Reactive fragments targeting carboxylate residues employing direct to biology, high-throughput chemistry-Reference-Cited by-同舟云学术

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

Published:2023 Issue:4 Volume:14 Page:671-679
ISSN:2632-8682
Container-title:RSC Medicinal Chemistry
language:en
Short-container-title:RSC Med. Chem.

Author:

Thomas Ross P.¹²,Grant Emma K.¹,Dickinson Eleanor R.¹^ORCID,Zappacosta Francesca³,Edwards Lee J.¹^ORCID,Hann Michael M.¹^ORCID,House David¹^ORCID,Tomkinson Nicholas C. O.²^ORCID,Bush Jacob T.¹^ORCID

Affiliation:

1. GlaxoSmithKline, Gunnels Wood Road, Stevenage, Hertfordshire, SG1 2NY, UK

2. Department of Pure and Applied Chemistry, University of Strathclyde, 295 Cathedral Street, Glasgow, G1 1XL, UK

3. GlaxoSmithKline, South Collegeville Road, Collegeville, PA 19426, USA

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.

Funder

Engineering and Physical Sciences Research Council

University of Strathclyde

GlaxoSmithKline

Publisher

Royal Society of Chemistry (RSC)

Subject

Organic Chemistry,Drug Discovery,Pharmaceutical Science,Pharmacology,Molecular Medicine,Biochemistry

Link

http://pubs.rsc.org/en/content/articlepdf/2023/MD/D2MD00453D

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1. Discovery of a Covalent Inhibitor of KRASG12C (AMG 510) for the Treatment of Solid Tumors