Strategies toward Discovery of Potent and Orally Bioavailable Proteolysis Targeting Chimera Degraders of Androgen Receptor for the Treatment of Prostate Cancer

Androgen receptor degraders overcome common resistance mechanisms developed during prostate cancer treatment

(2020) Steven Kregel et al.   NEOPLASIA

Enzalutamide and Survival in Nonmetastatic, Castration-Resistant Prostate Cancer

(2020) Cora N. Sternberg et al.   NEW ENGLAND JOURNAL OF MEDICINE

Preclinical Study Using ABT263 to Increase Enzalutamide Sensitivity to Suppress Prostate Cancer Progression Via Targeting BCL2/ROS/USP26 Axis Through Altering ARv7 Protein Degradation

(2020) Hua Xu et al.   Cancers

Systematic Investigation of the Permeability of Androgen Receptor PROTACs

(2020) Duncan E. Scott et al.   ACS Medicinal Chemistry Letters

A highly potent PROTAC androgen receptor (AR) degrader ARD-61 effectively inhibits AR-positive breast cancer cell growth in vitro and tumor growth in vivo

(2020) Lijie Zhao et al.   NEOPLASIA

Design and characterization of cereblon-mediated androgen receptor proteolysis-targeting chimeras

(2020) Akshay D. Takwale et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

The PROTAC technology in drug development

(2019) Yutian Zou et al.   CELL BIOCHEMISTRY AND FUNCTION

Discovery of ERD-308 as a Highly Potent Proteolysis Targeting Chimera (PROTAC) Degrader of Estrogen Receptor (ER)

(2019) Jiantao Hu et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of ARD-69 as a Highly Potent Proteolysis Targeting Chimera (PROTAC) Degrader of Androgen Receptor (AR) for the Treatment of Prostate Cancer

(2019) Xin Han et al.   JOURNAL OF MEDICINAL CHEMISTRY

Treatment of Prostate Cancers and Kennedy’s Disease by PROTAC-Androgen Receptor Degradation

(2019) Robert B. Kargbo   ACS Medicinal Chemistry Letters

Discovery and biological evaluation of novel androgen receptor antagonist for castration-resistant prostate cancer

(2019) Jiang Yu et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

A Potent and Selective Small-Molecule Degrader of STAT3 Achieves Complete Tumor Regression In Vivo

(2019) Longchuan Bai et al.   CANCER CELL

Discovery of Highly Potent and Efficient PROTAC Degraders of Androgen Receptor (AR) by Employing Weak Binding Affinity VHL E3 Ligase Ligands

(2019) Xin Han et al.   JOURNAL OF MEDICINAL CHEMISTRY

A selective BCL-XL PROTAC degrader achieves safe and potent antitumor activity

(2019) Sajid Khan et al.   NATURE MEDICINE

PROTACs: An Emerging Targeting Technique for Protein Degradation in Drug Discovery

(2018) Shanshan Gu et al.   BIOESSAYS

Discovery of QCA570 as an Exceptionally Potent and Efficacious Proteolysis Targeting Chimera (PROTAC) Degrader of the Bromodomain and Extra-Terminal (BET) Proteins Capable of Inducing Complete and Durable Tumor Regression

(2018) Chong Qin et al.   JOURNAL OF MEDICINAL CHEMISTRY

Small-molecule PROTACs: An emerging and promising approach for the development of targeted therapy drugs

(2018) Sainan An et al.   EBioMedicine

Discovery of MD-224 as a First-in-Class, Highly Potent, and Efficacious Proteolysis Targeting Chimera Murine Double Minute 2 Degrader Capable of Achieving Complete and Durable Tumor Regression

(2018) Yangbing Li et al.   JOURNAL OF MEDICINAL CHEMISTRY

Enhancing Antiproliferative Activity and Selectivity of a FLT-3 Inhibitor by Proteolysis Targeting Chimera Conversion

(2018) George M. Burslem et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Addressing Kinase-Independent Functions of Fak via PROTAC-Mediated Degradation

(2018) Philipp M. Cromm et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Development of Protein Degradation Inducers of Androgen Receptor by Conjugation of Androgen Receptor Ligands and Inhibitor of Apoptosis Protein Ligands

(2017) Norihito Shibata et al.   JOURNAL OF MEDICINAL CHEMISTRY

Protac-Induced Protein Degradation in Drug Discovery: Breaking the Rules or Just Making New Ones?

