Studies on Regulation of Dihydrotestosterone Binding to and Releasing from the Androgen Receptor

Author

Tahyra M. Resto Santos, The University of Texas Rio Grande ValleyFollow

Date of Award

5-2019

Document Type

Thesis

Degree Name

Master of Science (MS)

Department

Chemistry

First Advisor

Dr. Frank Dean

Second Advisor

Dr. Evangelia Kotsikorou

Third Advisor

Dr. James Bullard

Abstract

The androgen receptor (AR) is a nuclear receptor that responds to testosterone and 5α-dihydrotestosterone (DHT) by modulating gene expression in a variety of cells, including prostate and muscle tissues. Studies of small molecule interaction with AR have shown diphenyl compounds inhibiting through a binding site labeled Binding Function 3 (BF3). The goal of this research is to analyze the interaction of the BF3 site with DDT and related compounds. Amino acids that are exposed on the surface of the BF3 that might interact with different compounds were mutated. Mutant proteins were tested experimentally for their impact on the inhibition the AR. Results show that mutations in F673, G724, and L830 prevent the inhibition of DDE, suggesting that DDE and related compounds act by interacting at the BF3 site of the AR. Understanding how the BF3 site binds with these compounds may lead to the development of new anticancer medications.

Comments

Copyright 2019 Tahyra M. Resto Santos. All Rights Reserved.

https://go.openathens.net/redirector/utrgv.edu?url=https://www.proquest.com/dissertations-theses/studies-on-regulation-dihydrotestosterone-binding/docview/2245807823/se-2?accountid=7119

Recommended Citation

Resto Santos, Tahyra M., "Studies on Regulation of Dihydrotestosterone Binding to and Releasing from the Androgen Receptor" (2019). Theses and Dissertations. 329.
https://scholarworks.utrgv.edu/etd/329