Receptor fragment approach to the binding between CCK8 peptide and cholecystokinin receptors: A fluorescence study on type B receptor fragment CCKB-R (352-379)
Receptor fragment approach to the binding between CCK8 peptide and cholecystokinin receptors: A fluorescence study on type B receptor fragment CCKB-R (352-379)(540 views) De Luca S, Sanseverino M, Zocchi I, Pedone C, Morelli G, Ragone R
Keywords: Cholecystokinin Type B Receptor, Fluorescence Spectroscopy, Peptide-Receptor Binding, Surfactant Titration, Cck8 Peptides, Fluorescence Titrations, Receptor Fragment Approach, Binding Energy, Biological Membranes, Dissociation, Proteins, Spectroscopic Analysis, Polypeptides, Cholecystokinin A Receptor, Cholecystokinin B Receptor, Cholecystokinin Octapeptide, Cholecystokinin Receptor, Ligand, Solvent, Analytic Method, Article, Dissociation Constant, Drug Receptor Binding, Equilibrium Constant, Molecular Model, Reliability, Circular Dichroism, Peptide Fragments, Spectrometry
Affiliations: *** IBB - CNR ***
CIRPEB, Dipartimento di Chimica Biologica, Università Federico II, Via Mezzocannone 6/8, Naples, I-80134, Italy
INBIOS srl, Via Olivetti 1, Pozzuoli (NA), I-80078, Italy
Dipto. di Biochimica e Biofisica, CRISCEB, Seconda Universita di Napoli, Via Costantinopoli 16, I-80138 Naples, Italy
References: Not available.
Receptor fragment approach to the binding between CCK8 peptide and cholecystokinin receptors: A fluorescence study on type B receptor fragment CCKB-R (352-379)
Fluorescence titrations in a membrane mimetic solvent system allowed us to estimate that the dissociation constant of the bimolecular complex between CCK8 peptide and cholecystokinin type B receptor fragment CCKB-R (352-379) is in the micromolar range. When considered in the context of the full receptor/ligand model, these experiments demonstrate that the receptor fragment chosen on the basis of previous structural studies represents a reliable model system to monitor the ability of CCK8 or CCK8 analogs to bind the cholecystokinin receptor. Together with previous studies, this confirms that the receptor fragment approach adopted to define the binding mode of the CCK8 fragment of cholecystokinin with its two receptors, CCKA and CCKB can be used to characterize the binding from the equilibrium standpoint. In this context, fluorescence spectros-copy proves to be the favored technique to measure dissociation constants in the nanomolar to micromolar range. (C) 2005 Wiley Periodicals, Inc.
Receptor fragment approach to the binding between CCK8 peptide and cholecystokinin receptors: A fluorescence study on type B receptor fragment CCKB-R (352-379)
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Receptor fragment approach to the binding between CCK8 peptide and cholecystokinin receptors: A fluorescence study on type B receptor fragment CCKB-R (352-379)