(2017) Ian Churcher   JOURNAL OF MEDICINAL CHEMISTRY

Protein Degradation via CRL4CRBN Ubiquitin Ligase: Discovery and Structure–Activity Relationships of Novel Glutarimide Analogs That Promote Degradation of Aiolos and/or GSPT1

(2017) Joshua D. Hansen et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of a Small-Molecule Degrader of Bromodomain and Extra-Terminal (BET) Proteins with Picomolar Cellular Potencies and Capable of Achieving Tumor Regression

(2017) Bing Zhou et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structural basis of PROTAC cooperative recognition for selective protein degradation

(2017) Morgan S Gadd et al.   Nature Chemical Biology

Small-Molecule PROTACS: New Approaches to Protein Degradation

(2016) Momar Toure et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Protein Knockdown Technology: Application of Ubiquitin Ligase to Cancer Therapy

(2016) Nobumichi Ohoka et al.   CURRENT CANCER DRUG TARGETS

Induced protein degradation: an emerging drug discovery paradigm

(2016) Ashton C. Lai et al.   NATURE REVIEWS DRUG DISCOVERY

10-Year Outcomes after Monitoring, Surgery, or Radiotherapy for Localized Prostate Cancer

(2016) Freddie C. Hamdy et al.   NEW ENGLAND JOURNAL OF MEDICINE

PROTAC-induced BET protein degradation as a therapy for castration-resistant prostate cancer

(2016) Kanak Raina et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4

(2015) Jing Lu et al.   CHEMISTRY & BIOLOGY

Catalytic in vivo protein knockdown by small-molecule PROTACs

(2015) Daniel P Bondeson et al.   Nature Chemical Biology

Phthalimide conjugation as a strategy for in vivo target protein degradation

(2015) G. E. Winter et al.   SCIENCE

Enzalutamide for the treatment of metastatic castration-resistant prostate cancer

(2015) Alejo Rodriguez-Vida et al.   Drug Design Development and Therapy

Discovery of ODM-201, a new-generation androgen receptor inhibitor targeting resistance mechanisms to androgen signaling-directed prostate cancer therapies

(2015) Anu-Maarit Moilanen et al.   Scientific Reports

Identification of a Potent Antiandrogen that Targets the BF3 Site of the Androgen Receptor and Inhibits Enzalutamide-Resistant Prostate Cancer

(2014) Ravi S.N. Munuganti et al.   CHEMISTRY & BIOLOGY

A New Avenue toward Androgen Receptor Pan-antagonists: C2 Sterically Hindered Substitution of Hydroxy-propanamides

(2014) Andrea Guerrini et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

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

Novel therapeutic approaches for the treatment of castration-resistant prostate cancer

(2013) Isabel Heidegger 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

Overcoming mutation-based resistance to antiandrogens with rational drug design

(2013) Minna D Balbas et al.   eLife

ARN-509: A Novel Antiandrogen for Prostate Cancer Treatment

(2012) N. J. Clegg et al.   CANCER RESEARCH

Design, synthesis and biological evaluation of nuclear receptor-degradation inducers

(2011) Yukihiro Itoh et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Discovery of Aryloxy Tetramethylcyclobutanes as Novel Androgen Receptor Antagonists

(2011) Chuangxing Guo et al.   JOURNAL OF MEDICINAL CHEMISTRY

Development of a Second-Generation Antiandrogen for Treatment of Advanced Prostate Cancer

(2009) C. Tran et al.   SCIENCE

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

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

Targeted intracellular protein degradation induced by a small molecule: En route to chemical proteomics

(2008) Ashley R. Schneekloth et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Targeting steroid hormone receptors for ubiquitination and degradation in breast and prostate cancer

(2008) A Rodriguez-Gonzalez et al.   ONCOGENE