In vitro and in vivo characterisation of ASP9521: a novel, selective, orally bioavailable inhibitor of 17β-hydroxysteroid dehydrogenase type 5 (17βHSD5; AKR1C3)

Discovery of 2-methyl-1-{1-[(5-methyl-1H-indol-2-yl)carbonyl]piperidin-4-yl}propan-2-ol: A novel, potent and selective type 5 17β-hydroxysteroid dehydrogenase inhibitor

(2013) Kazushi Watanabe et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Steroidogenic Enzyme AKR1C3 Is a Novel Androgen Receptor-Selective Coactivator that Promotes Prostate Cancer Growth

(2013) M. Yepuru et al.   CLINICAL CANCER RESEARCH

AKR1C3 as a target in castrate resistant prostate cancer

(2013) Adegoke O. Adeniji et al.   JOURNAL OF STEROID BIOCHEMISTRY AND MOLECULAR BIOLOGY

Prostate cancer progression after androgen deprivation therapy: mechanisms of castrate resistance and novel therapeutic approaches

(2013) T Karantanos et al.   ONCOGENE

Characterization of Prostate Cancer Bone Metastases According to Expression Levels of Steroidogenic Enzymes and Androgen Receptor Splice Variants

(2013) Emma Jernberg et al.   PLoS One

Distinct Patterns of Dysregulated Expression of Enzymes Involved in Androgen Synthesis and Metabolism in Metastatic Prostate Cancer Tumors

(2012) N. Mitsiades et al.   CANCER RESEARCH

Overexpression of aldo-keto reductase 1C3 (AKR1C3) in LNCaP cells diverts androgen metabolism towards testosterone resulting in resistance to the 5α-reductase inhibitor finasteride

(2012) Michael C. Byrns et al.   JOURNAL OF STEROID BIOCHEMISTRY AND MOLECULAR BIOLOGY

Adaptation or selection—mechanisms of castration-resistant prostate cancer

(2012) Yang Zong et al.   Nature Reviews Urology

Discovery of substituted 3-(phenylamino)benzoic acids as potent and selective inhibitors of type 5 17β-hydroxysteroid dehydrogenase (AKR1C3)

(2011) Adegoke O. Adeniji et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Activation of the Androgen Receptor by Intratumoral Bioconversion of Androstanediol to Dihydrotestosterone in Prostate Cancer

(2011) James L. Mohler et al.   CANCER RESEARCH

Intratumoral De Novo Steroid Synthesis Activates Androgen Receptor in Castration-Resistant Prostate Cancer and Is Upregulated by Treatment with CYP17A1 Inhibitors

(2011) C. Cai et al.   CANCER RESEARCH

Resistance to CYP17A1 Inhibition with Abiraterone in Castration-Resistant Prostate Cancer: Induction of Steroidogenesis and Androgen Receptor Splice Variants

(2011) Elahe A. Mostaghel et al.   CLINICAL CANCER RESEARCH

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(2011) Minja Pfeiffer et al.   MOLECULAR MEDICINE

Blockade of testicular and adrenal androgens in prostate cancer treatment

(2011) Fernand Labrie   Nature Reviews Urology

Dihydrotestosterone synthesis bypasses testosterone to drive castration-resistant prostate cancer

(2011) K.-H. Chang et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Evidence of Limited Contributions for Intratumoral Steroidogenesis in Prostate Cancer

(2010) J. Hofland et al.   CANCER RESEARCH

Lack of functional and expression homology between human and mouse aldo-keto reductase 1C enzymes: implications for modelling human cancers

(2009) Pedro Veliça et al.   Molecular Cancer

Androgen deprivation therapy: progress in understanding mechanisms of resistance and optimizing androgen depletion

(2009) William P Harris et al.   Nature clinical practice. Urology

Maintenance of Intratumoral Androgens in Metastatic Prostate Cancer: A Mechanism for Castration-Resistant Tumor Growth

(2008) R. B. Montgomery et al.   CANCER RESEARCH

Phase I Clinical Trial of a Selective Inhibitor of CYP17, Abiraterone Acetate, Confirms That Castration-Resistant Prostate Cancer Commonly Remains Hormone Driven

(2008) Gerhardt Attard et al.   JOURNAL OF CLINICAL ONCOLOGY

Tissue Distribution of Human AKR1C3 and Rat Homolog in the Adult Genitourinary System

(2008) Joseph Azzarello et al.   JOURNAL OF HISTOCHEMISTRY & CYTOCHEMISTRY

Expression of androgen receptor through androgen-converting enzymes is associated with biological aggressiveness in prostate cancer

(2007) K Wako et al.   JOURNAL OF CLINICAL PATHOLOGY