Structure-activity relationship study on small peptidic GPR54 agonists.
Publication/Presentation Date
11-15-2006
Abstract
Metastin (kisspeptin-54) is an endogenous ligand that modulates gonadotropin-releasing hormone (GnRH) secretion through the interaction with a G protein-coupled receptor (GPCR), GPR54. The short-chain C-terminal decapeptide amide, metastin (45-54) (kisspeptin-10), exerts the identical bioactivities to metastin, such as metastasis suppression of cancer cells and inhibition of trophoblast migration and invasion. In order to understand the structural requirement for GPR54 agonistic activity, structure-activity relationship (SAR) study on pentapeptide-based C-terminal metastin analogues was carried out. As a result, H-Amb-Nal(2)-Gly-Leu-Arg-Trp-NH2 34 was identified as a novel GPR54 agonist that possessed the most potent GPR54 agonistic activity reported so far.
Volume
14
Issue
22
First Page
7595
Last Page
7603
ISSN
0968-0896
Published In/Presented At
Tomita, K., Niida, A., Oishi, S., Ohno, H., Cluzeau, J., Navenot, J. M., Wang, Z. X., Peiper, S. C., & Fujii, N. (2006). Structure-activity relationship study on small peptidic GPR54 agonists. Bioorganic & medicinal chemistry, 14(22), 7595–7603. https://doi.org/10.1016/j.bmc.2006.07.009
Disciplines
Business Administration, Management, and Operations | Health and Medical Administration | Management Sciences and Quantitative Methods
PubMedID
16879969
Department(s)
Administration and Leadership
Document Type
Article