinal chemistry, and molecular modeling. This overview concisely describes the basic principle of FBDD method and illustrates a few examples appealing to applying this method in China Drug in- novation.
作者 郭颖 郭宗儒
出处 《中国新药杂志》 CAS CSCD 北大核心 2013年第16期1873-1877,1911,共6页 Chinese Journal of New Drugs
关键词 基于片段的药物发现 结构生物学 配体效率 综合平台 fragment-based drug discovery structural biology structural efficiency integrated platform
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  • 1SHUKER SB, HYJDUK PJ, MEADOWS PE, et al high-affinity ligands for proteins: SAR by NMR [ J 1 - Science 1996, 274(5292) : 1531 - 1534.
  • 2SCOTT DE, COYNE AG, HUDSON SA, et al. Fragment-based approaches in drug discovery and chemical biology[ J]. Biochem- istry, 2012, 51 ( 25 ) :4990 - 5003.
  • 3BAKER M. Fragment-based lead discovery grows up[ J]. Nature Rev Drug Diseov, 2013, 12(1) : 5 -7.
  • 4CONGREVE M,CHESSARI G, TISI D, et al. Recent develop- ments in fragment-based drug discovery[ J]. J Med Chem, 2008, 51(13): 3661 -3680.
  • 5DE KLOE GE, BAILEY D, LEURS R, et al. Transforming frag- ments becomes big in medicinal chemistry [ J ]. Drug Discov To- day, 2009, 14( 13 - 14) : 630 -646.
  • 6TSAI J, LEE JT, WANG WR, et al. Discovery of a selective in- hibitor of oncogenic B-Raf kinase with potent antimelanoma activ- ity[ J], Proc Natl Acad Scl USA, 2008, 105 (8) : 3041 - 3046.
  • 7BOLLAG G, HIRTH P, TSAI J, et al. Clinical efficacy of a RAF inhibitor needs broadtarget blockade in BRAF-mutant mela- noma[J]. Nature. 2010. 467(7315): 596 -599.
  • 8ABADZAPATERO C, METZ J. Ligand efficiency indices as guideposts for drug discovery[ J]. Drug Discovery Today, 2005, 10(7) : 464 -469.
  • 9DAS THANKUR M, SALANGSANG F, LANDMAN AS, et al. Modelling vemurafenib resistance in melanoma reveals a strategy to forestall drug resistance [ J ]. Nature, 2013, 494 ( 7436 ) : 251 - 255.
  • 10BOLLAG G, TSAI J, ZHANG J. Vemurafenib : the first drug ap- proved for BRAF-mutant cancer [ J ]. Nat Rev Drug Discov, 2012, 11(11): 873 -886.

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