Interaction of lipophilic VIP derivatives with recombinant VIP1/PACAP and VIP2/PACAP receptors
Stearyl vasoactive intestinal polypeptide has been reported to be a VIP (vasoactive intestinal polypeptide) receptor agonist of high potency with an original bioavailability and action. We synthesized three fatty acyl derivatives, myristyl-, palmityl- and stearyl-[Nle17]VIP, and tested their capacit...
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| Veröffentlicht in: | European journal of pharmacology 1998-07, Vol.354 (1), p.105-111 |
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| container_title | European journal of pharmacology |
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| creator | GOURLET, P RATHE, J DE NEEF, P CNUDDE, J VANDERMEERS-PIRET, M.-C WAELBROECK, M ROBBERECHT, P |
| description | Stearyl vasoactive intestinal polypeptide has been reported to be a VIP (vasoactive intestinal polypeptide) receptor agonist of high potency with an original bioavailability and action. We synthesized three fatty acyl derivatives, myristyl-, palmityl- and stearyl-[Nle17]VIP, and tested their capacity to recognize recombinant rat- and human VIP1- and VIP2/PACAP (pituitary adenylate cyclase-activating polypeptide) receptors and to stimulate adenylate cyclase activity. The three lipophilic analogues bound with high affinity (from 0.5 to 20 nM) to both receptor subtypes but did not distinguish between them. In preparations expressing a high density of human VIP1/PACAP receptors, the three lipophilic analogues had the same efficacy as VIP and [Nle17]VIP. In preparations expressing the rat receptors, stearyl-[Nle17]VIP had a lower efficacy than the other peptides tested. In preparations expressing a low level of VIP1/PACAP receptors and in those expressing VIP2/PACAP receptors, all analogues behaved like partial agonists. The lowest efficacy was observed for stearyl-[Nle17]VIP on the VIP2/PACAP receptor subclass. Based on our results, a complex pattern of in vivo biological effects of the lipophilic VIP derivatives should be expected: these compounds might behave as full agonists, partial agonists, or antagonists of the VIP response, depending on the number and the subtype of receptor expressed. |
| doi_str_mv | 10.1016/S0014-2999(98)00435-X |
| format | Article |
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We synthesized three fatty acyl derivatives, myristyl-, palmityl- and stearyl-[Nle17]VIP, and tested their capacity to recognize recombinant rat- and human VIP1- and VIP2/PACAP (pituitary adenylate cyclase-activating polypeptide) receptors and to stimulate adenylate cyclase activity. The three lipophilic analogues bound with high affinity (from 0.5 to 20 nM) to both receptor subtypes but did not distinguish between them. In preparations expressing a high density of human VIP1/PACAP receptors, the three lipophilic analogues had the same efficacy as VIP and [Nle17]VIP. In preparations expressing the rat receptors, stearyl-[Nle17]VIP had a lower efficacy than the other peptides tested. In preparations expressing a low level of VIP1/PACAP receptors and in those expressing VIP2/PACAP receptors, all analogues behaved like partial agonists. The lowest efficacy was observed for stearyl-[Nle17]VIP on the VIP2/PACAP receptor subclass. Based on our results, a complex pattern of in vivo biological effects of the lipophilic VIP derivatives should be expected: these compounds might behave as full agonists, partial agonists, or antagonists of the VIP response, depending on the number and the subtype of receptor expressed.