Development of G-quadruplex Stabilizers as Anticancer Drug Therapy and Selective Agonists of the Human Oxytocin Receptor as a Therapeutic Tool for Neuropsychiatric Disorders

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  • March 21, 2019
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  • Sassano, Maria F.
    • Affiliation: Eshelman School of Pharmacy, Division of Chemical Biology and Medicinal Chemistry
Abstract
  • The principal aim of pharmacology in drug discovery is the characterization of drug activity by system-independent scales that allow prediction of drug activity in all cellular systems. This thesis concentrated in two drug targets: telomeres and GPCRs. Telomere biology is a validated anticancer drug target. G-protein-coupled receptors (GPCRs) recognize external ligands and transmit signals to cellular G-proteins (guanine-nucleotide-binding proteins) to elicit a response. These receptors are tractable for drug discovery because they are on the cell surface therefore drugs do not need to penetrate the cell to produce an effect [1]. In 2000, nearly half of all prescription drugs in the US were targeted towards GPCRs [2]. The projects in this dissertation will describe two different approaches to the successful identification of small-molecules that interact with their validated targets. The first project focused on the identification of new G-quadruplex stabilizers and their ability to inhibit human telomerase as an anticancer drug modality. The second project focused on the efforts made towards the identification of novel small molecules that selectively activate the human oxytocin receptor to regulate complex behaviors in animal models with therapeutic implications in various neuropsychiatric disorders.
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  • In Copyright
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  • "... in partial fulfillment of the requirements for the degree of Doctor of Philosophy in the School of Pharmacy (Medicinal Chemistry and Natural Products)."
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  • Jarstfer, Michael
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  • Chapel Hill, NC
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  • Open access
Date uploaded
  • March 18, 2013

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file details Development of g-quadruplex stabilizers as anticancer drug therapy and selective agonists of the human oxytocin receptor as a therapeutic tool for neuropsychiatric disorders 2019-04-15 Public Download