His381 of the rat CCKB receptor is essential for CCKB versus CCKA receptor antagonist selectivity
References (40)
- et al.
Enzyme-resistant CCK analogs with high affinities for central receptors
Peptides
(1988) - et al.
Biological actions of cholecystokinin
Peptides
(1994) - et al.
Molecular cloning, functional expression and chromosomal localization of the human cholecystokinin type A receptor
Biochem. Biophys. Res. Commun.
(1993) - et al.
Molecular basis for the species selectivity of the neurokinin-1 receptor antagonists CP-96,345 and RP-67580
J. Biol. Chem.
(1992) - et al.
The role of histidine 265 in antagonist binding to the neurokinin-1 receptor
J. Biol. Chem.
(1994) - et al.
Amino acids of the third transmembrane domain of the AT1A angiotensin II receptor are involved in the differential recognition of peptide and nonpeptide ligands
Biochem. Biophys. Res. Commun.
(1995) - et al.
Peripheral biological activity of SR-27,897: a new potent non-peptide antagonist of CCK-A receptors
Eur. J. Pharmacol.
(1993) - et al.
A single residue, aspartic acid 95, in the d opioid receptor specifies selective high affinity agonist binding
J. Biol. Chem.
(1993) - et al.
The role of the cholecystokinin B/gastrin receptor transmembrane domains in determining affinity for subtype-selective ligands
J. Biol. Chem.
(1995) - et al.
A new potent and selective non peptide gastrin antagonist and brain cholecystokinin receptor ligand: L-365,260
Eur. J. Pharmacol.
(1989)
The seventh transmembrane domain of gastrin/CCK receptors contributes to non peptide antagonist binding
Biochem. Biophys. Res. Commun.
A practical computer based approach to the analysis of radioligand binding experiments
Comput. Methods Programs Biomed.
Two brain CCK receptors: implications for behavioral action
Brain Res
Isolation, sequence analysis, and intron-exon arrangement of the gene encoding bovine Rhodopsin
Cell
Cloning, expression, and characterization of the unique bovine A1 adenosine
J. Biol. Chem.
Molecular cloning of the human brain and gastric cholecystokinin receptors: structure, functional expression and chromosomal localization
Biochem. Biophys. Res. Commun.
A deletion mutation in the third cytoplasmic loop of the mouse m1 muscarinic acetylcholine receptor unmask cryptic G protein binding site
J. Biol. Chem.
Structural model of antagonist and agonist binding to the angiotensin II, AT1 subtype, G protein coupled receptor
Chem. Biol.
A single amino acid of the cholecystokinin B/gastrin receptor determines specificity for non peptides antagonists
Nature
Site of attachment of retinal in rhodopsin
Nature
Cited by (33)
Molecular basis for binding and subtype selectivity of 1,4-benzodiazepine antagonist ligands of the cholecystokinin receptor
2012, Journal of Biological ChemistryCitation Excerpt :Selective, small molecule ligands have been developed for both CCK1R and CCK2R (22, 23). It is now clear, based on limited receptor mutagenesis, photoaffinity labeling, and pharmacological manipulations, that these ligands bind to an allosteric site within the intramembranous helical bundle that is distinct from the orthosteric CCK peptide-binding site of the CCK1R (24–27). However, the molecular basis for ligand selectivity between the two subtypes of CCK receptors remains unclear.
Structural basis of cholecystokinin receptor binding and regulation
2008, Pharmacology and TherapeuticsEvidence that interspecies polymorphism in the human and rat cholecystokinin receptor-2 affects structure of the binding site for the endogenous agonist cholecystokinin
2005, Journal of Biological ChemistryCitation Excerpt :This is likely the result of an increase of the collective contribution of other residues, such as His376, Met67, Cys107, and Phe110, to the binding site of the human CCK2R. This view fully agrees with previous mutagenesis data showing that exchange of His376 for a leucine decreased the affinity of CCK8 for the human CCK2R by 30-fold, whereas mutation of the corresponding amino acid in the rat CCK2R did not affect CCK8 recognition (19, 21). Thereafter, we demonstrated that different contributions of His207 in human versus rat CCK2R were likely not due to different protonated states.
Structure-activity function for binding and signaling in CHO-K1 and COS-7 cells expressing the cholecystokinin A receptor
2004, Biochemical and Biophysical Research CommunicationsConformational and molecular modeling studies of sulfated cholecystokinin-15
2002, Biochemical and Biophysical Research CommunicationsActivation of phospholipase C by cholecystokinin receptor subtypes with different G-protein-coupling specificities in hormone-secreting pancreatic cell lines
2000, Biochemical PharmacologyCitation Excerpt :Surprisingly, the affinity for [3H]L-365,260 was in the same low nM range, which is in contrast to what is generally accepted for the CCKB ligand. To our knowledge, this ligand has never been used in this cell line; hence, comparison to the affinity obtained in COS cells transfected with the CCKB receptor gene (Ki of about 3 nM [39] and ic50 of 2–6 nM [40]) should be made with caution. It bears mentioning that our initial approach, i.e. the use of iodinated CCK-8 as ligand, failed to yield reproducible results and therefore was abandoned in favor of the tritiated ligands.