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Target intelligence / Profile preview
Ras homolog family member A Y42C mutant (RhoA Y42C)
- Target
- RhoA Y42C
- Molecular classification
- Small GTPase, Rho family GTPase, Oncoprotein
01
Overview
RhoA Y42C is a gain-of-function mutant of the RhoA small GTPase, characterized by impaired GTP hydrolysis and enhanced interaction with effectors like ROCK. This leads to increased actin stress fiber formation, cell motility, and activation of signaling pathways such as FAK/YAP/TAZ and PI3K/AKT, contributing to oncogenesis, particularly in diffuse gastric cancer. It is considered a therapeutic target due to its role in cancer progression.
- Other names
- RhoA Y42C mutantRHOA(Y42C)RhoA tyrosine 42 cysteine mutant
02
Mechanism of action
Inhibition of downstream effectors of RhoA Y42C, such as ROCK.
03
Biological functions
Actin cytoskeleton organizationCell motilityCell adhesionCell proliferationCell survivalSignal transduction
04
Disease associations
CancerDiffuse gastric cancer
05
Safety considerations
Potential for off-target effects of inhibitorsResistance to targeted therapiesCompensation by other signaling pathways
06
Interacting drugs
ROCK inhibitors
07
Biomarkers
RhoA Y42C mutation status for patient selection in clinical trialsFAK activation levels
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