Optimization and Mechanistic Investigations of Novel Allosteric Activators of PKG1α

WuXi AppTec scientists recently contributed to a research article in the Journal of Medicinal Chemistry describing the optimization of a piperidine series of small molecules as novel allosteric activators of PKG1α (a compelling drug target for treatment of cardiovascular diseases).  This study reveals a mechanism of action for these compounds consistent with cGMP-induced activation, including antiproliferative effects in human pulmonary arterial smooth muscle cells.


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