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    The Melanocortin System: Structure Activity Relationships of Alpha-N-Methylated MT-II Analogues and Mutation Studies of Human Melanocortin Receptor Subtypes 1 and 4

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    Author
    Dedek, Matthew Milan
    Issue Date
    2007
    Keywords
    structure activity relationship
    melanocortin 1 receptor
    melanocortin
    MT-II
    mutagenesis
    melanocortin 4 receptor
    Advisor
    Hruby, Victor J.
    Committee Chair
    Hruby, Victor J.
    
    Metadata
    Show full item record
    Publisher
    The University of Arizona.
    Rights
    Copyright © is held by the author. Digital access to this material is made possible by the University Libraries, University of Arizona. Further transmission, reproduction or presentation (such as public display or performance) of protected items is prohibited except with permission of the author.
    Abstract
    The melanocortin system regulates various physiological processes including feeding behavior, sexual function, skin pigmentation and photoprotection via five G-protein coupled receptors and several endogenous ligands. There is a need for selective and potent ligands to the human melanocortin receptors (hMCRs) that can chemically resolve these various functions. This thesis presents three studies aimed at refining the understanding of the structural differences between binding pockets of the hMCR subtypes. In the first study α-N-methylated analogues of the non-selective agonist, MT-II, are evaluated for their in vitro function. This study produced the most potent hMC1R selective agonist to date. The following two studies examine the effects of mutations on the biological activity of melanocortin receptor subtypes 1 and 4. Much of the mutation study data is preliminary and requires a demonstration of reproducibility.
    Type
    text
    Electronic Thesis
    Degree Name
    MS
    Degree Level
    masters
    Degree Program
    Medical Pharmacology
    Graduate College
    Degree Grantor
    University of Arizona
    Collections
    Master's Theses

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