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- W2017574137 abstract "The melanocortin receptors are involved in many physiological functions, including pigmentation, sexual function, feeding behavior, and energy homeostasis, making them potential targets to treat obesity, sexual dysfunction, etc. Understanding the basis of the ligand-receptor interactions is crucial for the design of potent and selective ligands for these receptors. The conformational preferences of the cyclic melanocortin ligands MTII (Ac-Nle4-c[Asp5-His6-DPhe7-Arg8-Trp9-Lys10]–NH2) and SHU9119 (Ac-Nle4-c[Asp5-His6-DNal(2′)7-Arg8-Trp9-Lys10]–NH2), which show agonist and antagonist activity at the h-MC4R, respectively, were comprehensively investigated by solution NMR spectroscopy in different environments. In particular, water and water/DMSO (8:2) solutions were used as isotropic solutions and an aqueous solution of DPC (dodecylphosphocholine) micelles was used as a membrane mimetic environment. NMR-derived conformations of these two ligands were docked within h-MC4R models. NMR and docking studies revealed intriguing differences which can help explain the different activities of these two ligands." @default.
- W2017574137 created "2016-06-24" @default.
- W2017574137 creator A5024121378 @default.
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- W2017574137 creator A5040940946 @default.
- W2017574137 creator A5070184458 @default.
- W2017574137 creator A5076760321 @default.
- W2017574137 date "2011-09-01" @default.
- W2017574137 modified "2023-09-23" @default.
- W2017574137 title "Conformational study on cyclic melanocortin ligands and new insight into their binding mode at the MC4 receptor" @default.
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- W2017574137 doi "https://doi.org/10.1016/j.ejmech.2011.05.038" @default.
- W2017574137 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/5102844" @default.
- W2017574137 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/21652123" @default.
- W2017574137 hasPublicationYear "2011" @default.
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