Discovery and Optimization of Potent, Selective, and in Vivo Efficacious 2-Aryl Benzimidazole BCATm Inhibitors-Reference-Cited by-同舟云学术

Discovery and Optimization of Potent, Selective, and in Vivo Efficacious 2-Aryl Benzimidazole BCATm Inhibitors

Published:2016-02-12 Issue:4 Volume:7 Page:379-384
ISSN:1948-5875
Container-title:ACS Medicinal Chemistry Letters
language:en
Short-container-title:ACS Med. Chem. Lett.

Author:

Deng Hongfeng¹,Zhou Jingye¹,Sundersingh Flora¹,Messer Jeffrey A.¹,Somers Donald O.²,Ajakane Myriam³,Arico-Muendel Christopher C.¹,Beljean Arthur²,Belyanskaya Svetlana L.¹,Bingham Ryan²,Blazensky Emily⁴,Boullay Anne-Benedicte³,Boursier Eric³,Chai Jing¹,Carter Paul²,Chung Chun-Wa²,Daugan Alain³,Ding Yun¹,Herry Kenny³,Hobbs Clare²,Humphries Eric⁴,Kollmann Christopher¹,Nguyen Van Loc³,Nicodeme Edwige³,Smith Sarah E.²,Dodic Nerina³,Ancellin Nicolas³

Affiliation:

1. Platform of Technology and Science, GlaxoSmithKline, 830 Winter Street, Waltham, Massachusetts 02451, United States

2. Medicines Research Centre, GlaxoSmithKline, Gunnels Wood Road, Stevenage, Herts, SG1 2NY, U.K.

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

4. Chemistry Department, Northeastern University, Boston, Massachusetts 02115, United States

Publisher

American Chemical Society (ACS)

Subject

Organic Chemistry,Drug Discovery,Biochemistry

Link

https://pubs.acs.org/doi/pdf/10.1021/acsmedchemlett.5b00389

Reference12 articles.

1. Structure and function of branched chain aminotransferases

2. Structural Determinants for Branched-chain Aminotransferase Isozyme-specific Inhibition by the Anticonvulsant Drug Gabapentin

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

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

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

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