【摘要】：共價(jià)修飾類藥物通過(guò)共價(jià)鍵與靶標(biāo)結(jié)合而發(fā)揮其藥理作用,由于其可能帶來(lái)脫靶效應(yīng)及不良反應(yīng),長(zhǎng)期以來(lái)在藥物設(shè)計(jì)領(lǐng)域盡可能被避免。隨著對(duì)已上市的重磅級(jí)共價(jià)藥物結(jié)合模式的深入研究,越來(lái)越多共價(jià)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(yīng)的共價(jià)修飾類藥物已成為目前研究的熱點(diǎn)。本文對(duì)一些共價(jià)修飾類藥物進(jìn)行分類,對(duì)其與靶標(biāo)結(jié)合的模式以及近年來(lái)共價(jià)修飾類藥物設(shè)計(jì)的新策略進(jìn)行綜述,為共價(jià)藥物的合理藥物設(shè)計(jì)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(guó)藥科大學(xué)藥學(xué)院;
【基金】：國(guó)家自然科學(xué)基金資助項(xiàng)目(No.81573281)~~
【分類號(hào)】：R91
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本文編號(hào)：2385022