Inhibitors Of The N-Terminal Domain Of The Androgen Receptor

Dr. Matthew Rettig, Medical Director of the Prostate Cancer Program of the Institute of Urologic Oncology, and Dr. Michael Jung from the Department of Chemistry & Biochemistry have synthesized novel inhibitors targeting the N-terminal domain of the…

Dr. Matthew Rettig, Medical Director of the Prostate Cancer Program of the Institute of Urologic Oncology, and Dr. Michael Jung from the Department of Chemistry & Biochemistry have synthesized novel inhibitors targeting the N-terminal domain of the androgen receptor. These compounds have anticancer activity in castration-resistant prostate cancer (CRPC) cell lines, showing improved activity compared to current CRPC therapeutics. The lead compound also inhibits prostate cancer cell lines containing the most common splice variants found in CRPC, specifically AR-V7 and AR-V567.

Abstract

UCLA researchers under the guidance of Drs. Matthew Rettig and Mike Jung have developed a novel family of therapeutics for use against castration-resistant prostate cancer. These drugs have been shown to inhibit the androgen receptor and are unaffected by the most common drug-resistant mutations found in prostate cancer patients.

Website

https://techtransfer.universityofcalifornia.edu/NCD/27417.html?utm_source=AUTMGTP&utm_medium=webpage&utm_term=ncdid_27417&utm_campaign=TechWebsites

Advantages

  • Inhibits wild-type and splice variant androgen receptor
  • Does not inhibit the transcriptional activity of glucocorticoid receptor
  • Inhibits growth in vitro in a dose-dependent fashion
  • Better inhibition compared to currently approved therapies in a reporter assay

Potential Applications

  • Use as therapeutic treatment for castration-resistant prostate cancer
  • Use as therapeutic treatment for drug-resistant castration-resistant prostate cancer

Contact Information

Name: UCLA Technology Development Group

Email: ncd@tdg.ucla.edu

Phone: 310.794.0558