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Target intelligence / Profile preview
Guanine Nucleotide Exchange Factor H1 (GEF-H1)
- Target
- GEF-H1
- Molecular classification
- Enzyme, Guanine nucleotide exchange factor
01
Overview
Guanine Nucleotide Exchange Factor H1 (GEF-H1) is a guanine nucleotide exchange factor that activates RhoA by promoting the exchange of GDP for GTP. This activation triggers downstream signaling pathways, such as the RhoA/ROCK pathway, which are crucial for regulating cytoskeletal dynamics, cell motility, polarization, and epithelial barrier function. The activity of GEF-H1 is regulated by its association with microtubules. Overexpression or hyperactivation of GEF-H1 has been observed in several human cancers.
- Other names
- ARHGEF2Rho guanine nucleotide exchange factor 2Dbl family member
02
Mechanism of action
Inhibition of RhoA activation
03
Biological functions
Signal transductionCytoskeletal regulationCell motilityCell polarizationEpithelial barrier functionRhoA activation
04
Disease associations
CancerMetastasis
05
Safety considerations
Potential for off-target effects due to broad role in cytoskeletal regulationMicrotubule disruption
06
Biomarkers
GEF-H1 expression level in tumor tissue
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