Target intelligence / Profile preview

Ras-GEF domain-containing family member 1A (RASGEF1A)

Target
RASGEF1A
Molecular classification
Enzyme, Guanine nucleotide exchange factor (GEF), Ras family GEF protein
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Overview

Ras-GEF domain-containing family member 1A (RASGEF1A) is a protein encoded by the RASGEF1A gene in humans. It functions as a guanine nucleotide exchange factor (GEF) and is specific for Ras family GTPases such as RAP2A, KRAS, HRAS, and NRAS (at least in vitro). The protein facilitates Ras activation by promoting the exchange of GDP for GTP, regulating key cellular processes including cell migration and Ras-dependent signal transduction. It is predominantly found in the cytosol and may also be active at the plasma membrane. Dysregulation or mutations affecting Ras signaling are implicated in cancer and other diseases, making GEF proteins important for research into cancer mechanisms. However, RASGEF1A is not yet an established drug target, and further work will be needed to evaluate its utility for therapeutic intervention.

Other names
RasGEF domain family member 1ARASGEF1ACG4853FLJ37817CG4853 gene productRGF1A
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Mechanism of action

For theoretical or research-stage inhibitors: Inhibition of guanine nucleotide exchange factor activity, leading to decreased Ras activation and downstream signaling. For drugs targeting Ras family proteins indirectly: Blocking Ras-mediated MAPK pathway signaling.

03

Biological functions

Signal transduction (via Ras protein activation)Cell migration (positive regulation)Positive regulation of Ras protein signal transduction
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Disease associations

Cancer (associated specifically with hematologic cancer and cholangiocarcinoma)Other (implicated in MAPK family signaling cascades and breast cancer pathway)
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Safety considerations

The Ras signaling pathway is central to multiple cellular functions; targeting its upstream GEFs carries a theoretical risk of affecting normal cell migration and proliferation.Safety risks relate to off-target effects and the difficulty in achieving specific inhibition without impacting normal Ras signaling.
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Biomarkers

There is no clinical biomarker status for RASGEF1A known at present. Expression/activity is studied as a marker in cancer progression research.

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