Selection Method of DNA-Encoded Chemical Library for Irreversible Covalent Binders

Zhengrong Zhu

doi:10.1007/978-1-0716-2545-3_20

Selection Method of DNA-Encoded Chemical Library for Irreversible Covalent Binders

Methods Mol Biol. 2022:2541:165-172. doi: 10.1007/978-1-0716-2545-3_20.

Author

Zhengrong Zhu¹

Affiliation

¹ Merck Research Laboratories, Kenilworth, NJ, USA. [email protected].

PMID: 36083555
DOI: 10.1007/978-1-0716-2545-3_20

Abstract

Compounds acting through irreversible covalent interactions with therapeutic targets represent an important mechanism of drug action. Here I describe a selection method for DNA-encoded libraries to discover irreversible covalent binders to target proteins. This method offers an enabling tool in drug discovery for therapeutic targets that may be undruggable for reversible inhibition.

Keywords: Covalent; DNA-encoded library (DEL); Irreversible; Selection.

MeSH terms

DNA* / chemistry
Drug Discovery
Gene Library
Proteins
Small Molecule Libraries* / pharmacology

Substances

Proteins
Small Molecule Libraries
DNA