Category

Archives

ROCK

ROCK Inhibitors as an Alternative Therapy for Corneal Grafting: A Systematic Review

922 views | Feb 15 2024

The review on ROCK inhibitors for corneal wound healing showcases their diverse therapeutic potential across various ocular conditions, offering promise as an effective alternative to human donor tissue for addressing the significant unmet medical need in corneal blindness. [Read the Full Post]

Correlating Basal Gene Expression across Chemical Sensitivity Data to Screen for Novel Synergistic Interactors of HDAC Inhibitors in Pancreatic Carcinoma

228 views | Dec 22 2023

This study employs a bioinformatics screening protocol integrating drug-sensitivity data and basal gene expression to predict synergistic combinations of histone deacetylase inhibitors (HDACi), identifying the sphingolipid signaling pathway as a promising target; further experimental validation reveals novel synergisms between HDACi and a Rho-associated protein kinase (ROCK) inhibitor RKI-1447, as well as between HDACi and a sphingosine 1-phosphate (S1P) receptor agonist fingolimod in the treatment of pancreatic ductal adenocarcinoma (PDAC). [Read the Full Post]

5-HT6 receptor antagonists. Design, synthesis, and structure-activity relationship of substituted 2-(1-methyl-4-piperazinyl)pyridines

338 views | Dec 16 2023

The study presents a novel series of 6-piperazinyl-7-azaindoles demonstrating potent 5-HT6 receptor antagonism, with a focus on optimizing the lead structure and exploring structure-activity relationships, highlighting Compound 29 as a promising candidate for further drug development. [Read the Full Post]

Identifying promising GSK3β inhibitors for cancer management: a computational pipeline combining virtual screening and molecular dynamics simulations

306 views | Nov 21 2023

The computational screening study identified BMS-754807 and GSK429286A as promising GSK3β inhibitors with high binding affinities, suggesting their potential as novel anticancer drugs pending experimental validation. [Read the Full Post]

Effectiveness of netarsudil 0.02% in lowering intraocular pressure in patients with secondary glaucoma

356 views | Oct 01 2023

Netarsudil, 0.02%, was found to be effective in lowering intraocular pressure (IOP) in patients with secondary forms of glaucoma, especially uveitic glaucoma. [Read the Full Post]

Effectiveness of netarsudil 0.02% in lowering intraocular pressure in patients with secondary glaucoma

477 views | Sep 27 2023

Netarsudil, 0.02%, was found to effectively lower intraocular pressure in patients with secondary forms of glaucoma, particularly uveitic glaucoma, based on a retrospective study. [Read the Full Post]

Ripasudil-Brimonidine Fixed-Dose Combination vs Ripasudil or Brimonidine: Two Phase 3 Randomized Clinical Trials

336 views | Jul 10 2023

The results of the study demonstrated that the ripasudil-brimonidine fixed-dose combination (RBFC) had a greater ability to lower intraocular pressure (IOP) compared to ripasudil or brimonidine alone. [Read the Full Post]

Topical Ripasudil for the Treatment of Segmental Corneal Edema: A Case Series

505 views | Jul 10 2023

Topical ripasudil has shown promising results in improving vision and resolving corneal edema in patients with focal corneal edema following anterior segment surgeries, serving as an effective treatment option that may reduce the need for endothelial transplantation. [Read the Full Post]

Discovery of indoline-based derivatives as effective ROCK2 inhibitors for the potential new treatment of idiopathic pulmonary fibrosis

378 views | Jul 07 2023

A new series of selective ROCK2 inhibitors based on indoline, particularly compound 9b, showed promising results in inhibiting collagen gel contraction, suppressing fibrotic markers, and exhibiting anti-pulmonary fibrosis effects in a bleomycin-induced IPF rat model, suggesting its potential as a lead compound for IPF treatment. [Read the Full Post]

Comparative transcriptome profile of mouse macrophages treated with the RhoA/Rock pathway inhibitors Y27632, Fingolimod (Gilenya), and Rezurock (Belumosudil, SLx-2119)

310 views | Jul 07 2023

The transcriptome profiling study comparing macrophages treated with Y27632, Fingolimod, and Rezurock revealed distinct downregulation of GTPase and actin pathways in cell migration for Y27632 and Fingolimod, while Rezurock specifically downregulated fibrosis-related genes, providing insights into the differences in their anti-chronic rejection properties and aiding in the development of targeted therapies. [Read the Full Post]