4.7 Article

Selectively targeting individual bromodomain: Drug discovery and molecular mechanisms

Related references

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

Selective N-Terminal BET Bromodomain Inhibitors by Targeting Non-Conserved Residues and Structured Water Displacement**

Huarui Cui et al.

Summary: The study developed selective BET D1 inhibitors with higher selectivity for BRD4 D1, but BRD4 D1 inhibition may not be sufficient to stop Myc expression and could even lead to its upregulation. Future analysis of BRD4 D1 gene regulation may shed light on the differential functions of BET bromodomains.

ANGEWANDTE CHEMIE-INTERNATIONAL EDITION (2021)

Review Chemistry, Medicinal

Current development of CBP/p300 inhibitors in the last decade

Zhang-Xu He et al.

Summary: CBP/p300, as a potential target for treating diseases including malignant tumors, has attracted interest in the development of small-molecule inhibitors. The review focuses on the development of CBP/p300 inhibitors from 2010 to 2020, highlighting their structure-activity relationships, binding modes, selectivity, and pharmacological functions to facilitate rational design and development of potential inhibitors.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2021)

Article Multidisciplinary Sciences

Discovery of a hidden transient state in all bromodomain families

Lluis Raich et al.

Summary: Bromodomains are small protein modules that interact with acetylated marks in histones, crucial for gene expression regulation. A conserved transient state involving breaking of hydrogen bonds was discovered, serving as an allosteric regulatory switch potentially related to a recently unveiled mode of BD-DNA binding.

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2021)

Article Chemistry, Medicinal

Targeting Bromodomain and Extraterminal Proteins for Drug Discovery: From Current Progress to Technological Development

Pan Tang et al.

Summary: BET proteins regulate chromatin dynamics, cellular processes, and disease progression by binding acetylated lysine residues in histones and nonhistone proteins, making them a promising strategy for treating malignant tumors and chronic inflammation. However, the clinical efficacy of current BET inhibitors is limited, leading to the development of new technologies to improve outcomes and minimize side effects.

JOURNAL OF MEDICINAL CHEMISTRY (2021)

Article Biochemistry & Molecular Biology

BET inhibition blocks inflammation-induced cardiac dysfunction and SARS-CoV-2 infection

Richard J. Mills et al.

Summary: Cardiac injury and dysfunction in COVID-19 patients increase mortality risk. An inflammatory cytokine-storm can induce diastolic dysfunction, but BET inhibitors show promise in preventing cardiac damage and dysfunction induced by the virus.
Review Biochemistry & Molecular Biology

The BET family in immunity and disease

Nian Wang et al.

Summary: The BET family plays a crucial role in regulating the transcription of genes associated with inflammation and immunity by recognizing acetylated histones and recruiting transcription factors and elongation complexes. Manipulating the BET family holds promise as a new treatment approach for disease.

SIGNAL TRANSDUCTION AND TARGETED THERAPY (2021)

Letter Critical Care Medicine

More Insights into the Association between RVX-208 and Pulmonary Arterial Hypertension

Dong Ning et al.

AMERICAN JOURNAL OF RESPIRATORY AND CRITICAL CARE MEDICINE (2020)

Article Biochemistry & Molecular Biology

In silico design and molecular basis for the selectivity of Olinone toward the first over the second bromodomain of BRD4

Yoel Rodriguez et al.

PROTEINS-STRUCTURE FUNCTION AND BIOINFORMATICS (2020)

Review Biochemistry & Molecular Biology

Proteolysis-Targeting Chimeras as Therapeutics and Tools for Biological Discovery

George M. Burslem et al.

Article Multidisciplinary Sciences

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

Emily J. Faivre et al.

NATURE (2020)

Article Biochemistry & Molecular Biology

Covalent-Fragment Screening of BRD4 Identifies a Ligandable Site Orthogonal to the Acetyl-Lysine Binding Sites

Michael D. Olp et al.

ACS CHEMICAL BIOLOGY (2020)

Review Chemistry, Medicinal

Novel strategies targeting bromodomain-containing protein 4 (BRD4) for cancer drug discovery

Dailin Liang et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2020)

Article Chemistry, Medicinal

GSK789: A Selective Inhibitor of the First Bromodomains (BD1) of the Bromo and Extra Terminal Domain (BET) Proteins

Robert J. Watson et al.

