PUBLICATION

Development of a CCK1R-membrane nanoparticle as a fish-out tool for bioactive peptides

Authors
Staljanssens, D., Rico, C.A., Park, M., Van Camp, J., Yu, N., Huber, T., Sakmar, T.P., Smagghe, G.
ID
ZDB-PUB-170214-260
Date
2015
Source
Peptides   68: 219-27 (Journal)
Registered Authors
Keywords
Affinity-selection, Cholecystokinin, Cholecystokinin receptor type 1, GPCR, NABBs
MeSH Terms
  • Animals
  • Apolipoproteins/chemistry
  • Biosensing Techniques
  • Calcium Signaling
  • Drug Evaluation, Preclinical/methods
  • HEK293 Cells
  • Humans
  • Nanoparticles/chemistry*
  • Protein Transport
  • Rats
  • Receptors, Cholecystokinin/biosynthesis
  • Receptors, Cholecystokinin/chemistry*
  • Receptors, Cholecystokinin/genetics
  • Zebrafish Proteins/chemistry
PubMed
25451329 Full text @ Peptides
Abstract
The cholecystokinin receptor type 1 (CCK1R) is a G protein-coupled receptor (GPCR) that is involved in several biological processes including the regulation of the secretion of digestive enzymes. The peptide hormone cholecystokinin (CCK) binds to CCK1R, which is an important pharmacological target for several diseases, including obesity. Interestingly, nutritional dietary peptides also appear to activate CCK1R, and may play a role in CCK1R signaling in the gut. In this study, a novel technique to screen for CCK1R ligands based on affinity-selection is described. Functional expressed CCK1R is reconstituted into membrane nanoparticles called NABBs (nanoscale apo-lipoprotein bound bilayers). NABBs are native-like bilayer membrane systems for incorporation of GPCRs. CCK1R-NABBs were characterized using a fluorescently labeled CCK analog and can be used as a cutting-edge technology to screen for CCK1R ligands using affinity-selection mass spectrometry.
Genes / Markers
Figures
Expression
Phenotype
Mutations / Transgenics
Human Disease / Model
Sequence Targeting Reagents
Fish
Antibodies
Orthology
Engineered Foreign Genes
Mapping