期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 21, 期 10, 页码 3078-3083出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2011.03.032
关键词
PDK1; Selective; Tethering; Pyridinone; DFG-out; Fragment-based drug discovery
We report the use of a fragment-based lead discovery method, Tethering with extenders, to discover a pyridinone fragment that binds in an adaptive site of the protein PDK1. With subsequent medicinal chemistry, this led to the discovery of a potent and highly selective inhibitor of PDK1, which binds in the 'DFG-out' conformation. (C) 2011 Elsevier Ltd. All rights reserved.
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