期刊
ACS MEDICINAL CHEMISTRY LETTERS
卷 8, 期 3, 页码 316-320出版社
AMER CHEMICAL SOC
DOI: 10.1021/acsmedchemlett.6b00481
关键词
Apoptosis signal-regulating kinase 1 (ASK1); structure-based drug design (SBDD); cardiac injury
资金
- Office of Science, Office of Basic Energy Sciences, of the U.S. Department of Energy [DE-AC02-05CH11231]
- DOE Office of Science [DE-AC02-06CH11357]
Apoptosis signal-regulating kinase 1 (ASK1/ MAP3K) is a mitogen-activated protein kinase family member shown to contribute to acute ischemia/reperfusion injury. Using structure-based drug design, deconstruction, and reoptimization of a known ASK1 inhibitor, a lead compound was identified. This compound displayed robust MAP3K pathway inhibition and reduction of infarct size in an isolated perfused heart model of cardiac injury.
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