Accession Number : AD1022062

Title :   Development of a New Class of Drugs To Inhibit All Forms of Androgen Receptor in Castration Resistant Prostate Cancers

Descriptive Note : Technical Report,30 Sep 2015,29 Sep 2016

Corporate Author : University of Minnesota Minneapolis United States

Personal Author(s) : Dehm,Scott ; Rennie,Paul ; Gewirth,Daniel

Full Text :

Report Date : 01 Oct 2016

Pagination or Media Count : 16

Abstract : Prostate cancer is the most frequently diagnosed male cancer and second leading cause of male cancer death. Management of patients with advanced-stage disease relies on inhibiting the androgen receptor (AR) with conventional endocrine targeting therapies, and more recently with second-generation endocrine targeting therapies designed to block AR activity that re-emerges during castration. However, despite a growing armamentarium of drugs targeting the androgen/AR signaling axis, progression of castration-resistant prostate cancer (CRPC) remains a major clinical challenge that undermines survival and quality of life for prostate cancer patients. The proposed research is focused on the pre-clinical development of VPC14228, a drug-like small molecule that targets the AR:DNA interaction. During the first year of this award, we have made progress in investigating the functional effects of VPC14228 on DNA interaction and transcriptional activation mechanisms for AR, developing a definitive experimental and structural characterization of the VPC14228 interaction with the AR DBD, and conducting pre-clinical evaluation of VPC14228.

Descriptors :   prostate cancer , therapeutics , neoplasms , TARGETING , drug therapy , inhibitors , inhibition , xray crystallography , targets , mutations , drug resistance , cell line

Distribution Statement : APPROVED FOR PUBLIC RELEASE