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

Intrinsic cell-penetrating activity propels Omomyc from proof of concept to viable anti-MYC therapy

(2019) Marie-Eve Beaulieu et al.   Science Translational Medicine

Prospective Multicenter Validation of Androgen Receptor Splice Variant 7 and Hormone Therapy Resistance in High-Risk Castration-Resistant Prostate Cancer: The PROPHECY Study

(2019) Andrew J. Armstrong et al.   JOURNAL OF CLINICAL ONCOLOGY

Side chain to main chain hydrogen bonds stabilize a polyglutamine helix in a transcription factor

(2019) Albert Escobedo et al.   Nature Communications

Omomyc reveals new mechanisms to inhibit the MYC oncogene

(2019) Mark J. Demma et al.   MOLECULAR AND CELLULAR BIOLOGY

Hsp70 and Hsp40 inhibit an inter-domain interaction necessary for transcriptional activity in the androgen receptor

(2019) Bahareh Eftekharzadeh et al.   Nature Communications

Targeting the Hsp40/Hsp70 Chaperone Axis as a Novel Strategy to Treat Castration-Resistant Prostate Cancer

(2018) Michael A. Moses et al.   CANCER RESEARCH

Targeting Intrinsically Disordered Transcription Factors: Changing the Paradigm

(2018) K. Tsafou et al.   JOURNAL OF MOLECULAR BIOLOGY

IUPred2A: context-dependent prediction of protein disorder as a function of redox state and protein binding

(2018) Bálint Mészáros et al.   NUCLEIC ACIDS RESEARCH

Order within a Disordered Structure

(2018) Amy H. Tien et al.   STRUCTURE

Regulation of Androgen Receptor Activity by Transient Interactions of Its Transactivation Domain with General Transcription Regulators

(2018) Eva De Mol et al.   STRUCTURE

Assessment of the Validity of Nuclear-Localized Androgen Receptor Splice Variant 7 in Circulating Tumor Cells as a Predictive Biomarker for Castration-Resistant Prostate Cancer

(2018) Howard I. Scher et al.   JAMA Oncology

Targeting intrinsically disordered proteins at the edge of chaos

(2018) Hao Ruan et al.   DRUG DISCOVERY TODAY

Hsp70 Binds to the Androgen Receptor N-terminal Domain and Modulates the Receptor Function in Prostate Cancer Cells

(2018) Jun Dong et al.   MOLECULAR CANCER THERAPEUTICS

Proteostasis by STUB1/HSP70 complex controls sensitivity to androgen receptor targeted therapy in advanced prostate cancer

(2018) Chengfei Liu et al.   Nature Communications

Elucidating binding mechanisms and dynamics of intrinsically disordered protein complexes using NMR spectroscopy

(2018) Robert Schneider et al.   CURRENT OPINION IN STRUCTURAL BIOLOGY

Determination of protein structural ensembles using cryo-electron microscopy

(2018) Massimiliano Bonomi et al.   CURRENT OPINION IN STRUCTURAL BIOLOGY

Development of cell-penetrating bispecific antibodies targeting the N-terminal domain of androgen receptor for prostate cancer therapy†

(2017) Nancy L Goicochea et al.   PROTEIN ENGINEERING DESIGN & SELECTION

Targeting the MDM2–p53 Protein–Protein Interaction for New Cancer Therapy: Progress and Challenges

(2017) Shaomeng Wang et al.   Cold Spring Harbor Perspectives in Medicine

Inhibition of androgen receptor by decoy molecules delays progression to castration-recurrent prostate cancer

(2017) Jae-Kyung Myung et al.   PLoS One

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

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

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

(2016) Carmen A. Banuelos et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Molecular recognition features (MoRFs) in three domains of life

(2016) Jing Yan et al.   Molecular BioSystems

OmoMYC blunts promoter invasion by oncogenic MYC to inhibit gene expression characteristic of MYC-dependent tumors

(2016) L A Jung et al.   ONCOGENE

Association of AR-V7 on Circulating Tumor Cells as a Treatment-Specific Biomarker With Outcomes and Survival in Castration-Resistant Prostate Cancer

(2016) Howard I. Scher et al.   JAMA Oncology

Structure-based Inhibitor Design for the Intrinsically Disordered Protein c-Myc

(2016) Chen Yu et al.   Scientific Reports

Targeting intrinsically disordered proteins in rational drug discovery

(2015) Susmitha Ambadipudi et al.   Expert Opinion on Drug Discovery

Binding cavities and druggability of intrinsically disordered proteins

(2015) Yugang Zhang et al.   PROTEIN SCIENCE

Association Between Foldability and Aggregation Propensity in Small Disulfide-Rich Proteins

(2014) Hugo Fraga et al.   ANTIOXIDANTS & REDOX SIGNALING

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

(2014) Kush Dalal et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Therapeutic targeting of BET bromodomain proteins in castration-resistant prostate cancer

(2014) Irfan A. Asangani et al.   NATURE

Targeting the disordered C terminus of PTP1B with an allosteric inhibitor

(2014) Navasona Krishnan et al.   Nature Chemical Biology

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

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

Characterization of Niphatenones that Inhibit Androgen Receptor N-Terminal Domain

(2014) Carmen A. Banuelos et al.   PLoS One

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

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

Widespread Occurrence and Distribution of Bisphenol A Diglycidyl Ether (BADGE) and its Derivatives in Human Urine from the United States and China

(2012) Lei Wang et al.   ENVIRONMENTAL SCIENCE & TECHNOLOGY

The hinge region in androgen receptor control

(2012) Liesbeth Clinckemalie et al.   MOLECULAR AND CELLULAR ENDOCRINOLOGY

Small Molecule Inhibitors Targeting the “Achilles' Heel” of Androgen Receptor Activity: Figure 1.

(2011) Marianne D. Sadar   CANCER RESEARCH

Niphatenones, Glycerol Ethers from the Sponge Niphates digitalis Block Androgen Receptor Transcriptional Activity in Prostate Cancer Cells: Structure Elucidation, Synthesis, and Biological Activity

(2011) Labros G. Meimetis et al.   JOURNAL OF MEDICINAL CHEMISTRY

Small Molecule Inhibition of the Steroid Receptor Coactivators, SRC-3 and SRC-1

(2011) Ying Wang et al.   MOLECULAR ENDOCRINOLOGY

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

Multiple Independent Binding Sites for Small-Molecule Inhibitors on the Oncoprotein c-Myc

(2009) Dalia I. Hammoudeh et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Structural Characterization of the Native NH2-Terminal Transactivation Domain of the Human Androgen Receptor: A Collapsed Disordered Conformation Underlies Structural Plasticity and Protein-Induced Folding†

(2008) Derek N. Lavery et al.   BIOCHEMISTRY

Sintokamides A to E, Chlorinated Peptides from the SpongeDysideasp. that Inhibit Transactivation of the N-Terminus of the Androgen Receptor in Prostate Cancer Cells

(2008) Marianne D. Sadar et al.   ORGANIC LETTERS