JOURNAL OF MEDICINAL CHEMISTRY (2020)

Review Biochemistry & Molecular Biology

Recent Advances in the Development of CBP/p300 Bromodomain Inhibitors

Ying Xiong et al.

CURRENT MEDICINAL CHEMISTRY (2020)

Article Chemistry, Medicinal

GSK973 Is an Inhibitor of the Second Bromodomains (BD2s) of the Bromodomain and Extra-Terminal (BET) Family

Alex Preston et al.

ACS MEDICINAL CHEMISTRY LETTERS (2020)

Article Biochemistry & Molecular Biology

Degradation of Polycomb Repressive Complex 2 with an EED-Targeted Bivalent Chemical Degrader

Frances Potjewyd et al.

CELL CHEMICAL BIOLOGY (2020)

Article Biochemistry & Molecular Biology

Insight into selective mechanism of class of I-BRD9 inhibitors toward BRD9 based on molecular dynamics simulations

Jing Su et al.

CHEMICAL BIOLOGY & DRUG DESIGN (2019)

Article Biochemistry & Molecular Biology

Computational study on the selective inhibition mechanism of MS402 to the first and second bromodomains of BRD4

Qianqian Wang et al.

PROTEINS-STRUCTURE FUNCTION AND BIOINFORMATICS (2019)

Article Critical Care Medicine

Multicenter Preclinical Validation of BET Inhibition for the Treatment of Pulmonary Arterial Hypertension

Diederik E. Van der Feen et al.

AMERICAN JOURNAL OF RESPIRATORY AND CRITICAL CARE MEDICINE (2019)

Review Biochemistry & Molecular Biology

Targeted protein degradation: elements of PROTAC design

Stacey-Lynn Paiva et al.

CURRENT OPINION IN CHEMICAL BIOLOGY (2019)

Article Medicine, Research & Experimental

Structure-guided drug design identifies a BRD4-selective small molecule that suppresses HIV

Qingli Niu et al.

JOURNAL OF CLINICAL INVESTIGATION (2019)

Review Biotechnology & Applied Microbiology

Bromodomains: a new target class for drug development

Andrea G. Cochran et al.

NATURE REVIEWS DRUG DISCOVERY (2019)

Article Chemistry, Medicinal

Discovery, structural insight, and bioactivities of BY27 as a selective inhibitor of the second bromodomains of BET proteins

Deheng Chen et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2019)

Review Biochemistry & Molecular Biology

Bromodomain biology and drug discovery

Nilesh Zaware et al.

NATURE STRUCTURAL & MOLECULAR BIOLOGY (2019)

Article Chemistry, Medicinal

A Click Chemistry Platform for the Rapid Synthesis of Bispecific Molecules for Inducing Protein Degradation

Ryan P. Wurz et al.

JOURNAL OF MEDICINAL CHEMISTRY (2018)

Article Biochemistry & Molecular Biology

Pharmacological perturbation of CDK9 using selective CDK9 inhibition or degradation

Calla M. Olson et al.

NATURE CHEMICAL BIOLOGY (2018)

Article Biochemistry & Molecular Biology

Exploiting a water network to achieve enthalpy-driven, bromodomain-selective BET inhibitors

William R. Shadrick et al.

BIOORGANIC & MEDICINAL CHEMISTRY (2018)

Article Chemistry, Medicinal

Discovery of potent and selective BRD4 inhibitors capable of blocking TLR3-induced acute airway inflammation

Zhiqing Liu et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2018)

Article Chemistry, Medicinal

Structure-based discovery of selective BRPF1 bromodomain inhibitors

Jian Zhu et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2018)

Article Biochemistry & Molecular Biology

Plasticity in binding confers selectivity in ligand-induced protein degradation

Radoslaw P. Nowak et al.

NATURE CHEMICAL BIOLOGY (2018)

Article Biochemistry & Molecular Biology

Functional TRIM24 degrader via conjugation of ineffectual bromodomain and VHL ligands

Lara N. Gechijian et al.

NATURE CHEMICAL BIOLOGY (2018)

Article Biochemistry & Molecular Biology

Modulating PCAF/GCN5 Immune Cell Function through a PROTAC Approach

Zuni I. Bassi et al.

