Novel forms of prostate cancer chemoresistance to successful androgen deprivation therapy demand new approaches: Rationale for targeting BET proteins

The Functions of the Demethylase JMJD3 in Cancer

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A prospective clinical and transcriptomic feasibility study of oral‐only hormonal therapy with radiation for unfavorable prostate cancer in men 70 years of age and older or with comorbidity

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A phase 1 study of the pan‐bromodomain and extraterminal inhibitor mivebresib (ABBV‐075) alone or in combination with venetoclax in patients with relapsed/refractory acute myeloid leukemia

(2021) Gautam Borthakur et al.   CANCER

Metabolic pathways in obesity-related breast cancer

(2021) Kristy A. Brown   Nature Reviews Endocrinology

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Unravelling KDM4 histone demethylase inhibitors for cancer therapy

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Population pharmacokinetic modeling of molibresib and its active metabolites in patients with solid tumors: A semimechanistic autoinduction model

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Selective inhibition of the BD2 bromodomain of BET proteins in prostate cancer

(2020) Emily J. Faivre et al.   NATURE

Nutrition and its role in epigenetic inheritance of obesity and diabetes across generations

(2020) Daniela Kaspar et al.   MAMMALIAN GENOME

Potent BRD4 inhibitor suppresses cancer cell-macrophage interaction

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Epigenetics in Inflammatory Breast Cancer: Biological Features and Therapeutic Perspectives

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Bromodomain-selective BET inhibitors are potent antitumor agents against MYC-driven pediatric cancer

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BRD4 regulates key transcription factors that drive epithelial–mesenchymal transition in castration-resistant prostate cancer

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Histone Demethylase KDM5B as a Therapeutic Target for Cancer Therapy

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Epigenetic Mechanisms of Resistance to Immune Checkpoint Inhibitors

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B7-H3 is regulated by BRD4 and promotes TLR4 expression in pancreatic ductal adenocarcinoma

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BRD4 regulates metastatic potential of castration-resistant prostate cancer through AHNAK

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Back to Basics: Social Determinants of Health

(2019) Lisa Spruce   AORN JOURNAL

Transcriptomic Heterogeneity of Androgen Receptor Activity Defines a de novo low AR-Active Subclass in Treatment Naïve Primary Prostate Cancer

(2019) Daniel E. Spratt et al.   CLINICAL CANCER RESEARCH

First-in-Human Study of Mivebresib (ABBV-075), an Oral Pan-Inhibitor of Bromodomain and Extra Terminal Proteins, in Patients with Relapsed/Refractory Solid Tumors

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Molecular profiling stratifies diverse phenotypes of treatment-refractory metastatic castration-resistant prostate cancer

(2019) Mark P. Labrecque et al.   JOURNAL OF CLINICAL INVESTIGATION

BET protein targeting suppresses the PD-1/PD-L1 pathway in triple-negative breast cancer and elicits anti-tumor immune response

(2019) Guillaume P. Andrieu et al.   CANCER LETTERS

Bromodomain and Extraterminal Proteins as Novel Epigenetic Targets for Renal Diseases

(2019) Jose Luis Morgado-Pascual et al.   Frontiers in Pharmacology

Immunogenicity of prostate cancer is augmented by BET bromodomain inhibition

(2019) Wendy Mao et al.   Journal for ImmunoTherapy of Cancer

Comparative structure-function analysis of bromodomain and extraterminal motif (BET) proteins in a gene-complementation system

(2019) Michael T. Werner et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Systematic characterization of chromatin modifying enzymes identifies KDM3B as a critical regulator in castration resistant prostate cancer

(2019) Hilal Saraç et al.   ONCOGENE

Small molecule JQ1 promotes prostate cancer invasion via BET-independent inactivation of FOXA1

(2019) Leiming Wang et al.   JOURNAL OF CLINICAL INVESTIGATION

BET proteins in abnormal metabolism, inflammation, and the breast cancer microenvironment

(2018) Guillaume P. Andrieu et al.   JOURNAL OF LEUKOCYTE BIOLOGY

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

BET Proteins Exhibit Transcriptional and Functional Opposition in the Epithelial-to-Mesenchymal Transition

(2018) Guillaume P. Andrieu et al.   MOLECULAR CANCER RESEARCH

Epigenetics and Epigenomics: Implications for Diabetes and Obesity

(2018) Evan D. Rosen et al.   DIABETES

Targeting the BRD4-HOXB13 Co-regulated Transcriptional Networks with Bromodomain-Kinase Inhibitors to Suppress Metastatic Castration-Resistant Prostate Cancer

(2018) Niveditha Nerlakanti et al.   MOLECULAR CANCER THERAPEUTICS

DUB3 Promotes BET Inhibitor Resistance and Cancer Progression by Deubiquitinating BRD4

(2018) Xin Jin et al.   MOLECULAR CELL

Depression and Obesity: Integrating the Role of Stress, Neuroendocrine Dysfunction and Inflammatory Pathways

(2018) Silvia R. S. Ouakinin et al.   Frontiers in Endocrinology

Relative contribution of health-related behaviours and chronic diseases to the socioeconomic patterning of low-grade inflammation

(2017) Marialaura Bonaccio et al.   International Journal of Public Health

Prostate cancer–associated SPOP mutations confer resistance to BET inhibitors through stabilization of BRD4

(2017) Xiangpeng Dai et al.   NATURE MEDICINE

Intrinsic BET inhibitor resistance in SPOP-mutated prostate cancer is mediated by BET protein stabilization and AKT–mTORC1 activation

