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基于多靶标配体的合理药物设计的最新进展。

Recent Advances in the Rational Drug Design Based on Multi-target Ligands.

机构信息

Institute of Biomedical Materials and Engineering, College of Materials Science and Engineering, Qingdao University, Qingdao 266071, China.

出版信息

Curr Med Chem. 2020 Aug 6;27(28):4720-4740. doi: 10.2174/0929867327666200102120652.

Abstract

Multi-target drugs have gained considerable attention in the last decade owing to their advantages in the treatment of complex diseases and health conditions linked to drug resistance. Single-target drugs, although highly selective, may not necessarily have better efficacy or fewer side effects. Therefore, more attention is being paid to developing drugs that work on multiple targets at the same time, but developing such drugs is a huge challenge for medicinal chemists. Each target must have sufficient activity and have sufficiently characterized pharmacokinetic parameters. Multi-target drugs, which have long been known and effectively used in clinical practice, are briefly discussed in the present article. In addition, in this review, we will discuss the possible applications of multi-target ligands to guide the repositioning of prospective drugs.

摘要

多靶点药物在过去十年中受到了相当大的关注,因为它们在治疗与耐药性相关的复杂疾病和健康状况方面具有优势。单靶点药物虽然具有高度选择性,但并不一定具有更好的疗效或更少的副作用。因此,人们越来越关注开发同时作用于多个靶点的药物,但开发此类药物对药物化学家来说是一个巨大的挑战。每个靶点都必须具有足够的活性和充分表征的药代动力学参数。本文简要讨论了长期以来在临床实践中已知且有效的多靶点药物。此外,在本文综述中,我们将讨论多靶点配体的可能应用,以指导潜在药物的再定位。

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