ACS CHEMICAL BIOLOGY (2018)

Review Biochemistry & Molecular Biology

Targeting Brd4 for cancer therapy: inhibitors and degraders

Yingchao Duan et al.

MEDCHEMCOMM (2018)

Article Multidisciplinary Sciences

Defining the human C2H2 zinc finger degrome targeted by thalidomide analogs through CRBN

Quinlan L. Sievers et al.

SCIENCE (2018)

Article Chemistry, Multidisciplinary

Large-scale analysis of water stability in bromodomain binding pockets with grand canonical Monte Carlo

Matteo Aldeghi et al.

COMMUNICATIONS CHEMISTRY (2018)

Article Biochemistry & Molecular Biology

The polar warhead of a TRIM24 bromodomain inhibitor rearranges a water-mediated interaction network

Jiuyang Liu et al.

FEBS JOURNAL (2017)

Article Chemistry, Physical

Rapid and Reliable Binding Affinity Prediction of Bromodomain Inhibitors: A Computational Study

Shunzhou Wan et al.

JOURNAL OF CHEMICAL THEORY AND COMPUTATION (2017)

Article Chemistry, Multidisciplinary

Predictions of Ligand Selectivity from Absolute Binding Free Energy Calculations

Matteo Aldeghi et al.

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY (2017)

Article Biochemistry & Molecular Biology

Distinct Roles of Brd2 and Brd4 in Potentiating the Transcriptional Program for Th17 Cell Differentiation

Ka Lung Cheung et al.

MOLECULAR CELL (2017)

Article Biochemistry & Molecular Biology

Structural basis of PROTAC cooperative recognition for selective protein degradation

Morgan S. Gadd et al.

NATURE CHEMICAL BIOLOGY (2017)

Review Biotechnology & Applied Microbiology

Marked for death: targeting epigenetic changes in cancer

Sophia Xiao Pfister et al.

NATURE REVIEWS DRUG DISCOVERY (2017)

Review Cell Biology

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

Takao Fujisawa et al.

NATURE REVIEWS MOLECULAR CELL BIOLOGY (2017)

Article Multidisciplinary Sciences

BET N-terminal bromodomain inhibition selectively blocks Th17 cell differentiation and ameliorates colitis in mice

Kalung Cheung et al.

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2017)

Article Multidisciplinary Sciences

Selective BET bromodomain inhibition as an antifungal therapeutic strategy

Flore Mietton et al.

NATURE COMMUNICATIONS (2017)

Article Biochemistry & Molecular Biology

Isoform-Selective ATAD2 Chemical Probe with Novel Chemical Structure and Unusual Mode of Action

Amaury E. Fernandez-Montalvan et al.

ACS CHEMICAL BIOLOGY (2017)

Article Biochemistry & Molecular Biology

Selective Targeting of Bromodomains of the Bromodomain-PHD Fingers Family Impairs Osteoclast Differentiation

Julia C. Meier et al.

ACS CHEMICAL BIOLOGY (2017)

Review Biochemistry & Molecular Biology

Chemical modulators for epigenome reader domains as emerging epigenetic therapies for cancer and inflammation

Nilesh Zaware et al.

CURRENT OPINION IN CHEMICAL BIOLOGY (2017)

Article Chemistry, Multidisciplinary

Beyond the BET Family: Targeting CBP/p300 with 4-Acyl Pyrroles

Martin Huegle et al.

ANGEWANDTE CHEMIE-INTERNATIONAL EDITION (2017)

Review Biochemistry & Molecular Biology

Targeted Protein Degradation: from Chemical Biology to Drug Discovery

Philipp M. Cromm et al.

CELL CHEMICAL BIOLOGY (2017)

Review Oncology

BET inhibitors: a novel epigenetic approach

D. B. Doroshow et al.

ANNALS OF ONCOLOGY (2017)

Article Oncology

Targeted Degradation of BET Proteins in Triple-Negative Breast Cancer

Longchuan Bai et al.

CANCER RESEARCH (2017)

Article Chemistry, Multidisciplinary

Degradation of the BAF Complex Factor BRD9 by Heterobifunctional Ligands

David Remillard et al.

