Year of Award
2019
Document Type
Thesis
Degree Type
Master of Science (MS)
Degree Name
Pharmaceutical Sciences
Department or School/College
Biomedical and Pharmaceutical Sciences
Committee Chair
Dr. Travis Hughes
Committee Co-chair
Dr. Philippe Diaz
Commitee Members
Dr. Nigel Priestley, Dr. Keith Parker
Keywords
PPAR, nTZDpa, NMP422, biased agonism
Subject Categories
Biochemistry | Biophysics | Medicinal-Pharmaceutical Chemistry | Organic Chemistry | Structural Biology
Abstract
Peroxisome proliferator-activated receptor gamma (PPARγ) has been a drug target to treat type 2 diabetes for the last 20 years when rosiglitazone and pioglitazone were approved by the FDA in 1999. While effective at increasing insulin sensitivity, these drugs cause serious adverse effects due to their full agonist characteristics. For that reason, drug discovery efforts have attempted to reduce or prevent the amount of agonist character of new PPARγ targeting ligands. Unfortunately, there have been no new FDA approved drugs for the receptor. There is a need for new ideas to produce better quality pharmaceuticals that lessen the impact of adverse effects. This work aims to propose and expand on new ideas: biased agonism and interactions that anchor a consistent binding mode.
Recommended Citation
Patton, Trey M., "Avoiding Adverse Effects: New Ideas in Drug Discovery for Targeting PPARγ" (2019). Graduate Student Theses, Dissertations, & Professional Papers. 11416.
https://scholarworks.umt.edu/etd/11416
Included in
Biochemistry Commons, Biophysics Commons, Medicinal-Pharmaceutical Chemistry Commons, Organic Chemistry Commons, Structural Biology Commons
© Copyright 2019 Trey M. Patton