Plasminogen activator inhibitor-1 (PAI-1) is an endogenous serine protease inhibitor, pathologic levels of which have been implicated in a variety of conditions, including atherosclerosis, myocardial infarction, type 2 diabetes, and cancer. The development of potent and selective inhibitors of PAI-1 has therefore become a priority. A small-molecule inhibitor of PAI-1 based on a novel scaffold was identified by high-throughput screening and subsequent spectroscopic analysis of the screening mixture that provided the screening hit. The method of identification of the active component will be discussed, as will initial screening of related molecules as inhibitors of PAI-1.

Identification of a novel small-molecule inhibitor of plasminogen activator inhibitor-1

248th National Meeting (2014)

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