Year of Award
Master of Science (MS)
Department or School/College
Biomedical and Pharmaceutical Sciences
Dr. Travis Hughes
Dr. Philippe Diaz
Dr. Nigel Priestley, Dr. Keith Parker
PPAR, nTZDpa, NMP422, biased agonism
University of Montana
Biochemistry | Biophysics | Medicinal-Pharmaceutical Chemistry | Organic Chemistry | Structural Biology
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.
Patton, Trey M., "Avoiding Adverse Effects: New Ideas in Drug Discovery for Targeting PPARγ" (2019). Graduate Student Theses, Dissertations, & Professional Papers. 11416.
© Copyright 2019 Trey M. Patton