Document Detail

Binding of endomorphin-2 to mu-opioid receptors in experimental mouse mammary adenocarcinoma.
MedLine Citation:
PMID:  15813894     Owner:  NLM     Status:  MEDLINE    
Endomorphin-2 (Tyr-Pro-Phe-Phe-NH2) binds with high affinity and selectivity to the mu-opioid receptor. In the present study, [125I]endomorphin-2 has been used to characterize mu-opioid-binding sites on transplantable mouse mammary adenocarcinoma cells. Cold saturation experiments performed with [125I]endomorphin-2 (1 nM) show biphasic binding curves in Scatchard coordinates. One component represents high affinity and low capacity (K(d) = 18.79 +/- 1.13 nM, B(max) = 635 +/- 24 fmol/mg protein) and the other shows low affinity and higher capacity (K(d) = 7.67 +/- 0.81 microM, B(max) = 157 +/- 13 pmol/mg protein) binding sites. The rank order of agonists competing for the [125I]endomorphin-2 binding site was [d-1-Nal3]morphiceptin > endomorphin-2 >> [d-Phe3]morphiceptin > morphiceptin > [d-1-Nal3]endomorphin-2, indicating binding of these peptides to mu-opioid receptors. The uptake of 131I-labeled peptides administered intraperitoneally to tumor-bearing mice was also investigated. The highest accumulation in the tumor was observed for [d-1-Nal3)morphiceptin, which reached the value of 8.19 +/- 1.14% dose/g tissue.
J Fichna; J-C do-Rego; M Mirowski; J Costentin; A Janecka
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  The journal of peptide research : official journal of the American Peptide Society     Volume:  65     ISSN:  1397-002X     ISO Abbreviation:  J. Pept. Res.     Publication Date:  2005 Apr 
Date Detail:
Created Date:  2005-04-07     Completed Date:  2005-08-02     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  9707067     Medline TA:  J Pept Res     Country:  Denmark    
Other Details:
Languages:  eng     Pagination:  459-64     Citation Subset:  IM    
Department of Medicinal Chemistry, Medical University, Lodz, Poland.
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MeSH Terms
Adenocarcinoma / metabolism*
Binding, Competitive
Cell Membrane / metabolism
Iodine Radioisotopes / metabolism
Mammary Neoplasms, Experimental / metabolism*
Mice, Inbred C3H
Oligopeptides / metabolism*
Receptors, Opioid, mu / metabolism*
Reg. No./Substance:
0/Iodine Radioisotopes; 0/Oligopeptides; 0/Receptors, Opioid, mu; 0/endomorphin 2

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