【摘要】：共價修飾類藥物通過共價鍵與靶標結(jié)合而發(fā)揮其藥理作用,由于其可能帶來脫靶效應及不良反應,長期以來在藥物設計領域盡可能被避免。隨著對已上市的重磅級共價藥物結(jié)合模式的深入研究,越來越多共價修飾類藥物重新得到研發(fā)人員的重視,尋找高選擇性、低不良反應的共價修飾類藥物已成為目前研究的熱點。本文對一些共價修飾類藥物進行分類,對其與靶標結(jié)合的模式以及近年來共價修飾類藥物設計的新策略進行綜述,為共價藥物的合理藥物設計提供參考。
[Abstract]:Covalent modified drugs play a role in pharmacology through covalent bonding with targets. Because of their possible mismatch effect and adverse reactions, covalent modified drugs have been avoided in the field of drug design for a long time. With the in-depth study of the model of covalent drugs that have been listed, more and more covalent modified drugs have been paid more and more attention by researchers and researchers, looking for high selectivity. Covalent modified drugs with low adverse reactions have become the focus of research at present. In this paper, some covalent modified drugs are classified, the pattern of their binding to target and the new design strategies of covalent modified drugs in recent years are reviewed, which provides a reference for the rational design of covalent drugs.
【作者單位】： 中國藥科大學藥學院;
【基金】：國家自然科學基金資助項目(No.81573281)~~
【分類號】：R91
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本文編號：2385022