Structure-based design of ASK1 inhibitors as potential agents for heart failure

M Lanier, J Pickens, SV Bigi… - ACS medicinal …, 2017 - ACS Publications
M Lanier, J Pickens, SV Bigi, EL Bradshaw-Pierce, A Chambers, ZS Cheruvallath, D Cole…
ACS medicinal chemistry letters, 2017ACS Publications
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.
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.
ACS Publications