Development of a High-Throughput Screening Assay for Small-Molecule Inhibitors of Androgen Receptor Splice Variants

Eighty Years of Targeting Androgen Receptor Activity in Prostate Cancer: The Fight Goes on

(2021) Eva Estébanez-Perpiñá et al.   Cancers

Androgen receptor splice variant 7 functions independently of the full length receptor in prostate cancer cells

(2021) Jiaqian Liang et al.   CANCER LETTERS

Diverse AR Gene Rearrangements Mediate Resistance to Androgen Receptor Inhibitors in Metastatic Prostate Cancer

(2020) Yingming Li et al.   CLINICAL CANCER RESEARCH

Discovery of drugs that directly target the intrinsically disordered region of the androgen receptor

(2020) Marianne D. Sadar   Expert Opinion on Drug Discovery

Combination therapy with androgen receptor N‐terminal domain antagonist EPI‐7170 and enzalutamide yields synergistic activity in AR‐V7‐positive prostate cancer

(2020) Yukiyoshi Hirayama et al.   Molecular Oncology

Darolutamide is a potent androgen receptor antagonist with strong efficacy in prostate cancer models

(2019) Tatsuo Sugawara et al.   INTERNATIONAL JOURNAL OF CANCER

Targeting Quorum Sensing: High-Throughput Screening to Identify Novel LsrK Inhibitors

(2019) Viviana Gatta et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

Genomic Hallmarks and Structural Variation in Metastatic Prostate Cancer

(2018) David A. Quigley et al.   CELL

Androgen receptor splice variant-7 expression emerges with castration resistance in prostate cancer

(2018) Adam Sharp et al.   JOURNAL OF CLINICAL INVESTIGATION

Comprehensive Profiling of the Androgen Receptor in Liquid Biopsies from Castration-resistant Prostate Cancer Reveals Novel Intra-AR Structural Variation and Splice Variant Expression Patterns

(2017) Bram De Laere et al.   EUROPEAN UROLOGY

In Vitro Assay Development and HTS of Small-Molecule Human ABAD/17β-HSD10 Inhibitors as Therapeutics in Alzheimer’s Disease

(2017) Laura Aitken et al.   SLAS Discovery

EPI-001, A Compound Active against Castration-Resistant Prostate Cancer, Targets Transactivation Unit 5 of the Androgen Receptor

(2016) Eva De Mol et al.   ACS Chemical Biology

A sting in the tail: the N-terminal domain of the androgen receptor as a drug target

(2016) IainJ McEwan et al.   ASIAN JOURNAL OF ANDROLOGY

Targeting Androgen Receptor Activation Function-1 with EPI to Overcome Resistance Mechanisms in Castration-Resistant Prostate Cancer

(2016) Y. C. Yang et al.   CLINICAL CANCER RESEARCH

European Lead Factory hits its stride

(2016) Katie Kingwell   NATURE REVIEWS DRUG DISCOVERY

Drug discovery in advanced prostate cancer: translating biology into therapy

(2016) Timothy A. Yap et al.   NATURE REVIEWS DRUG DISCOVERY

Management of castrate-resistant prostate cancer in older men

(2016) Yasser Ged et al.   Journal of Geriatric Oncology

Androgen Receptor Splice Variants Dimerize to Transactivate Target Genes

(2015) D. Xu et al.   CANCER RESEARCH

AR splice variant dimerization—clinical implications

(2015) Emmanuel S. Antonarakis et al.   Nature Reviews Urology

Are androgen receptor variants a substitute for the full-length receptor?

(2015) Ji Lu et al.   Nature Reviews Urology

EPI-001 is a selective peroxisome proliferator-activated receptor-gamma modulator with inhibitory effects on androgen receptor expression and activity in prostate cancer

(2015) Lucas J. Brand et al.   Oncotarget

FOXA1 regulates androgen receptor variant activity in models of castrate-resistant prostate cancer

(2015) Dominic Jones et al.   Oncotarget

Androgen receptor and its splice variant, AR-V7, differentially regulate FOXA1 sensitive genes in LNCaP prostate cancer cells

(2014) William C. Krause et al.   INTERNATIONAL JOURNAL OF BIOCHEMISTRY & CELL BIOLOGY

AR-V7 and Resistance to Enzalutamide and Abiraterone in Prostate Cancer

(2014) Emmanuel S. Antonarakis et al.   NEW ENGLAND JOURNAL OF MEDICINE

Endocrine therapy in prostate cancer: time for reappraisal of risks, benefits and cost-effectiveness?

(2013) L Bourke et al.   BRITISH JOURNAL OF CANCER

An androgen receptor N-terminal domain antagonist for treating prostate cancer

(2013) Jae-Kyung Myung et al.   JOURNAL OF CLINICAL INVESTIGATION

A Lack of Premature Termination Codon Read-Through Efficacy of PTC124 (Ataluren) in a Diverse Array of Reporter Assays

(2013) Stuart P. McElroy et al.   PLOS BIOLOGY

Firefly Luciferase in Chemical Biology: A Compendium of Inhibitors, Mechanistic Evaluation of Chemotypes, and Suggested Use As a Reporter

(2012) Natasha Thorne et al.   CHEMISTRY & BIOLOGY

Nanosponge-encapsulated camptothecin exerts anti-tumor activity in human prostate cancer cells

(2012) Rosalba Minelli et al.   EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES

The Impact of Point Mutations in the Human Androgen Receptor: Classification of Mutations on the Basis of Transcriptional Activity

(2012) Colin W. Hay et al.   PLoS One

Alternatively spliced androgen receptor variants

(2011) Scott M Dehm et al.   ENDOCRINE-RELATED CANCER

Intrinsic disorder in the androgen receptor: identification, characterisation and drugability

(2011) Iain J. McEwan   Molecular BioSystems

Camptothecin disrupts androgen receptor signaling and suppresses prostate cancer cell growth

(2010) Shicheng Liu et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

Regression of Castrate-Recurrent Prostate Cancer by a Small-Molecule Inhibitor of the Amino-Terminus Domain of the Androgen Receptor

(2010) Raymond J. Andersen et al.   CANCER CELL

Molecular basis for the high-affinity binding and stabilization of firefly luciferase by PTC124

(2010) D. S. Auld et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Statins reduce the androgen sensitivity and cell proliferation by decreasing the androgen receptor protein in prostate cancer cells

(2010) Akira Yokomizo et al.   PROSTATE

A Cellular Conformation-Based Screen for Androgen Receptor Inhibitors

(2008) Jeremy O. Jones et al.   ACS Chemical Biology

Regulation of androgen receptor transcriptional activity by rapamycin in prostate cancer cell proliferation and survival

(2008) Y Wang et al.   ONCOGENE

Statins and prostate cancer prevention: where we are now and future directions

(2008) Teemu J Murtola et al.   Nature clinical practice. Urology