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.

https://pubs.acs.org/doi/full/10.1021/acs.jmedchem.1c02109