(2017) Pingzhao Zhang et al.   NATURE MEDICINE

Functions of bromodomain-containing proteins and their roles in homeostasis and cancer

(2017) Takao Fujisawa et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

Inhibitor of H3K27 demethylase JMJD3/UTX GSK-J4 is a potential therapeutic option for castration resistant prostate cancer

(2017) Viacheslav M. Morozov et al.   Oncotarget

The Social Determinants of Health: It's Time to Consider the Causes of the Causes

(2017) Paula Braveman et al.   PUBLIC HEALTH REPORTS

MLL-AF9 Expression in Hematopoietic Stem Cells Drives a Highly Invasive AML Expressing EMT-Related Genes Linked to Poor Outcome

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BRD4 Regulates Breast Cancer Dissemination through Jagged1/Notch1 Signaling

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Uncontrolled diabetes predicts poor response to novel antiandrogens

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Evaluating Strategies For Reducing Health Disparities By Addressing The Social Determinants Of Health

(2016) Rachel L. J. Thornton et al.   HEALTH AFFAIRS

Response and resistance to BET bromodomain inhibitors in triple-negative breast cancer

(2016) Shaokun Shu et al.   NATURE

The role of GATA2 in lethal prostate cancer aggressiveness

(2016) Veronica Rodriguez-Bravo et al.   Nature Reviews Urology

Structure of the Brd4 ET domain bound to a C-terminal motif from γ-retroviral integrases reveals a conserved mechanism of interaction

(2016) Brandon L. Crowe et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

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

Androgen receptor-dependent and -independent mechanisms driving prostate cancer progression: Opportunities for therapeutic targeting from multiple angles

(2016) David T. Hoang et al.   Oncotarget

Predictors of early androgen deprivation treatment failure in prostate cancer with bone metastases

(2016) Eberhard Varenhorst et al.   Cancer Medicine

BET Bromodomain Proteins Brd2, Brd3 and Brd4 Selectively Regulate Metabolic Pathways in the Pancreatic β-Cell

(2016) Jude T. Deeney et al.   PLoS One

Functions of BET proteins in erythroid gene expression

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Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4

(2015) Jing Lu et al.   CHEMISTRY & BIOLOGY

Understanding the influence of psychological and socioeconomic factors on diabetes self-care using structured equation modeling

(2015) Rebekah J. Walker et al.   PATIENT EDUCATION AND COUNSELING

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(2015) Michelle Lane et al.   TRENDS IN ENDOCRINOLOGY AND METABOLISM

Food-Insecure Dietary Patterns Are Associated With Poor Longitudinal Glycemic Control in Diabetes: Results From the Boston Puerto Rican Health Study

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

(2014) Irfan A. Asangani et al.   NATURE

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Epithelial plasticity in prostate cancer: principles and clinical perspectives

(2014) Rajdeep Das et al.   TRENDS IN MOLECULAR MEDICINE

The double bromodomain protein Brd2 promotes B cell expansion and mitogenesis

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The C-terminal domain of Brd2 is important for chromatin interaction and regulation of transcription and alternative splicing

(2013) Jarmila Hnilicová et al.   MOLECULAR BIOLOGY OF THE CELL

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

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Distinct Genetic and Epigenetic Signatures of Colorectal Cancers According to Ethnic Origin

(2012) T. T. Nieminen et al.   CANCER EPIDEMIOLOGY BIOMARKERS & PREVENTION

Androgen receptor (AR) aberrations in castration-resistant prostate cancer

(2012) Kati K. Waltering et al.   MOLECULAR AND CELLULAR ENDOCRINOLOGY

The mutational landscape of lethal castration-resistant prostate cancer

(2012) Catherine S. Grasso et al.   NATURE

EZH2 Oncogenic Activity in Castration-Resistant Prostate Cancer Cells Is Polycomb-Independent

(2012) K. Xu et al.   SCIENCE

Food Insecurity and Hypoglycemia Among Safety Net Patients With Diabetes

(2011) Hilary K. Seligman   ARCHIVES OF INTERNAL MEDICINE

BET Bromodomain Inhibition as a Therapeutic Strategy to Target c-Myc

(2011) Jake E. Delmore et al.   CELL

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(2011) Scott M Dehm et al.   ENDOCRINE-RELATED CANCER

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(2011) Fang Fang Zhang et al.   Epigenetics

End Points and Outcomes in Castration-Resistant Prostate Cancer: From Clinical Trials to Clinical Practice

(2011) Howard I. Scher et al.   JOURNAL OF CLINICAL ONCOLOGY

Inhibition of BET recruitment to chromatin as an effective treatment for MLL-fusion leukaemia

(2011) Mark A. Dawson et al.   NATURE

Current management of castrate-resistant prostate cancer

(2010) S. J. Hotte et al.   Current Oncology

Selective inhibition of BET bromodomains

(2010) Panagis Filippakopoulos et al.   NATURE

Epigenetic programming by maternal nutrition: shaping future generations

(2010) Cheryl Chui Ying Li et al.   Epigenomics

A Novel Androgen Receptor Splice Variant Is Up-regulated during Prostate Cancer Progression and Promotes Androgen Depletion-Resistant Growth

(2009) Z. Guo et al.   CANCER RESEARCH

Bromodomain 4 activation predicts breast cancer survival

(2008) N. P. S. Crawford et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Solution structure of the extraterminal domain of the bromodomain-containing protein BRD4

(2008) Yi-Jan Lin et al.   PROTEIN SCIENCE