Belumosudil, ROCK2-specific inhibitor, alleviates cardiac fibrosis by inhibiting cardiac fibroblasts activation
Quan Liu, Huayang Li, Shunjun Wang, Suiqing Huang, Yuan Yue, Adilai Maihemuti, Yi Zhang, Lin Huang, Li Luo, Kangni Feng, Zhongkai Wu
Abstract
Although ρ-associated kinase-2 (ROCK2) is the main isoform of ρ-associated kinases (ROCKs) in the heart and more important in cardiac hypertrophy and fibrosis than ρ-associated kinase-1 (ROCK1), there has not been any pharmacological approach to inhibit ROCK2 selectively. Our study demonstrates for the first time that belumosudil, the first ROCK2-specific inhibitor, effectively ameliorates cardiac hypertrophy, fibrosis, and dysfunction induced by TAC via inhibiting cardiac fibroblasts activation.
Topics & Concepts
Pressure overloadCardiac fibrosisFibrosisROCK2MedicineROCK1Muscle hypertrophyMyofibroblastMyocardial fibrosisInternal medicineEndocrinologyKinaseCancer researchRho-associated protein kinaseProtein kinase ABiologyCardiac hypertrophyCell biologyCardiac Fibrosis and RemodelingSignaling Pathways in DiseasePeptidase Inhibition and Analysis