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Novel ROCK inhibitors for the treatment of pulmonary arterial hypertension.

Shaw D, Hollingworth G, Soldermann N, Sprague E, Schuler W, Vangrevelinghe E, Duggan N, Thomas M, Kosaka T, Waters N, van Eis MJ
Bioorg Med Chem Lett 24 4812-7 (2014)
Cited: 18 times
EuropePMC logo PMID: 25248678

Abstract

A novel class of selective inhibitors of ROCK1 and ROCK2 has been identified by structural based drug design. PK/PD experiments using a set of highly selective Rho kinase inhibitors suggest that systemic Rho kinase inhibition is linked to a reversible reduction in lymphocyte counts. These results led to the consideration of topical delivery of these molecules, and to the identification of a lead molecule 7 which shows promising PK and PD in a murine model of pulmonary hypertension after intra-tracheal dosing.

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Reviews citing this publication (5)

  1. Rho kinase inhibitors: a patent review (2014 - 2016). Defert O, Boland S. Expert Opin Ther Pat 27 507-515 (2017)
  2. Discovery of Molecular Therapeutics for Glaucoma: Challenges, Successes, and Promising Directions. Donegan RK, Lieberman RL. J Med Chem 59 788-809 (2016)
  3. Investigational Rho Kinase Inhibitors for the Treatment of Glaucoma. Al-Humimat G, Marashdeh I, Daradkeh D, Kooner K. J Exp Pharmacol 13 197-212 (2021)
  4. Rho Kinases in Embryonic Development and Stem Cell Research. Shi J, Wei L. Arch Immunol Ther Exp (Warsz) 70 4 (2022)
  5. Insight Into Rho Kinase Isoforms in Obesity and Energy Homeostasis. Wei L, Shi J. Front Endocrinol (Lausanne) 13 886534 (2022)

Articles citing this publication (9)

  1. ROCK Inhibition Promotes Attachment, Proliferation, and Wound Closure in Human Embryonic Stem Cell-Derived Retinal Pigmented Epithelium. Croze RH, Thi WJ, Clegg DO. Transl Vis Sci Technol 5 7 (2016)
  2. In silico prediction of ROCK II inhibitors by different classification approaches. Cai C, Wu Q, Luo Y, Ma H, Shen J, Zhang Y, Yang L, Chen Y, Wen Z, Wang Q, Wang Q. Mol Divers 21 791-807 (2017)
  3. LncRNA PAXIP1-AS1 fosters the pathogenesis of pulmonary arterial hypertension via ETS1/WIPF1/RhoA axis. Song R, Lei S, Yang S, Wu SJ. J Cell Mol Med 25 7321-7334 (2021)
  4. Design, synthesis and biological evaluations of a long-acting, hypoxia-activated prodrug of fasudil, a ROCK inhibitor, to reduce its systemic side-effects. Al-Hilal TA, Hossain MA, Alobaida A, Alam F, Keshavarz A, Nozik-Grayck E, Stenmark KR, German NA, Ahsan F. J Control Release 334 237-247 (2021)
  5. Development of 2-(4-pyridyl)-benzimidazoles as PKN2 chemical tools to probe cancer. Scott F, Fala AM, Pennicott LE, Reuillon TD, Massirer KB, Elkins JM, Ward SE. Bioorg Med Chem Lett 30 127040 (2020)
  6. Polymorphisms and haplotype of ROCK2 associate with high altitude essential hypertension in native high altitude Ladakhi Indian population: a preliminary study. Pandey P, Mohammad G, Singh Y, Pasha MA. Clin Exp Hypertens 38 238-244 (2016)
  7. Cardiac Safety of Kinase Inhibitors - Improving Understanding and Prediction of Liabilities in Drug Discovery Using Human Stem Cell-Derived Models. Ziegler R, Häusermann F, Kirchner S, Polonchuk L. Front Cardiovasc Med 8 639824 (2021)
  8. High-throughput screening against ~6.1 million structurally diverse, lead-like compounds to discover novel ROCK inhibitors for cerebral injury recovery. Gong H, Yuan Z, Zhan L. Mol Divers 20 537-549 (2016)
  9. Tankyrase inhibition interferes with junction remodeling, induces leakiness, and disturbs YAP1/TAZ signaling in the endothelium. Ma N, Wibowo YC, Wirtz P, Baltus D, Wieland T, Jansen S. Naunyn Schmiedebergs Arch Pharmacol (2023)


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