Reactive fragments targeting carboxylate residues employing direct to biology, high-throughput chemistry

Ross P. Thomas; Emma K. Grant; Eleanor R. Dickinson; Francesca Zappacosta; Lee J. Edwards; Michael M. Hann; David House; Nicholas C. O. Tomkinson; Jacob T. Bush

doi:10.1039/d2md00453d

journal article Open Access Jan 01, 2023

Reactive fragments targeting carboxylate residues employing direct to biology, high-throughput chemistry

Ross P. Thomas Emma K. Grant Eleanor R. Dickinson

Francesca Zappacosta Lee J. Edwards

Michael M. Hann

David House

Nicholas C. O. Tomkinson

Jacob T. Bush

RSC Medicinal Chemistry Vol. 14 No. 4 pp. 671-679 · Royal Society of Chemistry (RSC)

View at Publisher Save 10.1039/d2md00453d

Abstract

We present a carboxylate-targeting reactive fragment screening platform using 2-aryl-5-carboxytetrazole (ACT) as the photoreactive functionality. This work will provide a simple accessible method to rapidly discover tool molecules to interrogate important biological targets.

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Details

Published: Jan 01, 2023
Vol/Issue: 14(4)
Pages: 671-679
License: View

Authors

R

Ross P. Thomas

GlaxoSmithKline, Gunnels Wood Road, Stevenage, Hertfordshire, SG1 2NY, UK; Department of Pure and Applied Chemistry, University of Strathclyde, 295 Cathedral Street, Glasgow, G1 1XL, UK

E

Emma K. Grant