Graduation Year
2018
Document Type
Dissertation
Degree
Ph.D.
Degree Name
Doctor of Philosophy (Ph.D.)
Degree Granting Department
Chemistry
Major Professor
Jianfeng Cai, Ph.D.
Committee Member
Kirpal Bisht, Ph.D.
Committee Member
Shengqian Ma, Ph.D.
Committee Member
Xingmin Sun, Ph.D.
Keywords
γ-AApeptide, antimicrobial agents, OBTC library, drug resistance
Abstract
Peptidomimetics can mimic hierarchical structures of peptides and proteins. Thus, they are extensively studied for therapeutic applications. To break the limitation of backbones and frameworks and expand the peptidomimetics family, a new class of peptidomimetics - “γ-AApeptides” was developed. Design of γ-AApeptides is based on the chiral peptide nucleic acids (PNAs) backbone.
The World Health Organization estimates that one -third of all deaths in the world are on account of infectious diseases. AMPs are important because of their high activity against broad spectrum microbes, less susceptible to grow resistance and selectivity in binding to bacterial cells over human cells. γ-AApeptides as a new class of peptidomimetics have increased stability and enhanced chemical diversity. We have developed polymyxin mimic cyclic peptides, small linear molecules and hydantoin derivatives as potent antibiotic agents with γ-AApeptides. They have good bioactivity and selectivity.
Combinatorial library is key technology for accelerating the discovery of novel therapeutic agents. One-bead-two-compound γ-AApeptides-based library was developed and screened against SMYD2 protein which is essential for tumor growing.
Scholar Commons Citation
Su, Ma, "Structure-based Design, Synthesis and Applications of a New Class of Peptidomimetics: 'Y-AA Peptides and Their Derivatives" (2018). USF Tampa Graduate Theses and Dissertations.
https://digitalcommons.usf.edu/etd/7580
