Discovery of A031 as effective proteolysis targeting chimera (PROTAC) androgen receptor (AR) degrader for the treatment of prostate cancer

Modeling acquired resistance to the second-generation androgen receptor antagonist enzalutamide in the TRAMP model of prostate cancer.

(2020) Marianna Cerasuolo et al.   CANCER RESEARCH

Proteolysis-Targeting Chimeras as Therapeutics and Tools for Biological Discovery

(2020) George M. Burslem et al.   CELL

Protein Engineering in the Ubiquitin System: Tools for Discovery and Beyond

(2020) Bo Zhao et al.   PHARMACOLOGICAL REVIEWS

Proteolysis-targeting chimera (PROTAC) for targeted protein degradation and cancer therapy

(2020) Xin Li et al.   Journal of Hematology & Oncology

LINC00675 activates androgen receptor axis signaling pathway to promote castration-resistant prostate cancer progression

(2020) Mengfei Yao et al.   Cell Death & Disease

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

Differential PROTAC substrate specificity dictated by orientation of recruited E3 ligase

(2019) Blake E. Smith et al.   Nature Communications

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

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

Targeting BCR-ABL1 in Chronic Myeloid Leukemia by PROTAC-mediated Targeted Protein Degradation

(2019) George M Burslem et al.   CANCER RESEARCH

Progress on small-molecule proteolysis-targeting chimeras

(2019) Wenhai Huang et al.   Future Medicinal Chemistry

Structural Dynamics of Agonist and Antagonist Binding to the Androgen Receptor

(2019) Ettayapuram Ramaprasad Azhagiya Singam et al.   JOURNAL OF PHYSICAL CHEMISTRY B

Highlights in Resistance Mechanism Pathways for Combination Therapy

(2019) Delou et al.   Cells

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

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

Androgen Receptor Signaling in the Development of Castration-Resistant Prostate Cancer

(2019) Qin Feng 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

Epidemiology of prostate cancer in Asian countries

(2018) Takahiro Kimura et al.   INTERNATIONAL JOURNAL OF UROLOGY

Androgen deprivation therapy and radiation therapy for prostate cancer: the mechanism underlying therapeutic synergy

(2018) Catherine S. Spina   Translational Cancer Research

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

(2018) Sainan An et al.   EBioMedicine

Enzalutamide-resistant castration-resistant prostate cancer: challenges and solutions

(2018) Marcello Tucci et al.   OncoTargets and Therapy

Structure of the homodimeric androgen receptor ligand-binding domain

(2017) Marta Nadal et al.   Nature Communications

Causes of death among cancer patients

(2016) NG Zaorsky et al.   ANNALS OF ONCOLOGY

The Effect of F877L and T878A Mutations on Androgen Receptor Response to Enzalutamide

(2016) Stefan Prekovic et al.   MOLECULAR CANCER THERAPEUTICS

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

Practical Guidance on the Role of Corticosteroids in the Treatment of Metastatic Castration-resistant Prostate Cancer

(2016) Maria De Santis et al.   UROLOGY

HaloPROTACS: Use of Small Molecule PROTACs to Induce Degradation of HaloTag Fusion Proteins

(2015) Dennis L. Buckley et al.   ACS Chemical Biology

Androgen receptor: structure, role in prostate cancer and drug discovery

(2014) MH Eileen Tan et al.   ACTA PHARMACOLOGICA SINICA

AR function in promoting metastatic prostate cancer

(2014) Michael A. Augello et al.   CANCER AND METASTASIS REVIEWS

Targeting tumour-supportive cellular machineries in anticancer drug development

(2014) Matthias Dobbelstein et al.   NATURE REVIEWS DRUG DISCOVERY

Can Single Positive Core Prostate Cancer at biopsy be Considered a Low-Risk Disease after Radical Prostatectomy?

(2014) Ricardo Kupka da Silva et al.   International Braz J Urol

Advances in Androgen Receptor Targeted Therapy for Prostate Cancer

(2013) Alia Ahmed et al.   JOURNAL OF CELLULAR PHYSIOLOGY

Androgen receptor functions in castration-resistant prostate cancer and mechanisms of resistance to new agents targeting the androgen axis

(2013) X Yuan et al.   ONCOGENE

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

(2013) T Karantanos et al.   ONCOGENE

Enzalutamide, an androgen receptor signaling inhibitor, induces tumor regression in a mouse model of castration-resistant prostate cancer

(2013) Javier Guerrero et al.   PROSTATE

Targeting the von Hippel–Lindau E3 Ubiquitin Ligase Using Small Molecules To Disrupt the VHL/HIF-1α Interaction

(2012) Dennis L. Buckley et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Discovery of Aryloxy Tetramethylcyclobutanes as Novel Androgen Receptor Antagonists

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

Target identification using drug affinity responsive target stability (DARTS)

(2009) B. Lomenick et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

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

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