Drug intelligence / Profile preview

SR3335

Development stage
Preclinical
Lead developer
Scripps Research
Modality
Small Molecules
Administration
Intraperitoneal
01

Overview

SR3335 is a selective small-molecule inverse agonist of the retinoic acid-related orphan receptor-alpha (RORα). It is primarily utilized as a chemical probe to study the role of RORα in various pathophysiological processes, including circadian rhythm, lipid metabolism, and more recently, fibrotic tissue remodeling. In the context of fibrosis, SR3335 has been shown to attenuate fibroblast activation and myofibroblast differentiation by modulating the Hippo signaling pathway, specifically reducing the nuclear translocation and levels of YAP and TAZ. Preclinical studies in mouse models of systemic sclerosis, pulmonary fibrosis, and liver fibrosis have demonstrated its efficacy in reducing collagen deposition and fibrotic gene expression, positioning RORα as a potential therapeutic target for systemic sclerosis and other fibrotic diseases.

02

Targets

PXR (Pregnane X receptor)LXRB (Liver X receptor beta)RORA (Retinoic acid-related orphan receptor alpha)

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