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Cover Feature: Covalent Inhibition in Drug Discovery (ChemMedChem 9/2019)
Author(s) -
Ghosh Avick Kumar,
Samanta Indranil,
Mondal Anushree,
Liu Wenshe Ray
Publication year - 2019
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.201900236
Subject(s) - covalent bond , chemistry , alkene , nucleophile , electrophile , combinatorial chemistry , adduct , conjugate , nitrile , stereochemistry , organic chemistry , mathematical analysis , mathematics , catalysis
The Cover Feature shows notable covalent inhibitors and structures of their complexes with protein targets. Covalent inhibitors involve mainly electrophilic functional groups to form covalent adducts with nucleophilic amino acid residues in protein targets. These functional groups include electrodeficient alkene, nitrile, lactone, lactam, expoxide, alkylhalide, etc.. A notable exception are thiol‐containing compounds that are redox active to conjugate to cysteines in proteins. More information can be found in the Review by Wenshe Liu et al. on page 889 in Issue 9, 2019 (DOI: 10.1002/cmdc.201900107).