ROCK1 inhibitor

ROCK1 inhibitors are a class of pharmacological agents that target Rho-associated protein kinase 1 (ROCK1), a serine/threonine kinase that serves as a key downstream effector of the Rho GTPase signaling pathway. ROCK1 is primarily involved in regulating the actin cytoskeleton, cell polarity, migration, and gene expression. Dysregulation of ROCK signaling is implicated in various pathologies, including cardiovascular diseases, fibrotic disorders, and metabolic conditions. While many inhibitors in this class are pan-ROCK inhibitors targeting both ROCK1 and ROCK2 isoforms, research has identified distinct roles for ROCK1, such as its negative regulation of fatty acid energy metabolism in kidney tubules, making it a target for diabetic kidney disease. A prominent clinical-stage candidate in this class is ROC-101, an oral small molecule pan-ROCK inhibitor being developed for pulmonary arterial hypertension (PAH) and pulmonary hypertension associated with interstitial lung disease (ILD-PH).

Other names

Rho-associated protein kinase 1 inhibitorROCK inhibitorROCK1 inhibitorROCK-1 inhibitorROCK 1 inhibitor