Discovery, SAR, and X-ray Binding Mode Study of BCATm Inhibitors from a Novel DNA-Encoded Library-Reference-Cited by-同舟云学术

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

Published:2015-07-24 Issue:8 Volume:6 Page:919-924
ISSN:1948-5875
Container-title:ACS Medicinal Chemistry Letters
language:en
Short-container-title:ACS Med. Chem. Lett.

Author:

Deng Hongfeng¹,Zhou Jingye¹,Sundersingh Flora S.¹,Summerfield Jennifer¹,Somers Don²,Messer Jeffrey A.¹,Satz Alexander L.¹,Ancellin Nicolas³,Arico-Muendel Christopher C.¹,(Sargent) Bedard Katie L.¹,Beljean Arthur²,Belyanskaya Svetlana L.¹,Bingham Ryan²,Smith Sarah E.²,Boursier Eric³,Carter Paul²,Centrella Paolo A.¹,Clark Matthew A.¹,Chung Chun-wa²,Davie Christopher P.¹,Delorey Jennifer L.¹,Ding Yun¹,Franklin G. Joseph¹,Grady LaShadric C.¹,Herry Kenny³,Hobbs Clare²,Kollmann Christopher S.¹,Morgan Barry A.¹,(Pothier) Kaushansky Laura J.¹,Zhou Quan⁴

Affiliation:

1. Platform 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, Brandeis University, Waltham, Massachusetts 02453, United States

Publisher

American Chemical Society (ACS)

Subject

Organic Chemistry,Drug Discovery,Biochemistry

Link

https://pubs.acs.org/doi/pdf/10.1021/acsmedchemlett.5b00179

Reference17 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. Signaling Pathways and Molecular Mechanisms through which Branched-Chain Amino Acids Mediate Translational Control of Protein Synthesis

4. Does leucine, leucyl-tRNA, or some metabolite of leucine regulate protein synthesis and degradation in skeletal and cardiac muscle?

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

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