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Last update 23 Jan 2025

Rho GTPase

Last update 23 Jan 2025

Basic Info

Synonyms-

Introduction-

Drugs associated with Rho GTPase

BAY-856

Target

Rho GTPase

Mechanism

Rho GTPase inhibitors

Active Org.

Nuvisan GmbH [+1]

Originator Org.-

Active Indication

Solid tumor

Inactive Indication-

Drug Highest PhasePreclinical

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

Praconase

Target

ROCK1 x Rho GTPase

Mechanism

ROCK1 inhibitors [+1]

Active Org.-

Originator Org.

BioAxone Therapeutic, Inc.

Active Indication-

Inactive Indication

acute spinal cord injury [+6]

Drug Highest PhaseDiscontinued

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

BA-207

Target

Rho GTPase

Mechanism

Rho GTPase inhibitors

Active Org.-

Originator Org.

BioAxone Therapeutic, Inc.

Active Indication-

Inactive Indication

Cardiovascular Diseases

Drug Highest PhasePending

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

Clinical Trials associated with Rho GTPase

NCT02669849

/ TerminatedPhase 2/3

A Phase 2b/3, Double-blind, Randomized, Placebo Controlled, Multicenter Study to Assess the Efficacy and Safety of VX-210 in Subjects With Acute Traumatic Cervical Spinal Cord Injury

The purpose of this study is to determine the efficacy and safety of VX-210 in subjects with Acute Traumatic Cervical Spinal Cord Injury. Secondary objectives include the specific evaluation of the effects of VX-210 on neurological recovery and daily function after spinal cord injury.

Start Date01 Jul 2016

Sponsor / Collaborator

Vertex Pharmaceuticals, Inc.

NCT02053883

/ WithdrawnPhase 2/3

A Phase II/III, Double-Blind, Randomized, Placebo-Controlled, Multicenter Study to Assess the Efficacy and Safety of Cethrin in Subjects With Acute Cervical Spinal Cord Injury

This is a multicenter, randomized, double-blind, placebo-controlled Phase IIb/III study designed to evaluate the efficacy and safety of Cethrin as a treatment for acute cervical spinal cord injury. During the trial, high and low doses of Cethrin will be compared with placebo.

Start Date01 Jul 2015

Sponsor / Collaborator

BioAxone BioSciences, Inc.

NCT00500812

/ CompletedPhase 1/2

A Phase I/IIa Dose-Ranging Study to Evaluate the Safety, Tolerability, and Pharmacokinetics of BA-210 and the Neurological Status of Patients Following Administration of a Single Extradural Application of Cethrin During Surgery for Acute Thoracic and Cervical Spinal Cord Injury

This trial is a multi-center, open-label, dose-escalation study designed to evaluate the safety, tolerability and pharmacokinetics of Cethrin in two types of spinal cord injury patients: those with a complete cervical injury or a complete thoracic injury. Dose levels from 0.3 mg - 9 mg of Cethrin will be administered.

Start Date01 Feb 2005

Sponsor / Collaborator

Vertex Pharmaceuticals, Inc.

100 Clinical Results associated with Rho GTPase

100 Translational Medicine associated with Rho GTPase

0 Patents (Medical) associated with Rho GTPase

3,372

Literatures (Medical) associated with Rho GTPase

01 Feb 2025·Glia

RhoA regulates oligodendrocyte differentiation and myelination by orchestrating cortical and membrane tension

Article

Author: de Paes de Faria, Joana ; Franklin, Robin J. M. ; Brakebusch, Cord ; Seixas, Ana Isabel ; Vale‐Silva, Raquel ; Relvas, João B.

AbstractTimely differentiation and myelin formation by oligodendrocytes are essential for the physiological functioning of the central nervous system (CNS). While the Rho GTPase RhoA has been hinted as a negative regulator of myelin sheath formation, the precise in vivo mechanisms have remained elusive. Here we show that RhoA controls the timing and progression of myelination by oligodendrocytes through a fine‐tuned balance between cortical tension, membrane tension and cell shape. Using a conditional mouse model, we observe that Rhoa ablation results in the acceleration of myelination driven by hastened differentiation and facilitated through membrane expansion induced by changes in MLCII activity and in F‐actin redistribution and turnover within the cell. These findings reveal RhoA as a central molecular integrator of alterations in actin cytoskeleton, actomyosin contractility and membrane tension underlying precise morphogenesis of oligodendrocytes and normal myelination of the CNS.

01 Feb 2025·Journal of Molecular Biology

Structural Dynamics of Rho GTPases

Review

Author: Zheng, Yi ; Lin, Yuan

Rho family GTPases are a part of the Ras superfamily and are signaling hubs for many cellular processes. While the detailed understanding of Ras structure and function has led to tremendous progress in oncogenic Ras-targeted drug discovery, studies of the related Rho GTPases are still catching up as the recurrent cancer-related Rho GTPase mutations have only been discovered in the last decade. Like that of Ras, an in-depth understanding of the structural basis of how Rho GTPases and their mutants behave as key oncogenic drivers benefits the development of clinically effective therapies. Recent studies of structure dynamics in Rho GTPase structure-function relationship have added new twists to the conventional wisdom of Rho GTPase signaling mechanism.

01 Jan 2025·Cellular Signalling

Regulation and functions of the DLC family of RhoGAP proteins: Implications for development and cancer

Review

Author: Olayioye, Monilola A. ; Frey, Yannick ; Lungu, Cristiana ; Olayioye, Monilola A

The DLC (Deleted in Liver Cancer) family of RhoGAP (Rho GTPase-activating) proteins has been extensively studied since the identification of the first family member nearly 30 years ago. Rho GTPase signaling is essential for various cellular processes, including cytoskeletal dynamics, cell migration, and proliferation. Members of the DLC family are key regulators of this signaling pathway, with well-established roles in development and carcinogenesis. Here, we provide a comprehensive review of research into DLC regulation and cellular functions over the last three decades. In particular, we summarize control mechanisms of DLC gene expression at both the transcriptional and post-transcriptional level. Additionally, recent advances in understanding the post-translational regulation of DLC proteins that allow for tuning of protein activity and localization are highlighted. This detailed overview will serve as resource for future studies aimed at further elucidating the complex regulatory mechanisms of DLC family proteins and exploring their potential as targets for therapeutic applications.

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Rho GTPase

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