Studies on mu and delta opioid receptor selectivity utilizing chimeric and site-mutagenized receptors.

Studies on mu and delta opioid receptor selectivity utilizing chimeric and site-mutagenized receptors. Research Abstract Details 

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Studies on mu and delta opioid receptor selectivity utilizing chimeric and site-mutagenized receptors. Abstract Text:

Opioid receptors are members of the guanine nucleotide binding protein (G protein)-coupled receptor family. Three types of opioid receptors have been cloned and characterized and are referred to as the delta, kappa and mu types. Analysis of receptor chimeras and site-directed mutant receptors has provided a great deal of information about functionally important amino acid side chains that constitute the ligand-binding domains and G-protein-coupling domains of G-protein-coupled receptors. We have constructed delta/mu opioid receptor chimeras that were express in human embryonic kidney 293 cells in order to define receptor domains that are responsible for receptor type selectivity. All chimeric receptors and wild-type delta and mu opioid receptors displayed high-affinity binding of etorphine (an agonist), naloxone (an antagonist), and bremazocine (a mixed agonist/antagonist). In contrast, chimeras that lacked the putative first extracellular loop of the mu receptor did not bind the mu-selective peptide [D-Ala2,MePhe4,Gly5-ol]enkephalin (DAMGO). Chimeras that lacked the putative third extracellular loop of the delta receptor did not bind the delta-selective peptide, [D-Ser2,D-Leu5]enkephalin-Thr (DSLET). Point mutations in the putative third extracellular loop of the wild-type delta receptor that converted vicinal arginine residues to glutamine abolished DSLET binding while not affecting bremazocine, etorphine, and naltrindole binding. We conclude that amino acids in the putative first extracellular loop of the mu receptor are critical for high-affinity DAMGO binding and that arginine residues in the putative third extracellular loop of the delta receptor are important for high-affinity DSLET binding.

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Studies on mu and delta opioid receptor selectivity utilizing chimeric and site-mutagenized receptors. Journal Published:

PUBLICATION TYPE: Research Support, U.S. Gov't,

Journal: Proceedings of the National Academy of Sciences of

VOLUME: 92

Page Numbers: 12436-40

Journal Abbreviation: Proc. Natl. Acad. Sci. U.S.A.

ISSN: 0027-8424

DAY: 19

MONTH: Dec

YEAR: 1995

Studies on mu and delta opioid receptor selectivity utilizing chimeric and site-mutagenized receptors. Information

Number of References:

LANGUAGE: eng

NlmUniqueID: 7505876

Studies on mu and delta opioid receptor selectivity utilizing chimeric and site-mutagenized receptors. Keywords Mesh Terms:

KEYWORDS: Transfection

MESH TERMS: metabolism

Chemical & Substance for Abstract: Studies on mu and delta opioid receptor selectivity utilizing chimeric and site-mutagenized receptors. Information

Substance Name: GTP-Binding Proteins

Registry Number: EC 3.6.1.-

Grant and Affiliation Information for Studies on mu and delta opioid receptor selectivity utilizing chimeric and site-mutagenized receptors.

AFFILIATION: Department of Biochemistry and Molecular Biology, New Jersey Medical School, Newark 07103, USA.

Country: UNITED STATES

AGENCY: United States NCRR

GRANT: 2 S07 RR05393

ACRONYM: RR

MEDLINETA: Proc Natl Acad Sci U S A

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