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- W2170416391 abstract "Melanocortin receptors (MC1R-MC5R) belong to the G-protein coupled receptor superfamily. The interactions of peptide hormones (ACTH, a-, |3and y-MSH) with the melanocortin receptors regulate multiple physiological functions in the human body. Pharmacological studies of the melanocortin receptors have revealed very broad biological effects including pigmentation, steroidogenesis, energy homeostasis, thermoregulation, anti-inflammation, nerve regeneration, sexual behavior, feeding behavior and memory, and others. Due to the lack of selectivity of the endogenous ligands (except ACTH) the exact biological roles of the melanocortin receptor subtypes have not been fully elucidated. The objectives of our research are the design and synthesis of new, selective and potent ligands for the melanocortin receptor subtypes to help elucidate their biological functions. Since the three-dimensional structures of the melanocortin receptors and their endogenous ligands are unknown, receptor structurebased design has not been applied. We have chosen a classical ligand-based design with the primary structure of an endogenous ligand, y-MSH, as a starting point. Our design strategy is to gain high selectivity and potency by fixing the spatial structure of this very flexible peptide ligand in hopes that we can induce the bioactive conformation. We have examined two strategies to constrain the peptide backbone. The first approach is based on global constraint of the peptides by cyclization. A group of 36 cyclic peptides has been synthesized using thioether bond formation as a cyclization step. Macrocyclic peptide ligands varied from 15to 30-membered rings. The truncated sequence of y-MSH" @default.
- W2170416391 created "2016-06-24" @default.
- W2170416391 creator A5016469829 @default.
- W2170416391 date "2004-01-01" @default.
- W2170416391 modified "2023-09-27" @default.
- W2170416391 title "DESIGN AND SYNTHESIS OF NOVEL MELANOCORTIN RECEPTOR LIGANDS" @default.
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