Intermolecular interactions between peptidic and nonpeptidic agonists and the third extracellular loop of the cholecystokinin 1 receptor.

  title={Intermolecular interactions between peptidic and nonpeptidic agonists and the third extracellular loop of the cholecystokinin 1 receptor.},
  author={Craig Giragossian and Elizabeth Ellen Sugg and Jerzy Ryszard Szewczyk and Dale F. Mierke},
  journal={Journal of medicinal chemistry},
  volume={46 16},
Intermolecular interactions were determined between a synthetic peptide corresponding to the third extracellular loop and several residues from the adjoining sixth and seventh transmembrane domains of the human cholecystokinin-1 receptor, CCK(1)-R(329-357), and the synthetic agonists Ace-Trp-Lys[NH(epsilon)CONH-o-(MePh)]-Asp-MePhe-NH(2) (GI5269) and the C1 N-isopropyl-N-(4-methoxyphenyl)acetamide derivative of 3-(1H-Indazol-3ylmethyl)-3-methyl-5-pyridin-3-yl-1,5-benzodiazepine (GI0122), using… 

Intermolecular interactions between the neurotensin and the third extracellular loop of human neurotensin 1 receptor

For the receptor fragment, NT binding modifies its central part, underlying the great flexibility and adaptability of this region, and despite some substitutions, the human receptor residues that are involved in the interaction with NT could be similar to those of the rat receptor which play an important role in NT binding.

Impact of polyphenols on receptor–ligand interactions by NMR: the case of neurotensin (NT)–neurotensin receptor fragment (NTS1) complex

Experimental modeling protocol will enable the evaluation of other anti-amyloidogenic compounds such as blockers of NT–NTS1 binding and help in understanding the specificity and influence in binding and can provide information to develop new molecules with a putative pharmacological interest.

Unraveling the structure and function of G protein-coupled receptors through NMR spectroscopy.

A summary of the NMR contributions to the study of the structure and function of GPCRs is provided, also in light of the published crystal structures.

The family of G protein-coupled receptors: an example of membrane proteins.

This chapter shows how the synergy between a laboratory experiment and computational modeling leads to structural delineation of the ligand binding pocket and how the knowledge of ligand-protein interactions is used for rational local and global drug design in which the structural knowledge of a particular receptor and its ligands is used in this particular GPCR and others.

How does cholecystokinin stimulate exocrine pancreatic secretion? From birds, rodents, to humans.

  • B. J. WangZ. Cui
  • Biology
    American journal of physiology. Regulatory, integrative and comparative physiology
  • 2007
Clear differences in the relative importance of neural and direct modes of CCK action on pancreatic acinar cells were identified and much further work needs to be directed to the neural mode to map out all sites ofCCK action and details of the full circuits.

GPCRs Revisited: New Insights Lead to Novel Drugs

Next generation ligands include those with novel pharmacologies such as allosteric regulators as well pepducins, that affect the interaction of GPCRs with G proteins, to either block selective receptor signaling pathways or mimic the actions of intracellular domains of receptors, thereby activating GPCR to signal selectively to intrace cellular pathways.

Membrane protein fragments reveal both secondary and tertiary structure of membrane proteins.

This chapter provides many examples of how the study of membrane protein fragments has provided new insight into the structure of the parent membrane protein.

Efficient Synthesis of 1,5‐Benzodiazepines Mediated by Sulfamic Acid under Neat Condition or in Solution

Abstract 2,3‐Dihydro‐1H‐1,5‐benzodiazepines have been synthesized in good to excellent yield from direct condensations of o‐phenylenediamines with ketones promoted by sulfamic acid at room