Application of covalent modality in proximity-induced drug pharmacology: Early development, current strategy, and feature directions

Eur J Med Chem. 2024 Apr 17;271:116394. doi: 10.1016/j.ejmech.2024.116394. Online ahead of print.ABSTRACTWith a growing number of covalent drugs securing FDA approval as successful therapies across various indications, particularly in the realm of cancer treatment, the covalent modulating strategy is undergoing a resurgence. The renewed interest in covalent bioactive compounds has captured significant attention from both the academic and biopharmaceutical industry sectors. Covalent chemistry presents several advantages over traditional noncovalent proximity-induced drugs, including heightened potency, reduced molecular size, and the ability to target "undruggable" entities. Within this perspective, we have compiled a comprehensive overview of current covalent modalities applied to proximity-induced molecules, delving into their advantages and drawbacks. Our aim is to stimulate more profound insights and ideas within the scientific community, guiding future research endeavors in this dynamic field.PMID:38643668 | DOI:10.1016/j.ejmech.2024.116394
Source: European Journal of Medicinal Chemistry - Category: Chemistry Authors: Source Type: research