4.7 Review

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

Related references

Note: Only part of the references are listed.
Article Chemistry, Medicinal

Discovery of JNJ-63576253: A Clinical Stage Androgen Receptor Antagonist for F877L Mutant and Wild-Type Castration-Resistant Prostate Cancer (mCRPC)

Zhuming Zhang et al.

Summary: Persistent activation of androgen receptor (AR) contributes to resistance to second-generation AR pathway inhibitors in advanced prostate cancer. The AR F877L mutation confers resistance to enzalutamide and apalutamide, but compound 4 (JNJ-pan-AR) has been identified as a potent pan-AR antagonist against this mutation. Lead optimization resulted in the nomination of 5 (JNJ-63576253) as a next-generation AR antagonist for the treatment of castration-resistant prostate cancer (CRPC).

JOURNAL OF MEDICINAL CHEMISTRY (2021)

Article Plant Sciences

Structure-Activity Relationships for the Marine Natural Product Sintokamides: Androgen Receptor N-Terminus Antagonists of Interest for Treatment of Metastatic Castration-Resistant Prostate Cancer

Luping Yan et al.

Summary: Synthetic analogues of the marine natural product sintokamides have been prepared to investigate the structure-activity relationships for the androgen receptor N-terminal domain antagonist activity. The data indicate the essentiality of chlorine atoms on leucine side chains for potency, and some analogues are even more active than natural products. Specific R configurations and N-terminus caps play a role in enhancing potency, while the tetramic acid fragment and methyl ether are crucial for activity.

JOURNAL OF NATURAL PRODUCTS (2021)

Article Oncology

Cancer statistics, 2020

Rebecca L. Siegel et al.

CA-A CANCER JOURNAL FOR CLINICIANS (2020)

Article Biochemistry & Molecular Biology

New steroidal oxazolines, benzoxazoles and benzimidazoles related to abiraterone and galeterone

Alexandra S. Latysheva et al.

STEROIDS (2020)

Article Biochemistry & Molecular Biology

The splicing modulator sulfonamide indisulam reduces AR-V7 in prostate cancer cells

James E. Melnyk et al.

BIOORGANIC & MEDICINAL CHEMISTRY (2020)

Article Chemistry, Medicinal

Systematic Investigation of the Permeability of Androgen Receptor PROTACs

Duncan E. Scott et al.

ACS MEDICINAL CHEMISTRY LETTERS (2020)

Review Biochemistry & Molecular Biology

The Androgen Receptor in Prostate Cancer: Effect of Structure, Ligands and Spliced Variants on Therapy

Elisabeth A. Messner et al.

BIOMEDICINES (2020)

Review Chemistry, Medicinal

Androgen receptor modulators: a review of recent patents and reports (2012-2018)

Shinya Fujii et al.

EXPERT OPINION ON THERAPEUTIC PATENTS (2019)

Review Cell Biology

Targeting Nuclear Receptors with PROTAC degraders

John J. Flanagan et al.

MOLECULAR AND CELLULAR ENDOCRINOLOGY (2019)

Review Chemistry, Multidisciplinary

Androgen Receptor-Directed Molecular Conjugates for Targeting Prostate Cancer

Giovanni L. Beretta et al.

FRONTIERS IN CHEMISTRY (2019)

Review Urology & Nephrology

Selective Androgen Receptor Modulators: Current Knowledge and Clinical Applications

Zachary J. Solomon et al.

SEXUAL MEDICINE REVIEWS (2019)

Article Biochemistry & Molecular Biology

Selective modulation of the androgen receptor AF2 domain rescues degeneration in spinal bulbar muscular atrophy

Nisha M. Badders et al.

NATURE MEDICINE (2018)

Review Oncology

Degradation of Androgen Receptor through Small Molecules for Prostate Cancer

Raoling Ge et al.

CURRENT CANCER DRUG TARGETS (2018)

Article Pharmacology & Pharmacy

Structural Based Screening of Antiandrogen Targeting Activation Function-2 Binding Site

Yangguang Liu et al.

FRONTIERS IN PHARMACOLOGY (2018)

Article Multidisciplinary Sciences

Structure of the homodimeric androgen receptor ligand-binding domain

Marta Nadal et al.

