Keyword

BRD2

Description: BRD2 is a bromodomain-containing protein that binds acetylated chromatin and participates in transcriptional regulation and cellular differentiation.

Primary topic: Protein Degradation and Inhibitors (48%)

OpenAlex ID: keywords/brd2

The Brd4 Extraterminal Domain Confers Transcription Activation Independent of pTEFb by Recruiting Multiple Proteins, Including NSD3

2011 · Shaila Rahman, Mathew E. Sowa, et al. · Molecular and Cellular Biology · 528

Bromodomain inhibitor OTX015 in patients with acute leukaemia: a dose-escalation, phase 1 study

2016 · Céline Berthon, Emmanuel Raffoux, et al. · The Lancet Haematology · 420

BET Protein Function Is Required for Inflammation: Brd2 Genetic Disruption and BET Inhibitor JQ1 Impair Mouse Macrophage Inflammatory Responses

2013 · Anna C Belkina, Barbara S Nikolajczyk, et al. · The Journal of Immunology · 419

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Bromodomain inhibitor OTX015 in patients with lymphoma or multiple myeloma: a dose-escalation, open-label, pharmacokinetic, phase 1 study

2016 · Sandy Amorim, Anastasios Stathis, et al. · The Lancet Haematology · 417

SPR-Measured Dissociation Kinetics of PROTAC Ternary Complexes Influence Target Degradation Rate

2019 · Michael J. Roy, Sandra Winkler, et al. · ACS Chemical Biology · 373

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The Double Bromodomain Proteins Brd2 and Brd3 Couple Histone Acetylation to Transcription

2008 · Gary LeRoy, Brenden Rickards, et al. · Molecular Cell · 372

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Selective Recognition of Acetylated Histones by Bromodomain Proteins Visualized in Living Cells

2004 · Tomohiko Kanno, Yuka Kanno, et al. · Molecular Cell · 361

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The Bromodomain and Extra-Terminal Domain (BET) Family: Functional Anatomy of BET Paralogous Proteins

2016 · Yasushi Taniguchi · International Journal of Molecular Sciences · 336

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Discovery and Characterization of Small Molecule Inhibitors of the BET Family Bromodomains

2011 · Chun-wa Chung, Hervé Coste, et al. · Journal of Medicinal Chemistry · 334

PHOTACs enable optical control of protein degradation

2020 · Martin Reynders, Bryan S. Matsuura, et al. · Science Advances · 324

Growth and Early Postimplantation Defects in Mice Deficient for the Bromodomain-Containing Protein Brd4

2002 · Denis Houzelstein, Simon L. Bullock, et al. · Molecular and Cellular Biology · 316

Discovery of Epigenetic Regulator I-BET762: Lead Optimization to Afford a Clinical Candidate Inhibitor of the BET Bromodomains

2013 · Olivier Mirguet, Romain Gosmini, et al. · Journal of Medicinal Chemistry · 305

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

2017 · Pingzhao Zhang, Dejie Wang, et al. · Nature Medicine · 297

The BET family in immunity and disease

2021 · Nian Wang, Runliu Wu, et al. · Signal Transduction and Targeted Therapy · 288

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BET inhibitor OTX015 targets BRD2 and BRD4 and decreases c-MYC in acute leukemia cells

2015 · Marie-Magdelaine Coudé, Thorsten Braun, et al. · Oncotarget · 275

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PFI-1, a Highly Selective Protein Interaction Inhibitor, Targeting BET Bromodomains

2013 · Sarah Picaud, David Da Costa, et al. · Cancer Research · 249

Clinical trials for BET inhibitors run ahead of the science

2016 · Guillaume Andrieu, Anna C. Belkina, et al. · Drug Discovery Today Technologies · 245

Trivalent PROTACs enhance protein degradation via combined avidity and cooperativity

2021 · Satomi Imaide, Kristin M. Riching, et al. · Nature Chemical Biology · 239

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BET bromodomain-targeting compounds reactivate HIV from latency via a Tat-independent mechanism

2013 · Daniela Boehm, Vincenzo Calvanese, et al. · Cell Cycle · 235

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BET bromodomain inhibition suppresses TH17-mediated pathology

2013 · Deanna A. Mele, Andres Salmeron, et al. · The Journal of Experimental Medicine · 229

Inhibition of BET bromodomains as a therapeutic strategy for cancer drug discovery

2015 · Lei-lei Fu, Mao Tian, et al. · Oncotarget · 221

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Targeted protein degradation via intramolecular bivalent glues

2024 · Oliver Hsia, Matthias Hinterndorfer, et al. · Nature · 216

3,5-Dimethylisoxazoles Act As Acetyl-lysine-mimetic Bromodomain Ligands

2011 · David S. Hewings, Minghua Wang, et al. · Journal of Medicinal Chemistry · 216

Histone Variant H2A.Z.2 Mediates Proliferation and Drug Sensitivity of Malignant Melanoma

2015 · Chiara Vardabasso, Alexandre Gaspar-Maia, et al. · Molecular Cell · 206

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Synthetic Lethal and Resistance Interactions with BET Bromodomain Inhibitors in Triple-Negative Breast Cancer

2020 · Shaokun Shu, Hua-Jun Wu, et al. · Molecular Cell · 202

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Works count: 1,012

Citation count: 22,750