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Rho family of GTPases (Rho GTPases)
- Target
- Rho GTPases
- Molecular classification
- Small GTPase, G protein, Signaling protein
01
Overview
The Rho family GTPases are a group of small signaling G proteins that act as molecular switches cycling between inactive GDP-bound and active GTP-bound states. They regulate actin cytoskeleton dynamics, cell shape, movement, and signaling pathways, and are implicated in various diseases including cancer, neurodegenerative diseases, and cardiovascular disorders. Targeting Rho GTPases is challenging due to high sequence homology and complex signaling networks.
- Other names
- Rho proteinsRas homolog gene family, member ARas-related C3 botulinum toxin substrate 1Cell division cycle 42Rac family small GTPase 1Cdc42Rac1RhoA
02
Mechanism of action
Inhibition of GTPase activity, inhibition of downstream effectors
03
Biological functions
Actin cytoskeleton regulationCell signalingCell morphologyCell migrationCell cycle progressionGene expression regulationOrganelle developmentSignal transduction
04
Disease associations
CancerNeurodegenerative diseaseCardiovascular diseaseInflammationInfectionDevelopmental disorders
05
Safety considerations
Off-target effects due to high sequence homology within the familyDevelopment of resistancePotential for paradoxical effects due to complex signaling networksLimited bioavailability of some inhibitorsSpecificity challenges in targeting individual Rho GTPases
06
Interacting drugs
NSC23766 (Rac1 inhibitor)
3 more in the full profile.
07
Biomarkers
Rho GTPase activity levelsExpression levels of Rho GTPasesActivation state of downstream targets
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