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The vasoactive intestinal peptide receptor 1 (VPAC(1) ) belongs to family B of GPCRs and is activated upon binding of vasoactive intestinal peptide (VIP) and pituitary AC-activating polypeptide neuropeptides. Widely distributed throughout body, VPAC(1) plays important regulatory roles in human physiology and physiopathology. Like most members of the GPCR-B family, VPAC(1) receptor is predicted to follow the actual paradigm of a common 'two-domain' model of natural ligand action. However the precise structural basis for ligand binding, receptor activation and signal transduction are still incompletely understood due in part to the absence of X-ray crystal structure of the whole receptor and to significant structural differences with the most extensively studied family of receptor, the GPCR-A/rhodopsin family. Here, we try to summarize the current knowledge of the molecular mechanisms involved in VPAC(1) receptor activation and signal transduction. This includes search for amino acids involved in the two-step process of VIP binding, in the stabilization of VPAC(1) inactive and active conformations, and in binding and activation of G proteins.

Titel:	Conformational switches in the VPAC(1) receptor.
Autor/in / Beteiligte Person:	Langer, I
Link:	Zum Volltext
Zeitschrift:	British journal of pharmacology, Jg. 166 (2012-05-01), Heft 1, S. 79-84
Veröffentlichung:	London : Wiley ; <i>Original Publication</i>: London, Macmillian Journals Ltd., 2012
Medientyp:	academicJournal
ISSN:	1476-5381 (electronic)
DOI:	10.1111/j.1476-5381.2011.01616.x
Schlagwort:	Amino Acid Sequence Animals Humans Ligands Neuropeptides metabolism Protein Binding Protein Conformation Receptors, Vasoactive Intestinal Polypeptide, Type I chemistry Signal Transduction Pituitary Adenylate Cyclase-Activating Polypeptide metabolism Receptors, Vasoactive Intestinal Polypeptide, Type I metabolism Vasoactive Intestinal Peptide metabolism
Sonstiges:	Nachgewiesen in: MEDLINE Sprachen: English Publication Type: Journal Article; Research Support, Non-U.S. Gov't; Review Language: English [Br J Pharmacol] 2012 May; Vol. 166 (1), pp. 79-84. MeSH Terms: Pituitary Adenylate Cyclase-Activating Polypeptide / metabolism ; Receptors, Vasoactive Intestinal Polypeptide, Type I / metabolism ; Vasoactive Intestinal Peptide / *metabolism ; Amino Acid Sequence ; Animals ; Humans ; Ligands ; Neuropeptides / metabolism ; Protein Binding ; Protein Conformation ; Receptors, Vasoactive Intestinal Polypeptide, Type I / chemistry ; Signal Transduction References: Mol Pharmacol. 2005 Jan;67(1):20-31. (PMID: 15615699) ; Nature. 2008 Jul 10;454(7201):183-7. (PMID: 18563085) ; Science. 2011 Apr 15;332(6027):322-7. (PMID: 21393508) ; Trends Biochem Sci. 2008 Jul;33(7):314-9. (PMID: 18555686) ; Proteins. 1999 Jun 1;35(4):375-86. (PMID: 10382665) ; Science. 2007 Nov 23;318(5854):1258-65. (PMID: 17962520) ; Cell Signal. 2006 Dec;18(12):2121-30. (PMID: 16650965) ; J Biol Chem. 1998 Feb 27;273(9):4990-6. (PMID: 9478946) ; Nature. 2008 Jul 24;454(7203):486-91. (PMID: 18594507) ; Br J Pharmacol. 2002 Aug;136(7):1042-8. (PMID: 12145104) ; Nature. 2009 May 21;459(7245):356-63. (PMID: 19458711) ; Biochemistry. 2006 Oct 31;45(43):12976-85. (PMID: 17059214) ; Nature. 2011 Jan 13;469(7329):236-40. (PMID: 21228876) ; Pharmacol Ther. 2009 Mar;121(3):294-316. (PMID: 19109992) ; Proc Natl Acad Sci U S A. 2007 Aug 28;104(35):13942-7. (PMID: 17715056) ; J Biol Chem. 2001 Jan 12;276(2):1084-8. (PMID: 11013258) ; Drug Discov Today. 2005 Mar 15;10(6):417-27. (PMID: 15808821) ; Mol Pharmacol. 2010 Sep;78(3):394-401. (PMID: 20573782) ; Nature. 2007 Nov 15;450(7168):383-7. (PMID: 17952055) ; Mol Pharmacol. 2006 Jan;69(1):363-73. (PMID: 16244179) ; Mol Endocrinol. 2008 Jan;22(1):147-55. (PMID: 17885205) ; Peptides. 2007 Sep;28(9):1631-9. (PMID: 17574305) ; Br J Pharmacol. 2006 Aug;148(8):1051-9. (PMID: 16783404) ; Structure. 2010 Sep 8;18(9):1083-93. (PMID: 20826335) ; Proc Natl Acad Sci U S A. 2007 May 8;104(19):7875-80. (PMID: 17470806) ; Science. 2008 Nov 21;322(5905):1211-7. (PMID: 18832607) ; Proc Natl Acad Sci U S A. 2008 Apr 1;105(13):5034-9. (PMID: 18375760) ; Mol Endocrinol. 2002 May;16(5):1089-96. (PMID: 11981043) ; Cell Signal. 2005 Jan;17(1):17-24. (PMID: 15451021) ; Proc Natl Acad Sci U S A. 2007 Mar 20;104(12):4858-63. (PMID: 17360332) ; Science. 2000 Aug 4;289(5480):739-45. (PMID: 10926528) ; Biochem Biophys Res Commun. 1999 Jan 8;254(1):15-20. (PMID: 9920725) ; J Mol Neurosci. 2001 Dec;17(3):325-30. (PMID: 11859928) ; J Biol Chem. 2003 Jan 31;278(5):3293-7. (PMID: 12446722) ; Mol Pharmacol. 2010 Jan;77(1):95-101. (PMID: 19854890) ; J Biol Chem. 2003 Jul 4;278(27):24759-66. (PMID: 12690118) ; J Biol Chem. 2008 Apr 25;283(17):11340-7. (PMID: 18287102) ; Neuropeptides. 2010 Apr;44(2):127-32. (PMID: 20031208) ; J Mol Neurosci. 2008 Nov;36(1-3):245-8. (PMID: 18597186) ; Nature. 2008 Sep 25;455(7212):497-502. (PMID: 18818650) ; J Biol Chem. 1999 Jul 2;274(27):19455-64. (PMID: 10383462) ; Mol Pharmacol. 1996 Oct;50(4):885-90. (PMID: 8863834) ; Neuropharmacology. 2003 Jan;44(1):125-31. (PMID: 12559130) Substance Nomenclature: 0 (Ligands) ; 0 (Neuropeptides) ; 0 (Pituitary Adenylate Cyclase-Activating Polypeptide) ; 0 (Receptors, Vasoactive Intestinal Polypeptide, Type I) ; 37221-79-7 (Vasoactive Intestinal Peptide) Entry Date(s): Date Created: 20110803 Date Completed: 20120806 Latest Revision: 20211020 Update Code: 20240513 PubMed Central ID: PMC3415639

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Conformational switches in the VPAC(1) receptor.