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Titolo:
CHIMERIC MELANOCORTIN MC1 AND MC3 RECEPTORS - IDENTIFICATION OF DOMAINS PARTICIPATING IN BINDING OF MELANOCYTE-STIMULATING HORMONE PEPTIDES
Autore:
SCHIOTH HB; YOOK P; MUCENIECE R; WIKBERG JES; SZARDENINGS M;
Indirizzi:
UNIV UPPSALA,DEPT PHARMACEUT PHARMACOL,BIOMED CTR,BOX 591 S-75124 UPPSALA SWEDEN UNIV UPPSALA,DEPT PHARMACEUT PHARMACOL,BIOMED CTR S-75124 UPPSALA SWEDEN INST ORGAN SYNTH,PHARMACOL LAB RIGA LATVIA
Titolo Testata:
Molecular pharmacology
fascicolo: 1, volume: 54, anno: 1998,
pagine: 154 - 161
SICI:
0026-895X(1998)54:1<154:CMMAMR>2.0.ZU;2-0
Fonte:
ISI
Lingua:
ENG
Soggetto:
POLYMERASE CHAIN-REACTION; MOLECULAR-CLONING; ALPHA-MELANOTROPIN; LIGAND-BINDING; BETA-2-ADRENERGIC RECEPTORS; RADIOLIGAND BINDING; BIOLOGICAL-ACTIVITY; ACTH RECEPTOR; EXPRESSION; ANTAGONIST;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Science Citation Index Expanded
Citazioni:
46
Recensione:
Indirizzi per estratti:
Citazione:
H.B. Schioth et al., "CHIMERIC MELANOCORTIN MC1 AND MC3 RECEPTORS - IDENTIFICATION OF DOMAINS PARTICIPATING IN BINDING OF MELANOCYTE-STIMULATING HORMONE PEPTIDES", Molecular pharmacology, 54(1), 1998, pp. 154-161

Abstract

The melanocortin receptors MC1 and MC3 are G protein-coupled receptors that have substantial structural similarities and bind melanocyte peptides but with different affinity profiles. We constructed a series of chimeric MC1/MC3 receptors to identify the epitopes that determine their selectivities for natural melanocyte peptides and synthetic analogues. The chimeric constructs were made by a polymerase chain reactionthat used identical regions in or just outside transmembranes (TM) 1,4, and 6 and divided the receptors into four segments. Saturation andcompetition studies on the expressed chimeric proteins indicate that TM1, TM2, TM3, and TM7 are involved in the subtype-specific binding ofmelanocyte peptides to these receptors. The results support the hypothesis that TM4 and TM5 may not contribute to the ligand-binding specificity of the MC receptors. This is the first report to describe the subtype-specific hormone-binding domains of the melanocortin receptor family.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 10/07/20 alle ore 15:13:45