ANGEWANDTE CHEMIE-INTERNATIONAL EDITION (2017)

Review Biochemistry & Molecular Biology

The Bromodomain: A New Target in Emerging Epigenetic Medicine

Steven G. Smith et al.

ACS CHEMICAL BIOLOGY (2016)

Article Chemistry, Medicinal

Discovery and Characterization of GSK2801, a Selective Chemical Probe for the Bromodomains BAZ2A and BAZ2B

Peiling Chen et al.

JOURNAL OF MEDICINAL CHEMISTRY (2016)

Article Chemistry, Medicinal

Discovery of I-BRD9, a Selective Cell Active Chemical Probe for Bromodomain Containing Protein 9 Inhibition

Natalie H. Theodoulou et al.

JOURNAL OF MEDICINAL CHEMISTRY (2016)

Article Chemistry, Medicinal

Structure-Guided Design of IACS-9571, a Selective High-Affinity Dual TRIM24-BRPF1 Bromodomain Inhibitor

Wylie S. Palmer et al.

JOURNAL OF MEDICINAL CHEMISTRY (2016)

Article Biochemistry & Molecular Biology

RVX-297-a novel BD2 selective inhibitor of BET bromodomains

Olesya A. Kharenko et al.

BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS (2016)

Article Pharmacology & Pharmacy

Bromodomains: Structure, function and pharmacology of inhibition

Elena Ferri et al.

BIOCHEMICAL PHARMACOLOGY (2016)

Article Biochemistry & Molecular Biology

Modulation of p300/CBP Acetylation of Nucleosomes by Bromodomain Ligand I-CBP112

Beth E. Zucconi et al.

BIOCHEMISTRY (2016)

Review Chemistry, Medicinal

Progress in the Development of non-BET Bromodomain Chemical Probes

Natalie H. Theodoulou et al.

CHEMMEDCHEM (2016)

Article Chemistry, Medicinal

Structure-Based Design of an in Vivo Active Selective BRD9 Inhibitor

Laetitia J. Martin et al.

JOURNAL OF MEDICINAL CHEMISTRY (2016)

Article Chemistry, Medicinal

Development of Selective CBP/P300 Benzoxazepine Bromodomain Inhibitors

Tobias A. Popp et al.

JOURNAL OF MEDICINAL CHEMISTRY (2016)

Article Oncology

AZD5153: A Novel Bivalent BET Bromodomain Inhibitor Highly Active against Hematologic Malignancies

Garrett W. Rhyasen et al.

MOLECULAR CANCER THERAPEUTICS (2016)

Review Biotechnology & Applied Microbiology

Epigenetic drug discovery: breaking through the immune barrier

David F. Tough et al.

NATURE REVIEWS DRUG DISCOVERY (2016)

Article Multidisciplinary Sciences

PROTAC-induced BET protein degradation as a therapy for castration-resistant prostate cancer

Kanak Raina et al.

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2016)

Article Chemistry, Medicinal

GSK6853, a Chemical Probe for Inhibition of the BRPF1 Bromodomain

Paul Bamborough et al.

ACS MEDICINAL CHEMISTRY LETTERS (2016)

Article Chemistry, Medicinal

Fragment-Based Discovery of a Selective and Cell-Active Benzodiazepinone CBP/EP300 Bromodomain Inhibitor (CPI-637)

Alexander M. Taylor et al.

ACS MEDICINAL CHEMISTRY LETTERS (2016)

Article Chemistry, Multidisciplinary

Protein Degradation by In-Cell Self-Assembly of Proteolysis Targeting Chimeras

Honorine Lebraud et al.

ACS CENTRAL SCIENCE (2016)

Review Chemistry, Multidisciplinary

Discovery of Chemical Inhibitors of Human Bromodomains

Guangtao Zhang et al.

CHEMICAL REVIEWS (2015)

Article Biochemistry & Molecular Biology

Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4

Jing Lu et al.

CHEMISTRY & BIOLOGY (2015)

Article Pharmacology & Pharmacy

An evaluation of RVX-208 for the treatment of atherosclerosis

Dragana Nikolic et al.

