| Binding of endomorphin-2 to mu-opioid receptors in experimental mouse mammary adenocarcinoma. | |
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MedLine Citation:
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PMID: 15813894 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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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. |
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Authors:
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J Fichna; J-C do-Rego; M Mirowski; J Costentin; A Janecka |
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Publication Detail:
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Type: Journal Article; Research Support, Non-U.S. Gov't |
Journal Detail:
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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:
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Created Date: 2005-04-07 Completed Date: 2005-08-02 Revised Date: 2006-11-15 |
Medline Journal Info:
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Nlm Unique ID: 9707067 Medline TA: J Pept Res Country: Denmark |
Other Details:
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Languages: eng Pagination: 459-64 Citation Subset: IM |
Affiliation:
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Department of Medicinal Chemistry, Medical University, Lodz, Poland. |
Export Citation:
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| MeSH Terms | |
Descriptor/Qualifier:
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Adenocarcinoma
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metabolism* Animals Binding, Competitive Cell Membrane / metabolism Female Iodine Radioisotopes / metabolism Mammary Neoplasms, Experimental / metabolism* Mice Mice, Inbred C3H Oligopeptides / metabolism* Receptors, Opioid, mu / metabolism* |
| Chemical | |
Reg. No./Substance:
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0/Iodine Radioisotopes; 0/Oligopeptides; 0/Receptors, Opioid, mu; 0/endomorphin 2 |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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