Small molecule agonists of the relaxin 1 receptor

National Center For Advancing Translational Sciences

Investigators

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Abstract

During this period, the collaborative team has worked to characterize the lead molecules using in vitro assays and in vivo models. In vivo pharmacokinetics and efficacy data were obtained for several molecules, identifying metabolically stable analogues displaying good pharmacokinetics. Additional formulation studies and corresponding PK studies have been completed, as well as testing of compounds in functional assays and in vivo models is ongoing. CryoEM structural determination of small molecule binding to the receptor is underway. The best optimized molecule has been evaluated in several models of fibrosis, pulmonary hypertension and cancer disease with encouraging results.