Target intelligence / Profile preview

Ras protein-specific guanine nucleotide-releasing factor 1 (RASGRF1)

Target
RASGRF1
Molecular classification
Guanine nucleotide exchange factor (GEF), Signaling protein, Enzyme, Other: Imprinted gene
01

Overview

Ras protein-specific guanine nucleotide-releasing factor 1 (RASGRF1) is a guanine nucleotide exchange factor (GEF) that activates the small GTPase Ras by promoting the exchange of GDP for GTP, thereby triggering downstream signaling pathways, particularly the Ras/MAPK cascade[1][2][3]. It is structurally complex, containing multiple regulatory domains including CDC25 (catalyzing GEF activity towards Ras GTPases), REM (stabilization), PH (lipid interaction), IQ (calmodulin and calcium binding), and DH (mediating GEF activity toward Rac GTPases, another family of small GTPases)[2][3]. Predominantly expressed in the brain and involved in synaptic plasticity, learning, and memory, RASGRF1 also functions in pancreatic β-cell proliferation and glucose metabolism. Dysregulation contributes to cognitive deficits, certain metabolic syndromes, and may play a role in oncogenic signaling[1][2][3][4]. RASGRF1 is a paternally imprinted gene and should not be confused with the Cdc25 phosphatases despite historical nomenclature overlap[1].

Other names
Ras-GRF1GRF1CDC25 (not to be confused with Cdc25 phosphatases)Ras guanine nucleotide-releasing factor 1
02

Mechanism of action

Drugs targeting this molecule (if developed) would aim to inhibit its GEF activity to reduce Ras pathway activation, modulate synaptic plasticity, or affect neurodevelopment and metabolism; see description for related pathway modulation[1][2][3].

03

Biological functions

Signal transductionCell proliferationSynaptic plasticityLearning and memoryRegulation of glucose metabolismNeuronal differentiation and morphology
04

Disease associations

CancerNeurodevelopmental disordersDiabetes/metabolic diseasesDrug-induced dyskinesia (e.g., L-DOPA-induced dyskinesia)
05

Safety considerations

Potential for adverse effects on cognition, memory, and glucose metabolism due to roles in neuronal plasticity and pancreatic β-cell proliferation[1][3].
06

Interacting drugs

None established as direct, clinically approved drugs for RASGRF1, but the pathway is a target for inhibitors of downstream Ras signaling (e.g., MEK inhibitors); experimental modulation via inhibitors or activators of Ras signaling may indirectly impact RASGRF1-related pathways[1][2][3].
07

Biomarkers

Not specifically used as a clinical biomarker, but altered expression or mutations in RASGRF1 can be studied as research biomarkers in cancers, neurodevelopmental, and metabolic diseases[1][3].

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