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药物杂交策略:是在先导化合物鉴定之前还是之后?

Drug hybridization strategies: before or after lead identification?

机构信息

Professor of Pharmaceutical and Medicinal Chemistry, Faculdade de Farmácia, Universidade Federal do Rio de Janeiro, Laboratório de Avaliação e Síntese de Substâncias Bioativas (LASSBio), Rio de Janeiro, RJ, PO Box 68023, ZIP 21941-902, Brazil +55 21 2562 6503 ; +55 21 2562 6478 ;

出版信息

Expert Opin Drug Discov. 2009 Jun;4(6):605-9. doi: 10.1517/17460440902956636. Epub 2009 May 6.

Abstract

The molecular hybridization approach is one of the most valuable structural modification tools useful for the discovery of ligands and prototypes presenting either optimized affinity for one bioreceptor or the ability to modulate more than one bioreceptor associated with the target disease. The growing efforts to discover hybrid drugs resulting from the combination of pharmacophoric moieties of different known lead compounds have brought a new hope for the treatment of multifactorial diseases in recent years. This editorial describes possible ways of exploring molecular hybridization strategies to plan new effective dual or symbiotic drug candidates.

摘要

分子杂交方法是最有价值的结构修饰工具之一,可用于发现配体和原型,这些配体和原型要么对一种生物受体具有优化的亲和力,要么能够调节与目标疾病相关的一种以上生物受体。近年来,人们越来越努力地发现由不同已知先导化合物的药效团组合而成的混合药物,这为治疗多因素疾病带来了新的希望。本社论描述了探索分子杂交策略的可能途径,以规划新的有效双或共生药物候选物。

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