Biochemical Characterization and Structure-Based Mutational Analysis Provide Insight into the Binding and Mechanism of Action of Novel Aspartate Aminotransferase Inhibitors

Author:

Holt Melissa C.1,Assar Zahra1,Beheshti Zavareh Reza2,Lin Lin3,Anglin Justin2,Mashadova Oksana4,Haldar Daniel5,Mullarky Edouard4,Kremer Daniel M.3,Cantley Lewis C.4,Kimmelman Alec C.6,Stein Adam J.1,Lairson Luke L.27ORCID,Lyssiotis Costas A.8ORCID

Affiliation:

1. Cayman Chemical Company, 1180 East Ellsworth, Ann Arbor, Michigan 48108, United States

2. California Institute for Biomedical Research, 11119 North Torrey Pines Road, La Jolla, California 92037, United States

3. Department of Molecular and Integrative Physiology, University of Michigan Medical School, Ann Arbor, Michigan 48109, United States

4. Meyer Cancer Center, Department of Medicine, Weill Cornell Medical College, New York, New York 10065, United States

5. Department of Systems Biology, Harvard Medical School, Boston, Massachusetts 02215, United States

6. Department of Radiation Oncology, Perlmutter Cancer Center, NYU Langone Medical Center, New York, New York 10016, United States

7. Department of Chemistry, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, California 92037, United States

8. Department of Molecular and Integrative Physiology, Department of Internal Medicine, Division of Gastroenterology, and Rogel Cancer Center, University of Michigan, Ann Arbor, Michigan 48109, United States

Funder

American Association for Cancer Research

National Cancer Institute

University of Michigan

Damon Runyon Cancer Research Foundation

National Institute of Diabetes and Digestive and Kidney Diseases

Lustgarten Foundation

Sidney Kimmel Foundation for Cancer Research

V Foundation for Cancer Research

Pancreatic Cancer Action Network

Charles Woodson Research Fund, University of Michigan

Publisher

American Chemical Society (ACS)

Subject

Biochemistry

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