Discovery of ARD-2585 as an Exceptionally Potent and Orally Active PROTAC Degrader of Androgen Receptor for the Treatment of Advanced Prostate Cancer

Using Biochemistry and Biophysics to Extinguish Androgen Receptor Signalling in Prostate Cancer

(2021) Irfan A. Asangani et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

An Overview of Next-Generation Androgen Receptor-Targeted Therapeutics in Development for the Treatment of Prostate Cancer

(2021) Michael L. Mohler et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

Proteolysis-Targeting Chimeras as Therapeutics and Tools for Biological Discovery

(2020) George M. Burslem et al.   CELL

First-in-human phase I study of ARV-110, an androgen receptor (AR) PROTAC degrader in patients (pts) with metastatic castrate-resistant prostate cancer (mCRPC) following enzalutamide (ENZ) and/or abiraterone (ABI).

(2020) Daniel Peter Petrylak et al.   JOURNAL OF CLINICAL ONCOLOGY

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

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

ARV-110: An oral androgen receptor PROTAC degrader for prostate cancer.

(2019) Taavi Neklesa et al.   JOURNAL OF CLINICAL ONCOLOGY

Orally Bioavailable Androgen Receptor Degrader, Potential Next-Generation Therapeutic for Enzalutamide-Resistant Prostate Cancer

(2019) Suriyan Ponnusamy et al.   CLINICAL CANCER RESEARCH

Second-Generation Antiandrogens: From Discovery to Standard of Care in Castration Resistant Prostate Cancer

(2019) Meghan A. Rice et al.   Frontiers in Oncology

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

Design, synthesis, and biological evaluation of small molecule PROTACs for potential anticancer effects

(2019) Yang Da et al.   MEDICINAL CHEMISTRY RESEARCH

Non-Steroidal Androgen Receptor Antagonists and Prostate Cancer: a Survey on Chemical Structures Binding this Fast-Mutating Target

(2018) Claudia Ferroni et al.   CURRENT MEDICINAL CHEMISTRY

New Generation of Selective Androgen Receptor Degraders: Our Initial Design, Synthesis, and Biological Evaluation of New Compounds with Enzalutamide-Resistant Prostate Cancer Activity

(2018) Dong-Jin Hwang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Beyond the Rule of 5: Lessons Learned from AbbVie’s Drugs and Compound Collection

(2017) David A. DeGoey et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

Induced protein degradation: an emerging drug discovery paradigm

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

Discovery of a novel binding pocket for CYP 2C9 inhibitors: crystallography, pharmacophore modelling and inhibitor SAR

(2016) Sarah E. Skerratt et al.   MedChemComm

Androgen Receptor Antagonists in Castration-Resistant Prostate Cancer

(2013) Dana Rathkopf et al.   CANCER JOURNAL

Discovery of Aryloxy Tetramethylcyclobutanes as Novel Androgen Receptor Antagonists

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

Non-peptidic substrate-mimetic inhibitors of Akt as potential anti-cancer agents

(2008) Katherine J. Kayser-Bricker et al.   BIOORGANIC & MEDICINAL CHEMISTRY

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

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