Novel, potent small molecule motilin receptor antagonists are described. These peptidomimetic macrocycles are composed of a tripeptide cyclized backbone-to-backbone with a nonpeptidic tether and bear new unnatural amino acids containing basic side chains.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/j.bmcl.2007.05.043 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Bitter-tasting drugs tune GDF15 and GLP-1 expression via bitter taste or motilin receptors in the intestine of patients with obesity.
Mol Metab
October 2024
Gut Peptide Research Lab, Translational Research for Gastrointestinal Disorders (TARGID), KU Leuven, Leuven, Belgium. Electronic address:
Article Synopsis
- Growth differentiation factor 15 (GDF15) is identified as a new satiety signal that works through the GFRAL receptor in the brain, and bitter compounds can trigger GDF15 expression in response to gut stress related to obesity.
- * A study tested the effects of the bitter drug hydroxychloroquine on plasma GDF15 levels, finding that it increased GDF15 and reduced hunger in healthy participants.
- * Results indicate that various bitter compounds influence GDF15 expression in gut cells, and this process is affected by specific taste receptors (TAS2Rs) and obesity-related factors.
Molecular characterization and distribution of motilin and motilin receptor in the Japanese medaka Oryzias latipes.
Cell Tissue Res
July 2024
Department of Biological Science, Graduate School of Science and Engineering, University of Toyama, Gofuku, Toyama, 3190, Japan.
Motilin (MLN) is a peptide hormone originally isolated from the mucosa of the porcine intestine. Its orthologs have been identified in various vertebrates. Although MLN regulates gastrointestinal motility in tetrapods from amphibians to mammals, recent studies indicate that MLN is not involved in the regulation of isolated intestinal motility in zebrafish, at least in vitro.
View Article and Find Full Text PDFMotilin, a Novel Orexigenic Factor, Involved in Feeding Regulation in Yangtze Sturgeon ().
Biomolecules
April 2024
Department of Aquaculture, College of Animal Science and Technology, Sichuan Agricultural University, Chengdu 611130, China.
Motilin is a gastrointestinal hormone that is mainly produced in the duodenum of mammals, and it is responsible for regulating appetite. However, the role and expression of motilin are poorly understood during starvation and the weaning stage, which is of great importance in the seeding cultivation of fish. In this study, the sequences of Yangtze sturgeon ( ()) motilin receptor () were cloned and characterized.
View Article and Find Full Text PDFThe role of free fatty acid receptor-1 in gastric contractions in .
Food Funct
February 2024
Area of Regulatory Biology, Division of Life Science, Graduate School of Science and Engineering, Saitama University, Saitama, Japan.
Motilin is an important hormonal regulator in the migrating motor complex (MMC). Free fatty acid receptor-1 (FFAR1, also known as GPR40) has been reported to stimulate motilin release in human duodenal organoids. However, how FFAR1 regulates gastric motility is unclear.
View Article and Find Full Text PDFDoes ghrelin regulate intestinal motility in rabbits? An in vitro study using isolated duodenal strips.
Gen Comp Endocrinol
December 2023
School of Veterinary Medicine, Rakuno Gakuen University, Ebetsu, Hokkaido 069-8501, Japan. Electronic address:
Article Synopsis
- The study investigates the effects of rat ghrelin and motilin on muscle contractions in the rabbit duodenum, particularly focusing on ghrelin's role, which has been previously linked to GI motility in other animals.
- Results show that rat ghrelin did not influence the contractile activity of the duodenum, as its receptor mRNA was found to have low expression in this region compared to other GI areas like the esophagus and stomach.
- Conversely, motilin successfully induced muscle contractions, suggesting that while motilin is an important player in GI motility, ghrelin does not regulate contractions in the rabbit duodenum due to a lack of its receptors.
Want AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!