Cholecystokinin A receptor
Encyclopedia
The extracellular, N-terminal, domain
of this protein adopts a tertiary structure consisting of a few helical turn
s and a disulfide
-cross linked loop. It is required for interaction of the cholecystokinin A receptor with its corresponding hormonal
ligand
.
Protein domain
A protein domain is a part of protein sequence and structure that can evolve, function, and exist independently of the rest of the protein chain. Each domain forms a compact three-dimensional structure and often can be independently stable and folded. Many proteins consist of several structural...
of this protein adopts a tertiary structure consisting of a few helical turn
Turn (biochemistry)
A turn is an element of secondary structure in proteins where the polypeptide chain reverses its overall direction.- Definition :According to the most common definition, a turn is a structural motif where the Cα atoms of two residues separated by few peptide bonds are in close approach A turn is...
s and a disulfide
Disulfide bond
In chemistry, a disulfide bond is a covalent bond, usually derived by the coupling of two thiol groups. The linkage is also called an SS-bond or disulfide bridge. The overall connectivity is therefore R-S-S-R. The terminology is widely used in biochemistry...
-cross linked loop. It is required for interaction of the cholecystokinin A receptor with its corresponding hormonal
Hormone
A hormone is a chemical released by a cell or a gland in one part of the body that sends out messages that affect cells in other parts of the organism. Only a small amount of hormone is required to alter cell metabolism. In essence, it is a chemical messenger that transports a signal from one...
ligand
Ligand (biochemistry)
In biochemistry and pharmacology, a ligand is a substance that forms a complex with a biomolecule to serve a biological purpose. In a narrower sense, it is a signal triggering molecule, binding to a site on a target protein.The binding occurs by intermolecular forces, such as ionic bonds, hydrogen...
.
Agonists
- CholecystokininCholecystokininCholecystokinin is a peptide hormone of the gastrointestinal system responsible for stimulating the digestion of fat and protein...
- CCK-4CCK-4Cholecystokinin tetrapeptide is a peptide fragment derived from the larger peptide hormone cholecystokinin...
- SR-146,131
- A-71623 - modified tetrapeptide, potent and selective CCKA agonist, IC50 3.7nM, 1200x selectivity over CCKB, CAS# 130408-77-4
Antagonists
- ProglumideProglumideProglumide is a drug that inhibits gastrointestinal motility and reduces gastric secretions. It acts as a cholecystokinin antagonist, which blocks both the CCKA and CCKB subtypes...
- LorglumideLorglumideLorglumide is a drug which inhibits gastrointestinal motility and reduces gastric secretions, acting as a cholecystokinin antagonist, with fairly high selectivity for the CCKA subtype...
- DevazepideDevazepideDevazepide is a drug which is structurally derived from the benzodiazepine family, but with quite different actions from most benzodiazepines, lacking affinity for GABAA receptors and instead acting as a cholecystokinin antagonist selective for the CCKA subtype...
- DexloxiglumideDexloxiglumideDexloxiglumide is a drug which acts as a cholecystokinin antagonist, selective for the CCKA subtype. It inhibits gastrointestinal motility and reduces gastric secretions, and despite older selective CCKA antagonists such as lorglumide and devazepide having had only limited success in trials and...
- AsperlicinAsperlicinAsperlicin is a mycotoxin, derived from the fungus Aspergillus alliaceus. It acts as a selective antagonist for the cholecystokinin receptor CCKA, and has been used as a lead compound for the development of a number of novel CCKA antagonists with potential clinical applications....
- SR-27897
- IQM-95333
- JNJ-17156516