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, 2017•ACS PublicationsApoptosis 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.
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