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Selective Inhibition Studies of Factor Inhibiting Hif (fih)

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dc.contributor.advisorMichael J. Knapp
dc.contributor.authorHolmes, Breanne E
dc.contributor.departmentUniversity of Massachusetts Amherst
dc.contributor.departmentChemistry
dc.date2023-09-23T04:36:16.000
dc.date.accessioned2024-04-26T21:13:55Z
dc.date.available2012-02-21T00:00:00Z
dc.date.issued2011-01-01
dc.date.submittedSeptember
dc.description.abstractThe control of oxygen delivery to cells in the body is the result of a small group of primary oxygen sensors, one of the most important of which is the hypoxia-inducible transcription factor-1 (HIF-1). Two alpha-ketoglutarate dependent non-heme iron dioxygenases are responsible for the regulation of HIF-1 through hydroxylation of residues on the HIF-1a subunit. One of these enzymes, known as the factor inhibiting HIF-1 (FIH-1) is responsible for hydroxylating residue Asn803 on HIF-1a, preventing the transcription of hypoxia related genes controlled by HIF-1. It was hypothesized that there would be a difference in inhibition of FIH-1 from the other HIF-1 regulating enzyme, the prolyl hydroxylase domain-2 (PHD2), when testing a series of ten small molecule inhibitors. The ten inhibitors chosen fell into three classes: pyrones, pyridines, and catechols. Of these inhibitors, it was found that catechols produced a significant inhibitory difference between PHD2 and FIH, and may provide useful in further inhibitor design and synthesis work.
dc.description.degreeMaster of Science (M.S.)
dc.identifier.doihttps://doi.org/10.7275/2192349
dc.identifier.urihttps://hdl.handle.net/20.500.14394/47596
dc.relation.urlhttps://scholarworks.umass.edu/cgi/viewcontent.cgi?article=1802&context=theses&unstamped=1
dc.source.statuspublished
dc.subjectFIH
dc.subjectHIF
dc.subjectInhibition
dc.subjectOxygen Sensing
dc.subjectInorganic Chemistry
dc.subjectMedicinal-Pharmaceutical Chemistry
dc.titleSelective Inhibition Studies of Factor Inhibiting Hif (fih)
dc.typecampus
dc.typearticle
dc.typethesis
digcom.contributor.authorisAuthorOfPublication|email:breanne.holmes@gmail.com|institution:University of Massachusetts Amherst|Holmes, Breanne E
digcom.date.embargo2012-02-21T00:00:00-08:00
digcom.identifiertheses/686
digcom.identifier.contextkey2192349
digcom.identifier.submissionpaththeses/686
dspace.entity.typePublication
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