Jove
Visualize
Contact Us
JoVE
x logofacebook logolinkedin logoyoutube logo
ABOUT JoVE
OverviewLeadershipBlogJoVE Help Center
AUTHORS
Publishing ProcessEditorial BoardScope & PoliciesPeer ReviewFAQSubmit
LIBRARIANS
TestimonialsSubscriptionsAccessResourcesLibrary Advisory BoardFAQ
RESEARCH
JoVE JournalMethods CollectionsJoVE Encyclopedia of ExperimentsArchive
EDUCATION
JoVE CoreJoVE BusinessJoVE Science EducationJoVE Lab ManualFaculty Resource CenterFaculty Site
Terms & Conditions of Use
Privacy Policy
Policies

Related Experiment Videos

Domains determining agonist selectivity in chimaeric VIP2 (VPAC2)/PACAP (PAC1) receptors.

E M Lutz1, C J MacKenzie, M Johnson

  • 1MRC Brain Metabolism Unit, 1 George Square, Edinburgh EH8 9JZ, UK. elutz@srv1.bmu.mrc.ac.uk

British Journal of Pharmacology
|November 11, 1999
PubMed
Summary

Researchers identified specific receptor domains that control how potent vasoactive intestinal peptide (VIP) and pituitary adenylyl cyclase-activating polypeptide (PACAP) are at VPAC2 and PAC1 receptors. The amino-terminal extracellular domain is key for this selectivity.

Related Concept Videos

You might also read

Related Articles

Articles linked to this work by shared authors, journal, and citation graph.

Sort by
Same author

Pushing Photons with Electrons: Observation of the Polariton Drag Effect.

Physical review letters·2025
Same author

Time, momentum, and energy resolved pump-probe tunneling spectroscopy of two-dimensional electron systems.

Nature communications·2023
Same author

Impact of the COVID-19 pandemic on a post-mortem CT service for adult non-suspicious death.

Clinical radiology·2023
Same author

Extensive mucocutaneous, oesophageal and otic lichen planus secondary to nivolumab therapy.

Skin health and disease·2022
Same author

Collective Excitations of Exciton-Polariton Condensates in a Synthetic Gauge Field.

Physical review letters·2021
Same author

Enhancement of Parametric Effects in Polariton Waveguides Induced by Dipolar Interactions.

Physical review letters·2021

Area of Science:

  • Molecular Biology
  • Receptor Pharmacology
  • G Protein-Coupled Receptors

Background:

  • VPAC2 and PAC1 receptors are Group II G protein-coupled receptors.
  • These receptors exhibit differential potency for VIP and PACAP-38.
  • Understanding receptor-ligand interactions is crucial for drug development.

Purpose of the Study:

  • To investigate the specific domains responsible for VPAC2 and PAC1 receptor selectivity.
  • To determine how different receptor segments influence agonist potency.

Main Methods:

  • Construction of four chimaeric receptors by exchanging segments between VPAC2 and PAC1 receptors.
  • Expression of chimaeric receptors in COS 7 cells.
  • Assay of cyclic AMP production in response to various agonists.

Related Experiment Videos

Main Results:

  • The amino-terminal extracellular domain of both VPAC2 and PAC1 receptors primarily determined agonist selectivity.
  • Exchanging other receptor domains had minimal impact on PACAP-38 and PACAP-27 potency.
  • Substitution of VPAC2 receptor portions in PAC1 chimeras altered VIP and helodermin potency.

Conclusions:

  • The amino-terminal extracellular domain is a major determinant of VPAC2 and PAC1 receptor selectivity.
  • Additional receptor domains may differentially influence VIP/helodermin interactions with the PAC1 receptor.
  • These findings provide insights into the structural basis of VIP/PACAP receptor signaling.