期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 22, 期 24, 页码 7523-7529出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2012.10.039
关键词
PYK2; FAK; DFG-out; Osteoporosis; Kinase inhibitor; BIRB-796
Previous drug discovery efforts identified classical PYK2 kinase inhibitors such as 2 and 3 that possess selectivity for PYK2 over its intra-family isoform FAK. Efforts to identify more kinome-selective chemical matter that stabilize a DFG-out conformation of the enzyme are described herein. Two sub-series of PYK2 inhibitors, an indole carboxamide-urea and a pyrazole-urea have been identified and found to have different binding interactions with the hinge region of PYK2. These leads proved to be more selective than the original classical inhibitors. (C) 2012 Elsevier Ltd. All rights reserved.
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