NATURE COMMUNICATIONS (2017)

Article Biochemistry & Molecular Biology

Steroidogenic Metabolism of Galeterone Reveals a Diversity of Biochemical Activities

Mohammad Alyamani et al.

CELL CHEMICAL BIOLOGY (2017)

Article Chemistry, Medicinal

Practical synthesis of a phthalimide-based Cereblon ligand to enable PROTAC development

Jasmin Lohbeck et al.

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2016)

Article Biochemistry & Molecular Biology

Sintokamide A Is a Novel Antagonist of Androgen Receptor That Uniquely Binds Activation Function-1 in Its Amino-terminal Domain

Carmen A. Banuelos et al.

JOURNAL OF BIOLOGICAL CHEMISTRY (2016)

Review Urology & Nephrology

Role of androgen receptor splice variants in prostate cancer metastasis

Jin Xu et al.

ASIAN JOURNAL OF UROLOGY (2016)

Article Chemistry, Medicinal

Discovery and Development of Galeterone (TOK-001 or VN/124-1) for the Treatment of All Stages of Prostate Cancer

Vincent C. O. Njar et al.

JOURNAL OF MEDICINAL CHEMISTRY (2015)

Article Biochemistry & Molecular Biology

Interaction mechanism exploration of R-bicalutamide/S-1 with WT/W741L AR using molecular dynamics simulations

Hongli Liu et al.

MOLECULAR BIOSYSTEMS (2015)

Article Pathology

Proposed Morphologic Classification of Prostate Cancer With Neuroendocrine Differentiation

Jonathan I. Epstein et al.

AMERICAN JOURNAL OF SURGICAL PATHOLOGY (2014)

Article Biochemistry & Molecular Biology

Selectively Targeting the DNA-binding Domain of the Androgen Receptor as a Prospective Therapy for Prostate Cancer

Kush Dalal et al.

JOURNAL OF BIOLOGICAL CHEMISTRY (2014)

Article Multidisciplinary Sciences

Characterization of Niphatenones that Inhibit Androgen Receptor N-Terminal Domain

Carmen A. Banuelos et al.

PLOS ONE (2014)

Article Pharmacology & Pharmacy

Androgen Receptor Gene Rearrangements: New Perspectives on Prostate Cancer Progression

Lucas J. Brand et al.

CURRENT DRUG TARGETS (2013)

Article Medicine, Research & Experimental

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

Jae-Kyung Myung et al.

JOURNAL OF CLINICAL INVESTIGATION (2013)

Review Cell Biology

Recent developments in antiandrogens and selective androgen receptor modulators

Bernard Haendler et al.

MOLECULAR AND CELLULAR ENDOCRINOLOGY (2012)

Review Biochemistry & Molecular Biology

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

Iain J. McEwan

MOLECULAR BIOSYSTEMS (2012)

Article Chemistry, Medicinal

Discovery of Aryloxy Tetramethylcyclobutanes as Novel Androgen Receptor Antagonists

Chuangxing Guo et al.

JOURNAL OF MEDICINAL CHEMISTRY (2011)

Article Chemistry, Medicinal

Targeting the Binding Function 3 (BF3) Site of the Human Androgen Receptor through Virtual Screening

Nathan A. Lack et al.

JOURNAL OF MEDICINAL CHEMISTRY (2011)

Article Oncology

Integrative Genomic Profiling of Human Prostate Cancer

Barry S. Taylor et al.

CANCER CELL (2010)

Article Chemistry, Medicinal

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

Ashley R. Schneekloth et al.

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2008)

Article Biochemistry & Molecular Biology

Structural basis for accommodation of nonsteroidal ligands in the androgen receptor

CE Bohl et al.

JOURNAL OF BIOLOGICAL CHEMISTRY (2005)

Article Pharmacology & Pharmacy

Pharmacodynamics of selective androgen receptor modulators

DH Yin et al.

JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS (2003)

Article Multidisciplinary Sciences

Protacs: Chimeric molecules that target proteins to the Skp1-Cullin-F box complex for ubiquitination and degradation

KM Sakamoto et al.

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2001)

Article Multidisciplinary Sciences

Crystallographic structures of the ligand-binding domains of the androgen receptor and its T877A mutant complexed with the natural agonist dihydrotestosterone

JS Sack et al.

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2001)