Wednesday, August 24, 2016

Development of Specific, Irreversible Inhibitors for a Receptor Tyrosine Kinase EphB3

Development of Specific, Irreversible Inhibitors for a Receptor Tyrosine Kinase EphB3

Alvin Kung, Ying-Chu Chen, Marianne Schimpl, Feng Ni, Jianfa Zhu, Maurice Turner, Henrik Molina, Ross Overman, and Chao Zhang

Department of Chemistry and Loker Hydrocarbon Research Institute, and Department of Biological Sciences, University of Southern California, Los Angeles, California 90089, United States
Discovery Sciences, Innovative Medicines and Early Development Biotech Unit, AstraZeneca, Building 310, Cambridge Science Park, Milton Road, Cambridge CB4 0WG, United Kingdom
Discovery Sciences, Innovative Medicines and Early Development Biotech Unit, AstraZeneca, Alderley Park, Macclesfield, Cheshire SK10 4TG, United Kingdom
Proteomic Resource Center, The Rockefeller University, New York, New York 10065, United States
J. Am. Chem. Soc., 2016, 138 (33), pp 10554–10560
DOI: 10.1021/jacs.6b05483
*zhang.chao@usc.edu

A covalent irreversible inhibitor binds in two mutually exclusive conformations to the active-site cysteine residue of human aldehyde dehydrogenase 1A3

Daniela Covaleda, David Vizarraga, Tulsi Upadhyay, Jiyun Zhu, Daniel Abegg, Raquel Pequerul, Martín Hugo, Alexander Adibekian, Ignacio Fita,...