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Proenkephalin A gene products activate a new family of sensory neuron--specific GPCRs.

Authors: Lembo, PM  Grazzini, E  Groblewski, T  O'Donnell, D  Roy, MO  Zhang, J  Hoffert, C  Cao, J  Schmidt, R  Pelletier, M  Labarre, M  Gosselin, M  Fortin, Y  Banville, D  Shen, SH  Strom, P  Payza, K  Dray, A  Walker, P  Ahmad, S 
Citation: Lembo PM, etal., Nat Neurosci 2002 Mar;5(3):201-9.
Pubmed: (View Article at PubMed) PMID:11850634
DOI: Full-text: DOI:10.1038/nn815

Several peptide fragments are produced by proteolytic cleavage of the opioid peptide precursor proenkephalin A, and among these are a number of enkephalin fragments, in particular bovine adrenal medulla peptide 22 (BAM22). These peptide products have been implicated in diverse biological functions, including analgesia. We have cloned a newly identified family of 'orphan' G protein--coupled receptors (GPCRs) and demonstrate that BAM22 and a number of its fragments bind to and activate these receptors with nanomolar affinities. This family of GPCRs is uniquely localized in the human and rat small sensory neuron, and we called this family the sensory neuron--specific G protein--coupled receptors (SNSRs). Receptors of the SNSR family are distinct from the traditional opioid receptors in their insensitivity to the classical opioid antagonist naloxone and poor activation by opioid ligands. The unique localization of SNSRs and their activation by proenkephalin A peptide fragments indicate a possible function for SNSRs in sensory neuron regulation and in the modulation of nociception.


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RGD Object Information
RGD ID: 625545
Created: 2002-09-30
Species: All species
Last Modified: 2002-09-30
Status: ACTIVE


RGD is funded by grant HL64541 from the National Heart, Lung, and Blood Institute on behalf of the NIH.