Developing Small Molecule Inhibitors To Restore Nuclear p27 As A Novel Therapeutic Method Against Endometrial Carcinoma Developing Bivalent Molecules Against Pathogens With Antimicrobial Resistance

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dc.contributor.advisorGilbertson, Scott R.
dc.contributor.committeeMemberDaugulis, Olafs
dc.contributor.committeeMemberHarth, Eva M.
dc.contributor.committeeMemberXu, Shoujun
dc.contributor.committeeMemberCuny, Gregory D.
dc.creatorDu, Chen
dc.date.accessioned2022-06-15T22:41:53Z
dc.date.createdDecember 2021
dc.date.issued2021-12
dc.date.submittedDecember 2021
dc.date.updated2022-06-15T22:41:54Z
dc.description.abstractDevelopment of novel therapeutics has been one of the most pivotal parts in medicinal chemistry, especially towards severe or terminal diseases. As time goes by, the research mode of interdisciplinary collaboration has greatly pushed the boundaries of new drugs, where lead compounds are identified via screening, and structure-activity relationship studies are followed up for better efficacy. Endometrial carcinoma is one of the most common cancers in the US and the world with low 5-year survival rate at its late stages. Studies of p27, a cyclin-dependent kinase inhibitor, have shown that regulating the level of p27 in the cell nucleus may serve as a new approach to treat this cancer. The lead compound was identified and synthesized with a couple of analogs. The chemistry involved and their biological activity will be discussed. Infections caused by antimicrobial resistant pathogens have been a grave threat to human health for the last few decades. Three non-antibiotic drugs, amoxapine, trifluoperazine, and doxapram, were found able to reduce the virulence in the cell upon the infection caused by various antimicrobial resistant pathogens. The synergistic effect of administering those lead drugs along with known antibiotics has been confirmed in vivo as well. Chemistry of synthesizing a bivalent molecule with one of the lead drugs attached to an antibiotic by click reaction will be discussed.
dc.description.departmentChemistry, Department of
dc.format.digitalOriginborn digital
dc.format.mimetypeapplication/pdf
dc.identifier.urihttps://hdl.handle.net/10657/9198
dc.language.isoeng
dc.rightsThe author of this work is the copyright owner. UH Libraries and the Texas Digital Library have their permission to store and provide access to this work. Further transmission, reproduction, or presentation of this work is prohibited except with permission of the author(s).
dc.subjectp27
dc.subjectubiquitination
dc.subjectquinolinone
dc.subjectantimicrobial resistance
dc.subjectbivalent molecule
dc.subjecthost directed therapeutics
dc.subjectclick reaction
dc.titleDeveloping Small Molecule Inhibitors To Restore Nuclear p27 As A Novel Therapeutic Method Against Endometrial Carcinoma Developing Bivalent Molecules Against Pathogens With Antimicrobial Resistance
dc.type.dcmiText
dc.type.genreThesis
dcterms.accessRightsThe full text of this item is not available at this time because the student has placed this item under an embargo for a period of time. The Libraries are not authorized to provide a copy of this work during the embargo period.
local.embargo.lift2023-12-01
local.embargo.terms2023-12-01
thesis.degree.collegeCollege of Natural Sciences and Mathematics
thesis.degree.departmentChemistry, Department of
thesis.degree.disciplineChemistry
thesis.degree.grantorUniversity of Houston
thesis.degree.levelDoctoral
thesis.degree.nameDoctor of Philosophy

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