PMID: 11907155Mar 22, 2002Paper

Elucidation of vasoactive intestinal peptide pharmacophore for VPAC(1) receptors in human, rat, and guinea pig

The Journal of Pharmacology and Experimental Therapeutics
Hisato IgarashiRobert T Jensen

Abstract

Vasoactive intestinal peptide (VIP) is a neurotransmitter involved in a number of pathological and physiological processes. VIP is rapidly degraded and simplified stable analogs are needed. VIP's action was extensively studied in rat and guinea pig. However, it is largely unknown whether its pharmacophore in these species resembles human. To address this issue we investigated the VIP pharmacophore for VPAC(1) (the predominant receptor subtype in cancers and widely distributed in normal tissues) by using alanine and D-amino acid scanning. Interaction with rat, guinea pig, and human VPAC(1) was assessed using transfected Chinese hamster ovary (CHO) and PANC1 cells and cells possessing native VPAC(1). Important species differences existed in the VIP pharmacophore. The human VPAC(1) expressed in CHO cells, which were used almost exclusively in previous studies, differed markedly from the native VPAC(1) in T47D cells. The most important amino acids for determining affinity are His(1), Asp(3), Phe(6), Arg(12), Arg(14), and Leu(23). Ser(2), Asp(8), Asn(9), Thr(11), Val(19), Asn(24), Ser(25), Leu(27), and Asn(28) are not essential for high-affinity interaction/activation. [Ala(2,8,9,11,19,24,25,27,28)]VIP, which contained 11 alanines, ...Continue Reading

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Citations

Jan 4, 2008·Naunyn-Schmiedeberg's Archives of Pharmacology·Satomi OnoueShizuo Yamada
Feb 4, 2005·Current Opinion in Gastroenterology·Yan Bi, John A Williams
Dec 16, 2010·Current Opinion in Endocrinology, Diabetes, and Obesity·Terry W MoodyRobert T Jensen
Apr 5, 2011·Expert Opinion on Drug Metabolism & Toxicology·Marlène PernotMuriel Barberi-Heyob
Nov 15, 2011·Journal of Immunological Methods·Rebecca J HermannGlenn P Dorsam
Nov 26, 2015·Frontiers in Pharmacology·Kelly J CulhaneElsa C Y Yan
Sep 12, 2006·Regulatory Peptides·David DangoorIllana Gozes
Oct 10, 2007·Journal of Peptide Science : an Official Publication of the European Peptide Society·David DangoorRaniero Rocchi
Aug 16, 2003·Endocrine Reviews·Jean Claude Reubi
May 6, 2011·British Journal of Pharmacology·Laurence J MillerKaleeckal G Harikumar
Jun 1, 2004·Pharmacological Reviews·Mario DelgadoDoina Ganea
Jun 3, 2018·Hormones : International Journal of Endocrinology and Metabolism·Vlasios KarageorgosGeorge Liapakis
Mar 29, 2011·Biochimica Et Biophysica Acta·Yoshitaka UmetsuHidekazu Hiroaki

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