STRUCTURAL REQUIREMENTS FOR THE BINDING OF THE PITUITARY ADENYLATE-CYCLASE-ACTIVATING PEPTIDE TO RECEPTORS AND ADENYLATE-CYCLASE ACTIVATION IN PANCREATIC AND NEURONAL MEMBRANES

被引：62

作者：

GOURLET, P ^{[1
]}

WOUSSENCOLLE, MC ^{[1
]}

ROBBERECHT, P ^{[1
]}

DENEEF, P ^{[1
]}

CAUVIN, A ^{[1
]}

VANDERMEERSPIRET, MC ^{[1
]}

VANDERMEERS, A ^{[1
]}

CHRISTOPHE, J ^{[1
]}

机构：

[1] UNIV LIBRE BRUXELLES,SCH MED,DEPT BIOCHEM & NUTR,115 BD WATERLOO,B-1000 BRUSSELS,BELGIUM

来源：

EUROPEAN JOURNAL OF BIOCHEMISTRY | 1991年 / 195卷 / 02期

关键词：

D O I：

10.1111/j.1432-1033.1991.tb15734.x

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

PACAP (pituitary adenylate-cyclase-activating peptide)-binding receptors were investigated in membranes from the rat pancreatic acinar cell line, AR 4-2J, the rat hippocampus and the human neuroblastoma cell line NB-OK, by I-125-PACAP(1-27) (amino acid residues 1-27 of N-terminal amidated PACAP) binding and adenylate cyclase activation. The relative binding of I-125-PACAP(1-27) to the receptor, and ability to activate adenylate cyclase were PACAP greater-than-or-equal-to PACAP(1-27) > PACAP(2-38) > PACAP(1-9)-VIP(10-28)(PACAP-VIP) > PACAP(2-27) > [Ser9, Tyr13]VIP > [Tyr13]VIP greater-than-or-equal-to [Ser9]VIP greater-than-or-equal-to VIP(1-23)-PACAP(24-27)(VIP-PACAP) > VIP (vasoactive intestinal peptide). The N-terminal moiety of PACAP(1-27) was more important than the three amino acids at the C-terminus for I-125-PACAP(1-27)-binding site recognition. For rat pancreatic I-125-VIP-binding sites tested with I-125-VIP, the order of binding affinity was PACAP = PACAP(1-27) greater-than-or-equal-to VIP = [Ser9]VIP = [Tyr13]VIP = [Ser9,Tyr13]VIP greater-than-or-equal-to PACAP-VIP greater-than-or-equal-to VIP-PACAP > PACAP(2-38) = PACAP(2-27). Pancreatic I-125-VIP-binding sites, when compared to I-125-PACAP(1-27)-binding sites, showed little specificity and only weak coupling, so that PACAP and VIP-PACAP acted only as partial VIP agonists on adenylate cyclase.

引用

页码：535 / 541

页数：7

共 24 条

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