Motilin Family Related Drug Discovery Products
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Motilin, a 22 amino acid hormone present in some endocrine cells of the human jejunum and duodenum as well as, to a lesser extent, the human gastric antrum, is known to enhance gastrointestinal (GI) motility. Besides increasing stomach motility and easing symptoms in those with delayed gastric emptying, the antibiotic erythromycin also stimulates the motilin receptor.
With years of experience in the field of drug discovery, Creative Biolabs can offer high-quality motilin family tools to contribute to the success of your project:
Overview of Motilin Family
The thyroid gland's orphan G protein-coupled receptor GPR38 was first identified as the human motilin receptor (MLNR). The MLNR, meanwhile, has been cloned from dogs and rabbits, two other species. These receptors share 84% and 71% of the human MLNR's sequence, respectively. Although their precise distribution varies depending on the species, motilin receptors are primarily present throughout the Gastrointestinal tract. In addition to neurons of the myenteric plexus, MLNRs are expressed in smooth muscle cells from the antrum, duodenum, and colon. In humans, the gastroduodenal area has the highest MLNR density, which declines distally in the small intestine toward the colon. For its medicinal applications, this could have significant ramifications. The colon of rabbits has the highest motilin receptor density. Moreover, MLNRs have been discovered outside of the Gastrointestinal tract in the thyroid, bone marrow, and central nervous system.
Fig.1 Schematic representation of motilin-induced MLNR desensitization. (De Smet, 2009)
Motilin and Ghrelin Receptor
The genes for the receptors for motilin and ghrelin are thought to have shared ancestry. Both of the peptides that are secreted from the stomach while fasting can increase gastric motility. The increasing distribution of ghrelin and its receptor outside the GI tract creates more non-GI activities, yet the ligands for each receptor do not readily activate the other. The roles of motilin differ substantially between species. In instance, the finding that rodents lack a functional motilin system but do have pseudogenes shows that motilin functions have been lost via evolution. This loss, which was not observed for ghrelin, has been connected to pronounced morphological and functional abnormalities of the rodent stomach, such as the particular inability to vomit.
Fig.2 Phylogenetic tree showing alignment of motilin receptors. (Sanger, 2012)
Motilin Family Drug Discovery
It is obvious that motilin's lack of pleiotropy over ghrelin is one of its main advantages. Future ghrelin agonist development for the treatment of GI problems may encounter difficulties due to the drug's endocrine effects, which include stimulating the release of growth hormone and inhibiting the production of insulin. Hence, ghrelin antagonists or agonists in particular may have negative effects on memory and mood. Hence, the development of ghrelin antagonists with low central nervous system penetration seems justified. Hence, narrowing the focus will be a difficult task for ghrelin agonist development.
References
- De Smet, B.; et al. Motilin and ghrelin as prokinetic drug targets. Pharmacology & therapeutics. 2009, 123(2): 207-223.
- Sanger, G.J. Motilin receptor neuropharmacology: revised understanding. Current Opinion in Pharmacology. 2012, 12(6): 641-646.
