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Target intelligence / Profile preview
Guanine nucleotide exchange factor VAV3 (VAV3)
- Target
- VAV3
- Molecular classification
- Enzyme, Guanine nucleotide exchange factor (GEF)
01
Overview
Guanine nucleotide exchange factor VAV3 is a member of the VAV family of GEFs, which activate Rho/Rac family GTPases to regulate actin cytoskeletal rearrangements, signal transduction, and transcriptional changes[2][4][7][8]. VAV3 is widely expressed and participates in immune and hematopoietic cell signaling, cell division, migration, and proliferation. It is regulated by tyrosine phosphorylation, crucial for its activity[1][3]. VAV3 is implicated in cancer progression and is being evaluated as a potential therapeutic target, notably via its structurally unique C1 domain[5]. Expression levels of VAV3 can serve as biomarkers in oncology. Therapeutic targeting requires careful consideration due to the broad importance of VAV3 in normal cellular functions.
- Other names
- VAV3VAV-3vav 3 guanine nucleotide exchange factorvav 3 oncogeneguanine nucleotide exchange factor VAV3
02
Mechanism of action
Drugs targeting VAV3 (under investigation) act by inhibiting or modifying its nucleotide exchange activity, often through interaction with regulatory domains (such as the C1 domain)
03
Biological functions
Signal transduction (by activating Rho/Rac family GTPases)Actin cytoskeletal rearrangementTranscriptional regulationCell cycle regulation, particularly cytokinesisImmune cell signaling and synapse formationCell proliferation and migration
04
Disease associations
Cancer (prostate cancer, glioblastoma, breast cancer, colon cancer, oral squamous cell carcinoma)OsteopetrosisInflammation (via immune cell signaling)Neurodevelopment (implicated in axon guidance and cerebellar function)
05
Safety considerations
Potential challenges include off-target immunosuppression or unwanted effects on actin dynamics and cell division, due to VAV3's role in normal cell signaling and cytoskeletal regulation
06
Interacting drugs
No FDA-approved drugs directly target VAV3; however, it is under investigation as a potential therapeutic target, particularly via its atypical C1 domain
07
Biomarkers
VAV3 expression level (used in cancer diagnosis/prognosis, e.g., glioblastoma, prostate cancer)
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