Shaw, Duncan, Smith, Nichola, Cotesta, Simona, Williams, Gareth, Sohal, Bindi, Rynn, Caroline, Troxler, Thomas J., D'Souza, Anne-Marie, Lattmann, Rene, Beerli, Rene, Pulz, Robert, Guth-Gundel, Sabine and Rowlands, David (2023) Design and synthesis of inhibitors of the E3 ligase SMAD Specific E3 Ubiquitin Protein Ligase 1 (SMURF1) as a treatment for lung remodeling in Pulmonary Arterial Hypertension (PAH). Journal of medicinal chemistry. ISSN 1520-4804; 0022-2623

Abstract

Design and synthesis of inhibitors of the E3 ligase SMAD Specific E3 Ubiquitin Protein Ligase 1 (SMURF1) as a treatment for lung remodeling in Pulmonary Arterial Hypertension (PAH)
A series of selective SMURF1 ligase inhibitors have been identified, optimized for potency and properties to enable excellant rat pharmacokinetic properties. Furthermore compounds from the series have been shown to potently block the remodeling of vascular smooth muscle in the rat Hypoxia –Sugen model of PAH.

Item Type:	Article
Keywords:	SMURF1, LIGASE, PAH,
Date Deposited:	20 Jul 2023 00:45
Last Modified:	20 Jul 2023 00:45
URI:	https://oak.novartis.com/id/eprint/48049