</description><identifier>ISSN: 0014-2999</identifier><identifier>EISSN: 1879-0712</identifier><identifier>DOI: 10.1016/S0014-2999(98)00435-X</identifier><identifier>PMID: 9726637</identifier><identifier>CODEN: EJPHAZ</identifier><language>eng</language><publisher>Amsterdam: Elsevier</publisher><subject>Adenylyl Cyclases - drug effects ; Adenylyl Cyclases - metabolism ; Animals ; Apud cells. Peptide and protein hormones. Growth factors ; Binding, Competitive ; Biological and medical sciences ; CHO Cells - metabolism ; CHO Cells - ultrastructure ; Cricetinae ; Enzyme Activation - drug effects ; Fundamental and applied biological sciences. Psychology ; Humans ; Kinetics ; Neuropeptides - drug effects ; Neuropeptides - metabolism ; Pituitary Adenylate Cyclase-Activating Polypeptide ; Rats ; Receptors, Pituitary Adenylate Cyclase-Activating Polypeptide ; Receptors, Pituitary Hormone - drug effects ; Receptors, Pituitary Hormone - metabolism ; Receptors, Vasoactive Intestinal Peptide - drug effects ; Receptors, Vasoactive Intestinal Peptide - metabolism ; Stimulation, Chemical ; Structure-Activity Relationship ; Vasoactive Intestinal Peptide - analogs & derivatives ; Vasoactive Intestinal Peptide - chemical synthesis ; Vasoactive Intestinal Peptide - pharmacology ; Vertebrates: endocrinology</subject><ispartof>European journal of pharmacology, 1998-07, Vol.354 (1), p.105-111</ispartof><rights>1998 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c385t-fe69acc6d64b842b7f736699617e5c4d1aab6a20e8b31f37b5bd9c2f6f1ba6863</citedby><cites>FETCH-LOGICAL-c385t-fe69acc6d64b842b7f736699617e5c4d1aab6a20e8b31f37b5bd9c2f6f1ba6863</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,780,784,27923,27924</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=2406223$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/9726637$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>GOURLET, P</creatorcontrib><creatorcontrib>RATHE, J</creatorcontrib><creatorcontrib>DE NEEF, P</creatorcontrib><creatorcontrib>CNUDDE, J</creatorcontrib><creatorcontrib>VANDERMEERS-PIRET, M.-C</creatorcontrib><creatorcontrib>WAELBROECK, M</creatorcontrib><creatorcontrib>ROBBERECHT, P</creatorcontrib><title>Interaction of lipophilic VIP derivatives with recombinant VIP1/PACAP and VIP2/PACAP receptors</title><title>European journal of pharmacology</title><addtitle>Eur J Pharmacol</addtitle><description>Stearyl vasoactive intestinal polypeptide has been reported to be a VIP (vasoactive intestinal polypeptide) receptor agonist of high potency with an original bioavailability and action. We synthesized three fatty acyl derivatives, myristyl-, palmityl- and stearyl-[Nle17]VIP, and tested their capacity to recognize recombinant rat- and human VIP1- and VIP2/PACAP (pituitary adenylate cyclase-activating polypeptide) receptors and to stimulate adenylate cyclase activity. The three lipophilic analogues bound with high affinity (from 0.5 to 20 nM) to both receptor subtypes but did not distinguish between them. In preparations expressing a high density of human VIP1/PACAP receptors, the three lipophilic analogues had the same efficacy as VIP and [Nle17]VIP. In preparations expressing the rat receptors, stearyl-[Nle17]VIP had a lower efficacy than the other peptides tested. In preparations expressing a low level of VIP1/PACAP receptors and in those expressing VIP2/PACAP receptors, all analogues behaved like partial agonists. The lowest efficacy was observed for stearyl-[Nle17]VIP on the VIP2/PACAP receptor subclass. Based on our results, a complex pattern of in vivo biological effects of the lipophilic VIP derivatives should be expected: these compounds might behave as full agonists, partial agonists, or antagonists of the VIP response, depending on the number and the subtype of receptor expressed.