Distinct molecular mechanisms for agonist peptide binding to types A and B cholecystokinin receptors demonstrated using fluorescence spectroscopy

J Biol Chem. 2005 Jan 14;280(2):1044-50. doi: 10.1074/jbc.M409480200. Epub 2004 Nov 1.

Abstract

Fluorescence spectroscopy provides a direct method for evaluating the environment of a fluorescent ligand bound to its receptor. We utilized this methodology to determine the environment of Alexa within a cholecystokinin (CCK)-like probe (Alexa488-Gly-[(Nle(28,31))CCK-26-33]; CCK-8 probe) bound to the type A CCK receptor (Harikumar, K. G., Pinon, D. L., Wessels, W. S., Prendergast, F. G., and Miller, L. J. (2002) J. Biol. Chem. 277, 18552-18560). Here, we study this probe at the type B CCK receptor and develop another probe with its fluorophore closer to the carboxyl-terminal pharmacophore of type B receptor ligands (Alexa488-Trp-Nle-Asp-Phe-NH2; CCK-4 probe). Both probes bound to type B CCK receptors in a saturable and specific manner and represented full agonists. Similar to the type A receptor, at the type B receptor these probes exhibited shorter lifetimes and lower anisotropy when the receptor was in the active conformation than when it was shifted to its inactive, G protein-uncoupled state using guanosine 5'-[beta,gamma-imido]-triphosphate trisodium salt. Absolute values for lifetime and anisotropy were lower for the CCK-8 probe bound to the type B receptor than for this probe bound to the type A receptor, and Alexa fluorescence was more easily quenched by iodide at the type B receptor. This represents the first direct evidence that, despite having identical affinities for binding and potencies for activating type A and B receptors, CCK is docked via distinct mechanisms, with the amino terminus more exposed to the aqueous milieu when bound to the type B CCK receptor than to the type A CCK receptor. Of interest, despite this difference in binding, activation of both receptors results in analogous direction of movement of the fluorescent indicator probes.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Amino Acid Sequence
  • Animals
  • CHO Cells
  • Cholecystokinin / chemistry
  • Cholecystokinin / metabolism
  • Cricetinae
  • Fluorescence Polarization
  • Fluorescent Dyes / chemistry
  • Fluorescent Dyes / metabolism
  • Fluorescent Dyes / pharmacology
  • Guanylyl Imidodiphosphate / pharmacology
  • Humans
  • Iodides / pharmacology
  • Ligands
  • Molecular Probes / chemistry
  • Molecular Probes / metabolism
  • Molecular Probes / pharmacology
  • Peptides / chemistry
  • Peptides / metabolism*
  • Peptides / pharmacology*
  • Protein Binding / drug effects
  • Receptors, Cholecystokinin / agonists*
  • Receptors, Cholecystokinin / classification
  • Receptors, Cholecystokinin / genetics
  • Receptors, Cholecystokinin / metabolism*
  • Spectrometry, Fluorescence

Substances

  • Fluorescent Dyes
  • Iodides
  • Ligands
  • Molecular Probes
  • Peptides
  • Receptors, Cholecystokinin
  • Guanylyl Imidodiphosphate
  • Cholecystokinin