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Titolo:
Melanocortins and the brain: from effects via receptors to drug targets
Autore:
Adan, RAH; Gispen, WH;
Indirizzi:
Univ Utrecht, Med Ctr, Rudolf Magnus Inst Neurosci, Dept Med Pharmacol, NL-3584 CG Utrecht, Netherlands Univ Utrecht Utrecht Netherlands NL-3584 CG3584 CG Utrecht, Netherlands
Titolo Testata:
EUROPEAN JOURNAL OF PHARMACOLOGY
fascicolo: 1-3, volume: 405, anno: 2000,
pagine: 13 - 24
SICI:
0014-2999(20000929)405:1-3<13:MATBFE>2.0.ZU;2-K
Fonte:
ISI
Lingua:
ENG
Soggetto:
MELANOCYTE-STIMULATING-HORMONE; MORPHINE-INDUCED ANALGESIA; ACTH(4-9) ANALOG ORG-2766; BETA-LIPOTROPIN PRECURSOR; MOLECULAR-CLONING; ALPHA-MSH; GROOMING BEHAVIOR; RAT-BRAIN; MELANOTROPIN ANALOGS; BIOLOGICAL-ACTIVITY;
Keywords:
ACTH (adrenocorticotropic hormone); MSH (melanocyte-stimulating hormone); melanocortin receptor; brain melanocortin system; peptide-receptor interaction; avoidance; grooming; food intake; pain;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
88
Recensione:
Indirizzi per estratti:
Indirizzo: Adan, RAH Univ Utrecht, Med Ctr, Rudolf Magnus Inst Neurosci, Dept Med Pharmacol, Univ Weg 100, NL-3584 CG Utrecht, Netherlands Univ Utrecht Univ Weg100 Utrecht Netherlands NL-3584 CG rlands
Citazione:
R.A.H. Adan e W.H. Gispen, "Melanocortins and the brain: from effects via receptors to drug targets", EUR J PHARM, 405(1-3), 2000, pp. 13-24

Abstract

The lack of specific receptors (and antagonists) has hampered the researchon the neural mechanism of action of adrenocorticotropic hormone (ACTH)- and melanocyte-stimulating hormone (MSH)-like peptides. Yet the original observations in the 1970s already pointed to cAMP as a possible mediator of ACTH/MSH effects in neurons. The cloning of melanocortin receptors since 1992, the identification of at least two subtypes (melanocortin MC3 and MC4 receptors) that are present in neural tissue and the development of selective and potent agonists as well as antagonists have markedly furthered the position of melanocortins as important neuropeptides. In this paper we discuss the role of especially the receptor subtype melanocortin MC4 in various behaviors including grooming behavior and feeding behavior and consider new insights in the interaction between the opioid and the melanocortin system atthe level of the spinal cord (i.e. pain perception). Finally, based on newdata obtained in molecular pharmacological studies on brain melanocortin receptors, we suggest a general concept for selective receptor-ligand interaction: ligand residues outside the peptide core-sequence may direct the conformation of the residues in the ligand core-sequence that interact directly with the receptor-binding pocket and thereby determine selectivity. (C) 2000 Elsevier Science B.V. All rights reserved.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 05/04/20 alle ore 04:00:15