Issue 8, 2020

Covalent inhibitors: a rational approach to drug discovery

Abstract

Covalent inhibitors are recognized as an important component in drug discovery and therapeutics. Since the first appearance of covalent inhibitors in the late 18th century, the field has advanced significantly and currently about 30% of the marketed drugs are covalent inhibitors. The numerous advantages of covalent inhibitors are counteracting the initial concerns regarding potential off-target toxicity. Thus, continuous research, especially for cancer targets is reported. The aim of this review is to provide a short historic overview and focus on recently developed covalent inhibitors (2011–2019), including structural aspects and examples on challenging targets.

Graphical abstract: Covalent inhibitors: a rational approach to drug discovery

Article information

Article type
Review Article
Submitted
09 May 2020
Accepted
19 Jun 2020
First published
02 Jul 2020
This article is Open Access
Creative Commons BY-NC license

RSC Med. Chem., 2020,11, 876-884

Covalent inhibitors: a rational approach to drug discovery

F. Sutanto, M. Konstantinidou and A. Dömling, RSC Med. Chem., 2020, 11, 876 DOI: 10.1039/D0MD00154F

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