CCK8 peptide derivatized with diphenylphosphine for rhenium labelling: Synthesis and molecular mechanics calculations(447 views) Morelli G, De Luca S, Tesauro D, Saviano M, Pedone C, Dolmella A, Visentin R, Mazzi U
Keywords: Cck8 Derivatives, Molecular Mechanics Calculations, Rhenium-Peptide Complex, Solid-Phase Peptide Synthesis, Amide, Chelating Agent, Cholecystokinin A Receptor, Cholecystokinin Derivative, Cholecystokinin Octapeptide, Cholecystokinin Receptor, Coordination Compound, Cysteine, Ligand, Metal Complex, Nitrogen, Phosphine, Phosphine Derivative, Phosphorus, Sulfur, Peptide Fragment, Phenol Derivative, Amino Terminal Sequence, Article, Binding Affinity, Complex Formation, Controlled Study, Isotope Labeling, Molecular Model, Priority Journal, Protein Analysis, Protein Conformation, Protein Interaction, Protein Modification, Protein Structure, Protein Synthesis, Receptor Binding, Amino Acid Sequence, Chemical Structure, Chemistry, Methodology, Molecular Structure, Support, Non-U S Gov
Affiliations: *** IBB - CNR ***
Centro Interuniversitario Per la Ricerca Sui Peptidi Bioattivi (CIRPEB), Istituto di Biostrutture e Bioimmagini, CNR, 80134 Napoli, Italy
Dipartimento di Scienze Farmaceutiche, Università di Padova, 35131 Padova, Italy
References: Not available.
CCK8 peptide derivatized with diphenylphosphine for rhenium labelling: Synthesis and molecular mechanics calculations
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.
CCK8 peptide derivatized with diphenylphosphine for rhenium labelling: Synthesis and molecular mechanics calculations
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CCK8 peptide derivatized with diphenylphosphine for rhenium labelling: Synthesis and molecular mechanics calculations