</description><subject>Adenylyl Cyclases - drug effects</subject><subject>Adenylyl Cyclases - metabolism</subject><subject>Animals</subject><subject>Apud cells. Peptide and protein hormones. Growth factors</subject><subject>Binding, Competitive</subject><subject>Biological and medical sciences</subject><subject>CHO Cells - metabolism</subject><subject>CHO Cells - ultrastructure</subject><subject>Cricetinae</subject><subject>Enzyme Activation - drug effects</subject><subject>Fundamental and applied biological sciences. Psychology</subject><subject>Humans</subject><subject>Kinetics</subject><subject>Neuropeptides - drug effects</subject><subject>Neuropeptides - metabolism</subject><subject>Pituitary Adenylate Cyclase-Activating Polypeptide</subject><subject>Rats</subject><subject>Receptors, Pituitary Adenylate Cyclase-Activating Polypeptide</subject><subject>Receptors, Pituitary Hormone - drug effects</subject><subject>Receptors, Pituitary Hormone - metabolism</subject><subject>Receptors, Vasoactive Intestinal Peptide - drug effects</subject><subject>Receptors, Vasoactive Intestinal Peptide - metabolism</subject><subject>Stimulation, Chemical</subject><subject>Structure-Activity Relationship</subject><subject>Vasoactive Intestinal Peptide - analogs & derivatives</subject><subject>Vasoactive Intestinal Peptide - chemical synthesis</subject><subject>Vasoactive Intestinal Peptide - pharmacology</subject><subject>Vertebrates: endocrinology</subject><issn>0014-2999</issn><issn>1879-0712</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1998</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNo9kMtKAzEUhoMotVYfoTALEV2MzWUmmSxL8VIoWPBCV4Ykk2BkbibTim_vTDt0dfg5338OfABMEbxHENHZK4QoiTHn_JZndxAmJI03J2CMMsZjyBA-BeMjcg4uQviGEKYcpyMw4gxTStgYfC6r1nipW1dXUW2jwjV18-UKp6OP5TrKjXc72bqdCdGva78ib3RdKlfJqu0BNFvPF_N1JKu8j3iIHWWatvbhEpxZWQRzNcwJeH98eFs8x6uXp-Vivoo1ydI2toZyqTXNaaKyBCtmGaGUc4qYSXWSIykVlRiaTBFkCVOpyrnGllqkJM0omYCbw93G1z9bE1pRuqBNUcjK1NsgGMk4JynswPQAal-H4I0VjXel9H8CQdF7FXuvopcmeCb2XsWm602HB1tVmvzYGkR2--thL4OWhfWy0i4cMZxAijEh__SEf60</recordid><startdate>19980731</startdate><enddate>19980731</enddate><creator>GOURLET, P</creator><creator>RATHE, J</creator><creator>DE NEEF, P</creator><creator>CNUDDE, J</creator><creator>VANDERMEERS-PIRET, M.-C</creator><creator>WAELBROECK, M</creator><creator>ROBBERECHT, P</creator><general>Elsevier</general><scope>IQODW</scope><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7X8</scope></search><sort><creationdate>19980731</creationdate><title>Interaction of lipophilic VIP derivatives with recombinant VIP1/PACAP and VIP2/PACAP receptors</title><author>GOURLET, P ; RATHE, J ; DE NEEF, P ; CNUDDE, J ; VANDERMEERS-PIRET, M.-C ; WAELBROECK, M ; ROBBERECHT, P</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c385t-fe69acc6d64b842b7f736699617e5c4d1aab6a20e8b31f37b5bd9c2f6f1ba6863</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1998</creationdate><topic>Adenylyl Cyclases - drug effects</topic><topic>Adenylyl Cyclases - metabolism</topic><topic>Animals</topic><topic>Apud cells. Peptide and protein hormones. Growth factors</topic><topic>Binding, Competitive</topic><topic>Biological and medical sciences</topic><topic>CHO Cells - metabolism</topic><topic>CHO Cells - ultrastructure</topic><topic>Cricetinae</topic><topic>Enzyme Activation - drug effects</topic><topic>Fundamental and applied biological sciences. Psychology</topic><topic>Humans</topic><topic>Kinetics</topic><topic>Neuropeptides - drug effects</topic><topic>Neuropeptides - metabolism</topic><topic>Pituitary Adenylate Cyclase-Activating Polypeptide</topic><topic>Rats</topic><topic>Receptors, Pituitary Adenylate Cyclase-Activating Polypeptide</topic><topic>Receptors, Pituitary Hormone - drug effects</topic><topic>Receptors, Pituitary Hormone - metabolism</topic><topic>Receptors, Vasoactive Intestinal Peptide - drug effects</topic><topic>Receptors, Vasoactive Intestinal Peptide - metabolism</topic><topic>Stimulation, Chemical</topic><topic>Structure-Activity Relationship</topic><topic>Vasoactive Intestinal Peptide - analogs & derivatives</topic><topic>Vasoactive Intestinal Peptide - chemical synthesis</topic><topic>Vasoactive Intestinal Peptide - pharmacology</topic><topic>Vertebrates: endocrinology</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>GOURLET, P</creatorcontrib><creatorcontrib>RATHE, J</creatorcontrib><creatorcontrib>DE NEEF, P</creatorcontrib><creatorcontrib>CNUDDE, J</creatorcontrib><creatorcontrib>VANDERMEERS-PIRET, M.