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Opioid Receptors: Overview

Opioid receptors, including the mu (μ, MOR), delta (δ, DOR), and kappa (κ, KOR) types, belong to the rhodopsin family of G protein-coupled receptors. These receptors are located throughout the central and peripheral nervous systems and in non-neuronal tissues such as macrophages and astrocytes. Opioid receptor ligands can be categorized into agonists or antagonists. Highly selective agonists include [d-Ala2, MePhe4, Gly(ol)5]-enkephalin or DAMGO for MOR, [D-Pen2, D-Pen5]-enkephalin or DPDPE for...
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G-Protein Gated Ion Channels01:21

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Characterization of G Protein-coupled Receptors by a Fluorescence-based Calcium Mobilization Assay
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Structural and functional differences between pheromonotropic and melanotropic PK/PBAN receptors.

Aliza Hariton-Shalev1, Moran Shalev, Noam Adir

  • 1Department of Entomology, The Volcani Center, Bet Dagan 50250, Israel.

Biochimica Et Biophysica Acta
|July 16, 2013
PubMed
Summary

Pyrokinin/pheromone biosynthesis-activating neuropeptide (PK/PBAN) receptors in insects show distinct structural and functional differences. These variations suggest specific receptors mediate different PK/PBAN functions, aiding in developing targeted insect control agents.

Keywords:
CAPA-DHDHDiapause hormoneECLG-protein-coupled receptorGPCRHeliothis peltigeraICLInsect neuropeptideNpPIPK/PBANPK/PBAN receptorPK/PBAN-RPheromone biosynthesis-activating neuropeptide-receptorSGNPsSpodoptera littoraliscapa-gene-derived peptidediapause hormoneextra-cellular loopintra-cellular loopneuropeptidepre-immune serumpyrokinin/pheromone biosynthesis-activating neuropeptideβ- and γ-subesophageal Nps

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Area of Science:

  • * Entomology
  • * Molecular Biology
  • * Biochemistry

Background:

  • * Pyrokinin/pheromone biosynthesis-activating neuropeptide (PK/PBAN) is crucial for insect physiology.
  • * The diverse roles of PK/PBAN raise questions about receptor mechanisms.

Purpose of the Study:

  • * To investigate the structural and functional properties of PK/PBAN receptors.
  • * To understand how different PK/PBAN peptides interact with their receptors.

Main Methods:

  • * Cloning and stable expression of PK/PBAN receptors from Heliothis peltigera and Spodoptera littoralis.
  • * Structural modeling, electrostatic potential analysis, and cellular functional assays (calcium mobilization).

Main Results:

  • * Homology modeling revealed conserved residues typical of class A G-protein coupled receptors.
  • * Structural and electrostatic differences were identified between the two receptors.
  • * Both receptors mediated PK/PBAN signal transduction via calcium influx.
  • * Differential responses to PBAN and diapause hormone (DH) were observed, with Spl-PK/PBAN-R showing high DH sensitivity.

Conclusions:

  • * Distinct PK/PBAN receptors likely mediate specific in vivo functions.
  • * Different peptides may elicit responses through these specific receptors.
  • * Findings support the development of novel insect control agents targeting PK/PBAN receptors.