Synthesis and Characterization of Reversible Covalent HDAC4 Inhibitors

Overview

Journal Methods Mol Biol

Specialty Molecular Biology

Date 2022 Oct 18

PMID 36255627

Authors

Anton Fruhauf

Benjamin Wolff

Markus Schweipert

Franz-Josef Meyer-Almes

Affiliations

Soon will be listed here.

Abstract

Cyanoacrylates define a class of inhibitors which are capable to form a transient covalent bond with a cysteine flanking the binding site, thereby increasing the residence time and prolonging the inhibitory effect on the target protein under nonequilibrium conditions. Herein, we describe the synthetic access to cyanoacrylate-based HDAC4 inhibitors and the procedures for the characterization of the transient nature of the covalent bond between cyanoacrylates and thiols or cysteines in HDAC4.

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PMID: 38567529 PMC: 11040609. DOI: 10.1021/acschembio.3c00805.

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