Jump to main content
Jump to site search

Issue 8, 2020
Previous Article Next Article

Covalent inhibitors: a rational approach to drug discovery

Author affiliations

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

Back to tab navigation

Article information


Submitted
09 May 2020
Accepted
19 Jun 2020
First published
02 Jul 2020

This article is Open Access

RSC Med. Chem., 2020,11, 876-884
Article type
Review Article

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

This article is licensed under a Creative Commons Attribution-NonCommercial 3.0 Unported Licence. Material from this article can be used in other publications provided that the correct acknowledgement is given with the reproduced material and it is not used for commercial purposes.

Reproduced material should be attributed as follows:

  • For reproduction of material from NJC:
    [Original citation] - Published by The Royal Society of Chemistry (RSC) on behalf of the Centre National de la Recherche Scientifique (CNRS) and the RSC.
  • For reproduction of material from PCCP:
    [Original citation] - Published by the PCCP Owner Societies.
  • For reproduction of material from PPS:
    [Original citation] - Published by The Royal Society of Chemistry (RSC) on behalf of the European Society for Photobiology, the European Photochemistry Association, and RSC.
  • For reproduction of material from all other RSC journals:
    [Original citation] - Published by The Royal Society of Chemistry.

Information about reproducing material from RSC articles with different licences is available on our Permission Requests page.


Social activity

Search articles by author

Spotlight

Advertisements