-C</creatorcontrib><creatorcontrib>WAELBROECK, M</creatorcontrib><creatorcontrib>ROBBERECHT, P</creatorcontrib><collection>Pascal-Francis</collection><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>MEDLINE - Academic</collection><jtitle>European journal of pharmacology</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>GOURLET, P</au><au>RATHE, J</au><au>DE NEEF, P</au><au>CNUDDE, J</au><au>VANDERMEERS-PIRET, M.-C</au><au>WAELBROECK, M</au><au>ROBBERECHT, P</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Interaction of lipophilic VIP derivatives with recombinant VIP1/PACAP and VIP2/PACAP receptors</atitle><jtitle>European journal of pharmacology</jtitle><addtitle>Eur J Pharmacol</addtitle><date>1998-07-31</date><risdate>1998</risdate><volume>354</volume><issue>1</issue><spage>105</spage><epage>111</epage><pages>105-111</pages><issn>0014-2999</issn><eissn>1879-0712</eissn><coden>EJPHAZ</coden><abstract>Stearyl vasoactive intestinal polypeptide has been reported to be a VIP (vasoactive intestinal polypeptide) receptor agonist of high potency with an original bioavailability and action. We synthesized three fatty acyl derivatives, myristyl-, palmityl- and stearyl-[Nle17]VIP, and tested their capacity to recognize recombinant rat- and human VIP1- and VIP2/PACAP (pituitary adenylate cyclase-activating polypeptide) receptors and to stimulate adenylate cyclase activity. The three lipophilic analogues bound with high affinity (from 0.5 to 20 nM) to both receptor subtypes but did not distinguish between them. In preparations expressing a high density of human VIP1/PACAP receptors, the three lipophilic analogues had the same efficacy as VIP and [Nle17]VIP. In preparations expressing the rat receptors, stearyl-[Nle17]VIP had a lower efficacy than the other peptides tested. In preparations expressing a low level of VIP1/PACAP receptors and in those expressing VIP2/PACAP receptors, all analogues behaved like partial agonists. The lowest efficacy was observed for stearyl-[Nle17]VIP on the VIP2/PACAP receptor subclass. Based on our results, a complex pattern of in vivo biological effects of the lipophilic VIP derivatives should be expected: these compounds might behave as full agonists, partial agonists, or antagonists of the VIP response, depending on the number and the subtype of receptor expressed.</abstract><cop>Amsterdam</cop><pub>Elsevier</pub><pmid>9726637</pmid><doi>10.1016/S0014-2999(98)00435-X</doi><tpages>7</tpages></addata></record> |
| fulltext | fulltext |
| identifier | ISSN: 0014-2999 |
| ispartof | European journal of pharmacology, 1998-07, Vol.354 (1), p.105-111 |
| issn | 0014-2999 1879-0712 |
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| subjects | Adenylyl Cyclases - drug effects Adenylyl Cyclases - metabolism Animals Apud cells. Peptide and protein hormones. Growth factors Binding, Competitive Biological and medical sciences CHO Cells - metabolism CHO Cells - ultrastructure Cricetinae Enzyme Activation - drug effects Fundamental and applied biological sciences. Psychology Humans Kinetics Neuropeptides - drug effects Neuropeptides - metabolism Pituitary Adenylate Cyclase-Activating Polypeptide Rats Receptors, Pituitary Adenylate Cyclase-Activating Polypeptide Receptors, Pituitary Hormone - drug effects Receptors, Pituitary Hormone - metabolism Receptors, Vasoactive Intestinal Peptide - drug effects Receptors, Vasoactive Intestinal Peptide - metabolism Stimulation, Chemical Structure-Activity Relationship Vasoactive Intestinal Peptide - analogs & derivatives Vasoactive Intestinal Peptide - chemical synthesis Vasoactive Intestinal Peptide - pharmacology Vertebrates: endocrinology |
| title | Interaction of lipophilic VIP derivatives with recombinant VIP1/PACAP and VIP2/PACAP receptors |
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