EXPERT OPINION ON INVESTIGATIONAL DRUGS (2015)

Article Chemistry, Medicinal

Structure-Based Optimization of Naphthyridones into Potent ATAD2 Bromodomain Inhibitors

Paul Bamborough et al.

JOURNAL OF MEDICINAL CHEMISTRY (2015)

Article Chemistry, Medicinal

Structure Enabled Design of BAZ2-ICR, A Chemical Probe Targeting the Bromodomains of BAZ2A and BAZ2B

Ludovic Drouin et al.

JOURNAL OF MEDICINAL CHEMISTRY (2015)

Article Multidisciplinary Sciences

CBP30, a selective CBP/p300 bromodomain inhibitor, suppresses human Th17 responses

Ariane Hammitzsch et al.

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2015)

Article Multidisciplinary Sciences

Phthalimide conjugation as a strategy for in vivo target protein degradation

Georg E. Winter et al.

SCIENCE (2015)

Article Biochemistry & Molecular Biology

Design and synthesis of potent and selective inhibitors of BRD7 and BRD9 bromodomains

Duncan A. Hay et al.

MEDCHEMCOMM (2015)

Review Genetics & Heredity

Targeting BET bromodomains for cancer treatment

Marie Jung et al.

EPIGENOMICS (2015)

Article Biochemistry & Molecular Biology

Acetyl-lysine Binding Site of Bromodomain-Containing Protein 4 (BRD4) Interacts with Diverse Kinase Inhibitors

Stuart W. J. Ember et al.

ACS CHEMICAL BIOLOGY (2014)

Article Biochemistry & Molecular Biology

Selective Chemical Modulation of Gene Transcription Favors Oligodendrocyte Lineage Progression

Mar Gacias et al.

CHEMISTRY & BIOLOGY (2014)

Article Chemistry, Multidisciplinary

Discovery and Optimization of Small-Molecule Ligands for the CBP/p300 Bromodomains

Duncan A. Hay et al.

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY (2014)

Review Biochemistry & Molecular Biology

The Mechanisms behind the Therapeutic Activity of BET Bromodomain Inhibition

Junwei Shi et al.

MOLECULAR CELL (2014)

Review Biotechnology & Applied Microbiology

Targeting bromodomains: epigenetic readers of lysine acetylation

Panagis Filippakopoulos et al.

NATURE REVIEWS DRUG DISCOVERY (2014)

Article Chemistry, Medicinal

1,3-Dimethyl Benzimidazolones Are Potent, Selective Inhibitors of the BRPF1 Bromodomain

Emmanuel H. Demont et al.

ACS MEDICINAL CHEMISTRY LETTERS (2014)

Article Chemistry, Medicinal

Structure-Guided Design of Potent Diazobenzene Inhibitors for the BET Bromodomains

Guangtao Zhang et al.

JOURNAL OF MEDICINAL CHEMISTRY (2013)

Article Biochemistry & Molecular Biology

Acetylation of RNA Polymerase II Regulates Growth-Factor-Induced Gene Transcription in Mammalian Cells

Sebastian Schroeder et al.

MOLECULAR CELL (2013)

Article Multidisciplinary Sciences

RVX-208, an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain

Sarah Picaud et al.

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2013)

Article Biochemistry & Molecular Biology

Histone Recognition and Large-Scale Structural Analysis of the Human Bromodomain Family

Panagis Filippakopoulos et al.

Article Chemistry, Medicinal

Druggability Analysis and Structural Classification of Bromodomain Acetyl-lysine Binding Sites

Lewis R. Vidler et al.

JOURNAL OF MEDICINAL CHEMISTRY (2012)

Review Oncology

BET domain co-regulators in obesity, inflammation and cancer

Anna C. Belkina et al.

NATURE REVIEWS CANCER (2012)

Article Multidisciplinary Sciences

Bromodomain protein Brd3 associates with acetylated GATA1 to promote its chromatin occupancy at erythroid target genes

Janine M. Lamonica et al.

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2011)

Article Biochemistry & Molecular Biology

Recruitment of P-TEFb for stimulation of transcriptional elongation by the bromodomain protein brd4

ZY Yang et al.

MOLECULAR CELL (2005)

Review Multidisciplinary Sciences

Translating the histone code

T Jenuwein et al.

SCIENCE (2001)

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)