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Target intelligence / Profile preview
Vasoactive Intestinal Peptide Receptor 1 (VPAC1)
- Target
- VPAC1
- Molecular classification
- G protein-coupled receptor, GPCR, Receptor, Class B GPCR
01
Overview
VPAC1 is a G protein-coupled receptor that binds vasoactive intestinal peptide (VIP) and pituitary adenylate cyclase activating polypeptide (PACAP). It is widely expressed and mediates a variety of physiological effects, including regulation of exocrine secretions, hormone release, fetal development, and immune response. VPAC1 signals primarily through activation of adenylyl cyclase, leading to increased cAMP levels. It is a potential therapeutic target for various diseases, including cancer, inflammatory disorders, and infections. Selective agonists and antagonists are being developed to probe function and therapeutic potential.
- Other names
- VIPR1Vasoactive intestinal peptide receptor type 1
02
Mechanism of action
Agonists activate VPAC1, stimulating adenylyl cyclase and increasing intracellular cAMP levels. Antagonists block VIP/PACAP binding and downstream signaling.
03
Biological functions
Signal transductionRegulation of exocrine secretionsHormone release modulationFetal developmentImmune response regulationcAMP increase via adenylyl cyclase
04
Disease associations
CancerInflammationInfectionOther
05
Safety considerations
Potential for off-target effects due to structural similarity with other GPCRs.Complex role in immune modulation may lead to unintended consequences.Lack of well-defined small molecule antagonists complicates therapeutic development.
06
Interacting drugs
Ala^11,22,28VIP
2 more in the full profile.
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