Structurally Diverse Mitochondrial Branched Chain Aminotransferase (BCATm) Leads with Varying Binding Modes Identified by Fragment Screening-Reference-Cited by-同舟云学术

Structurally Diverse Mitochondrial Branched Chain Aminotransferase (BCATm) Leads with Varying Binding Modes Identified by Fragment Screening

Published:2016-03-16 Issue:6 Volume:59 Page:2452-2467
ISSN:0022-2623
Container-title:Journal of Medicinal Chemistry
language:en
Short-container-title:J. Med. Chem.

Author:

Borthwick Jennifer A.¹²,Ancellin Nicolas³,Bertrand Sophie M.¹²,Bingham Ryan P.¹,Carter Paul S.¹,Chung Chun-wa¹,Churcher Ian¹,Dodic Nerina³,Fournier Charlène¹,Francis Peter L.¹,Hobbs Andrew¹,Jamieson Craig²,Pickett Stephen D.¹,Smith Sarah E.¹,Somers Donald O’N.¹,Spitzfaden Claus¹,Suckling Colin J.²,Young Robert J.¹

Affiliation:

1. Medicines Research Centre, GlaxoSmithKline R&D, Gunnels Wood Road, Stevenage, Hertfordshire, SG1 2NY, U.K.

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

3. Les Ulis, Centre de Recherche, GlaxoSmithKline R&D, 25,27 Avenue du Québec, 91140 Villebon sur Yvette, France

Publisher

American Chemical Society (ACS)

Subject

Drug Discovery,Molecular Medicine

Link

https://pubs.acs.org/doi/pdf/10.1021/acs.jmedchem.5b01607

Reference25 articles.

1. Branched-chain amino acid catabolism: unique segregation of pathway enzymes in organ systems and peripheral nerves

2. Disruption of BCATm in Mice Leads to Increased Energy Expenditure Associated with the Activation of a Futile Protein Turnover Cycle

3. Disruption of BCAA metabolism in mice impairs exercise metabolism and endurance

4. The Discovery of in Vivo Active Mitochondrial Branched-Chain Aminotransferase (BCATm) Inhibitors by Hybridizing Fragment and HTS Hits

5. Discovery, SAR, and X-ray Binding Mode Study of BCATm Inhibitors from a Novel DNA-Encoded Library

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