Identification of Novel Therapies for lung fibrosis and Glaucoma.

National Center For Advancing Translational Sciences

Investigators

Abstract

The goal of this program is to perform a small molecule screen to identify a new class of compounds which can act as myosolvins by disrupting myosin polymerization, and serve as a novel therapeutic to relax airway bronchoconstriction. Prior to this period, the collaborative team identified small molecules that inhibit smooth muscle myosin polymerization, relax human airway myocytes, and blunt bronchoconstriction in mouse lung slices and selected a lead compound for optimization towards desirable pharmacological and pharmaceutical properties. During this period, numerous active analogs have been synthesized and tested as part of an extensive Structure-Activity Relationship (SAR) campaign. Concurrent efforts include target identification through a variety of cell-based and proteomic assays.