ROCK Inhibition as Potential Target for Treatment of Pulmonary Hypertension

Cells. 2021 Jun 30;10(7):1648. doi: 10.3390/cells10071648.

Abstract

Pulmonary hypertension (PH) is a cardiovascular disease caused by extensive vascular remodeling in the lungs, which ultimately leads to death in consequence of right ventricle (RV) failure. While current drugs for PH therapy address the sustained vasoconstriction, no agent effectively targets vascular cell proliferation and tissue inflammation. Rho-associated protein kinases (ROCKs) emerged in the last few decades as promising targets for PH therapy, since ROCK inhibitors demonstrated significant anti-remodeling and anti-inflammatory effects. In this review, current aspects of ROCK inhibition therapy are discussed in relation to the treatment of PH and RV dysfunction, from cell biology to preclinical and clinical studies.

Keywords: ROCK; pulmonary hypertension; right ventricle dysfunction.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Clinical Trials as Topic
  • Disease Models, Animal
  • Drug Approval
  • Humans
  • Hypertension, Pulmonary / drug therapy*
  • Protein Kinase Inhibitors / pharmacology
  • Protein Kinase Inhibitors / therapeutic use*
  • rho-Associated Kinases / antagonists & inhibitors*
  • rho-Associated Kinases / chemistry
  • rho-Associated Kinases / metabolism

Substances

  • Protein Kinase Inhibitors
  • rho-Associated Kinases