Graduation Year
2021
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
James Leahy, Ph.D.
Committee Member
Kirpal Bisht, Ph.D.
Committee Member
Feng Cheng, Ph.D.
Keywords
antimicrobial agents, drug resistance, OBTC library, helix mimics
Abstract
Peptidomimetics are small protein like chains which can mimic primary, secondary or eventertiary structures of peptides. They have been attracting more and more attention because of their special advantages, such as high tolerance to proteolytic degradation and thousands of chemical diversities. γ-AApeptides were developed by our group as a kind of peptidomimetics that represent γ-substituted-N-acylated-N-aminoethyl amino acids. Many biological functions of γ-AApeptides have already been discovered. To expand the potential application of γ-AApeptides, I designed and synthesized three series of antimicrobial derivatives with broad-spectrum of antibacterial activity. A one-bead-two-compound thioether bridged macrocyclic γ-AApeptides library was built and screened against NRF2 protein. Moreover, γ-AApeptides sequences mimicking MLL and c-Myb protein were designed and synthesized to inhibit their protein-protein interaction with KIX domain.
Scholar Commons Citation
Wang, Minghui, "The Development of Bioactive Peptidomimetics Based on γ-AApeptides" (2021). USF Tampa Graduate Theses and Dissertations.
https://digitalcommons.usf.edu/etd/9729
