CCK8 peptide derivatized with diphenylphosphine for rhenium labelling: Synthesis and molecular mechanics calculations

被引：10

作者：

Morelli, G

De Luca, S

Tesauro, D

Saviano, M

Pedone, C

Dolmella, A

Visentin, R

Mazzi, U

机构：

[1] CIRPEB, I-80134 Naples, Italy

[2] CNR, Ist Biostrutture & Bioimmagini, I-80134 Naples, Italy

[3] Univ Padua, Dipartimento Sci Farmaceut, I-35131 Padua, Italy

来源：

JOURNAL OF PEPTIDE SCIENCE | 2002年 / 8卷 / 07期

关键词：

CCK8; derivatives; molecular mechanics calculations; rhenium-peptide complex; solid-phase peptide synthesis;

D O I：

10.1002/psc.400

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：

A novel CCK8 derivative bearing a chelating agent at its N- end and its oxo-rhenium(V) complex have been synthesized and characterized. The chelating agent N-{N-[3-(diphenylphosphino)propionyl]glycyl}cysteine (PN2S) ligand, the coordination set of which is made by the phosphorus atom of phosphine, the nitrogen atoms of the two amido groups and the sulphur atom of cysteine, has been used due to its high affinity towards the oxo-rhenium(V) moiety. Molecular modelling studies indicate that the CCK8 peptide adopts the right conformation for cholecystokinin receptor binding, and that modifications on the N-terminal side of CCK8 obtained by introducing chelating agents and its metal complexes should not affect the interaction with CCKA receptor. Copyright (C) 2002 European Peptide Society and John Wiley Sons, Ltd.

引用

页码：373 / 381

页数：9

共 20 条

[1] The Protein Data Bank [J].