Activation of the androgen receptor by intratumoral bioconversion of androstanediol to dihydrotestosterone in prostate cancer

JL Mohler, MA Titus, S Bai, BJ Kennerley, FB Lih… - Cancer research, 2011 - AACR
The androgen receptor (AR) mediates the growth of benign and malignant prostate in
response to dihydrotestosterone (DHT). In patients undergoing androgen deprivation …

Potential prostate cancer drug target: bioactivation of androstanediol by conversion to dihydrotestosterone

JL Mohler, MA Titus, EM Wilson - Clinical Cancer Research, 2011 - AACR
High-affinity binding of dihydrotestosterone (DHT) to the androgen receptor (AR) initiates
androgen-dependent gene activation, required for normal male sex development in utero …

Androgen deprivation promotes intratumoral synthesis of dihydrotestosterone from androgen metabolites in prostate cancer

F Ishizaki, T Nishiyama, T Kawasaki, Y Miyashiro… - Scientific reports, 2013 - nature.com
Intratumoral synthesis of dihydrotestosterone (DHT) from precursors cannot completely
explain the castration resistance of prostate cancer. We showed that DHT was intratumorally …

Increased expression of genes converting adrenal androgens to testosterone in androgen-independent prostate cancer

M Stanbrough, GJ Bubley, K Ross, TR Golub… - Cancer research, 2006 - AACR
Androgen receptor (AR) plays a central role in prostate cancer, and most patients respond to
androgen deprivation therapies, but they invariably relapse with a more aggressive prostate …

Androgen synthesis in prostate cancer: do all roads lead to Rome?

R Stuchbery, PJ McCoy, CM Hovens… - Nature Reviews …, 2017 - nature.com
The accumulation of high concentrations of signalling androgens within prostate tumours
that progress despite use of androgen-deprivation therapy is a clinically important …

Canonical androstenedione reduction is the predominant source of signaling androgens in hormone-refractory prostate cancer

M Fankhauser, Y Tan, G Macintyre, I Haviv… - Clinical Cancer …, 2014 - AACR
Purpose: It has been recognized for almost a decade that concentrations of signaling
androgens sufficient to activate the androgen receptor are present in castration-resistant …

Intratumoral androgen biosynthesis in prostate cancer pathogenesis and response to therapy

C Cai, SP Balk - Endocrine-related cancer, 2011 - erc.bioscientifica.com
The majority of prostate cancers (PCa) express high levels of androgen receptor (AR) and
are dependent for their growth on testosterone produced by the testes, which is reduced in …

Direct metabolic interrogation of dihydrotestosterone biosynthesis from adrenal precursors in primary prostatectomy tissues

C Dai, YM Chung, E Kovac, Z Zhu, J Li… - Clinical Cancer …, 2017 - AACR
Purpose: A major mechanism of castration-resistant prostate cancer (CRPC) involves
intratumoral biosynthesis of dihydrotestosterone (DHT) from adrenal precursors. We have …

Evidence of limited contributions for intratumoral steroidogenesis in prostate cancer

J Hofland, WM van Weerden, NFJ Dits, J Steenbergen… - Cancer research, 2010 - AACR
Androgen-deprivation therapy for prostate cancer (PC) eventually leads to castration-
resistant PC (CRPC). Intratumoral androgen production might contribute to tumor …

The androgen axis in recurrent prostate cancer

JL Mohler, CW Gregory, OH Ford III, D Kim… - Clinical cancer …, 2004 - AACR
Purpose. Prostate cancer that recurs during androgen deprivation therapy is referred to as
androgen-independent. High levels of expression of androgen receptor and androgen …