Where Electrophile Signaling and Covalent Ligand–Target Mining Converge

Authors

  • Yimon Aye Swiss Federal Institute of Technology Lausanne (EPFL), CH-1015 Lausanne, Switzerland;, Email: yimon.aye@epfl.ch

DOI:

https://doi.org/10.2533/chimia.2020.659

PMID:

32958101

Keywords:

Covalent ligands, Electrophile signalling, Ligand–target mining

Abstract

Interests in learning how to engineer most effective covalent ligands, identify novel functional targets, and define precise mechanism-of-action are rapidly growing in both academia and pharmaceutical industries. We here illuminate the establishment of a multifunctional platform that offers new capabilities to logically engineer covalent ligands and dissect 'on-target' bioactivity with precise biological context and precision hitherto inaccessible. Broadly aimed at non-specialist readers, this opinion piece is aimed to stoke the interest of emerging chemists and biologists/bioengineers, but the underlying technological and conceptual topicality is anticipated to also appeal to experts leading ligand–target mining, validation, and -discovery research programs.

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Published

2020-09-30