Cholecystokinin Family Related Drug Discovery Products
Creative Biolabs has the assays you can rely on for high throughput screening, lead optimization, characterizing and discovering targets, and uncovering the complexity of disease pathways. We can offer membrane protein in vitro assay kits that save valuable laboratory time and is ideal for high throughput screening.
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Cholecystokinin (CCK) is a neurotransmitter that is primarily found in the gastrointestinal tract and is a regulatory peptide hormone. CCK controls stomach emptying, gastric acid secretion, pancreatic enzyme secretion, and motility in the digestive system. CCK plays a role in memory and learning processes, nociception, satiety, and anxiogenesis within the nervous system. Moreover, in some regions of the Brain, CCK interacts with other neurotransmitters. Two distinct G protein coupled receptor subtypes known as CCK1 and CCK2 mediate the pharmacological actions of CCK.
Creative Biolabs offers a range of cholecystokinin family drug discovery tools with our well-established high-efficient drug discovery strategy in a timely and cost-effective manner:
Overview of Cholecystokinin Family
Many cellular processes crucial for nutrient absorption are carried out by CCK1 receptors (CCKAR). They include gastrointestinal motility, pancreatic exocrine secretion, post-cibal gallbladder contraction stimulation, and satiety. They are mediated by receptors on the enteric neurons, central nervous system nuclei, pyloric smooth muscle, pancreatic neurons (in humans, as well as directly on pancreatic acinar cells in rodents), and gallbladder muscularis.
Fig.1 The amino acid sequences of the human CCK1. (Miller & Gao, 2008)
The striatum, cerebral cortex, and limbic system are where CCK2 receptors (CCKBR) are most abundant in the brain. They are also found in the gastric oxyntic mucosa. These receptors contribute to anxiety and nociception in addition to promoting stomach acid secretion. Many neoplasms have also been found to express CCK1 and CCK2 receptors, both of which have the capacity to stimulate cell proliferation and may play a role in the development of cancer and aggressive tumor behavior.
Fig.2 The amino acid sequences of the human CCK2. (Miller & Gao, 2008)
Chemoattractant Family Drug Discovery
In addition to exhibiting remarkable diversity in ligand recognition specificity and mechanisms of biochemical and cellular regulation, two structurally similar G protein-coupled receptors for two closely related peptides, CCK and gastrin, have evolved. These receptors also play unique and different roles in physiology and pathophysiology. Several members of this amazing receptor superfamily should be amenable to the paradigms for ligand recognition, receptor modulation, and activity. The physiologic functions of gastrin, CCK, and their receptors are extensive and important. Almost all of CCK's physiological effects are related to nutritional homeostasis, which is obviously crucial to the organism's survival. In order to create the ideal luminal environment for peptic activity and vitamin B12 absorption, gastrin directly stimulates stomach acid secretion. Irritable bowel syndrome has been linked to the dysfunction of this signaling system because CCK may cause an overly reactive motility response.
Reference
- Miller, L. J., & Gao, F. Structural basis of cholecystokinin receptor binding and regulation. Pharmacology & therapeutics. 2008, 119(1): 83-95.