ArticleMolecular and cellular biology2011
Structural basis and specificity of acetylated transcription factor GATA1 recognition by BET family bromodomain protein Brd3.
Article in Molecular and cellular biology, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 62 papers.
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Who cites it
62 citing papers in PubMed, 122 citations in OpenAlex.
- Development of 2 Bromodomain and Extraterminal Inhibitors With Distinct Pharmacokinetic and Pharmacodynamic Profiles for the Treatment of Advanced Malignancies.Clinical cancer research : an official journal of the American Association for Cancer Research · 2020Trial
- Eyes Toward the Clinic: Selective Inhibition and Degradation Approaches to Bromodomain-Containing Proteins.Chembiochem : a European journal of chemical biology · 2026Review
- The BRD4-nucleosome interaction is enhanced modestly and non-selectively by histone acetylation.Nucleic acids research · 2025Article
- Sustained Clinical Response to Immunotherapy Followed by BET Inhibitor in a Patient with Unresectable Sinonasal NUT Carcinoma.Journal of immunotherapy and precision oncology · 2024Article
- mRNA display reveals a class of high-affinity bromodomain-binding motifs that are not found in the human proteome.The Journal of biological chemistry · 2023Article
- New cytotoxic dammarane type saponins from Ziziphus spina-christi.Scientific reports · 2023Article
- Domain-Selective BET Ligands Yield Next-Generation Synthetic Genome Readers/Regulators with Nonidentical Cellular Functions.Journal of the American Chemical Society · 2023Article
- Article
- Selective BD2 Inhibitor Exerts Anti-Fibrotic Effects via BRD4/FoxM1/Plk1 Axis in Orbital Fibroblasts From Patients With Thyroid Eye Disease.Investigative ophthalmology & visual science · 2023Article
- BET Bromodomain Inhibitors: Novel Design Strategies and Therapeutic Applications.Molecules (Basel, Switzerland) · 2023Review
- Gene silencing dynamics are modulated by transiently active regulatory elements.Molecular cell · 2023Article
- Viral Hijacking of BET Proteins.Viruses · 2022Review
- A Structure-based Design Approach for Generating High Affinity BRD4 D1-Selective Chemical Probes.Journal of medicinal chemistry · 2022Article
- A Comprehensive Review of BET Protein Biochemistry, Physiology, and Pathological Roles.Frontiers in pharmacology · 2022Review
- HDAC1 is required for GATA-1 transcription activity, global chromatin occupancy and hematopoiesis.Nucleic acids research · 2021Article
- Improved methods for targeting epigenetic reader domains of acetylated and methylated lysine.Current opinion in chemical biology · 2021Review
- Relevance of BET Family Proteins in SARS-CoV-2 Infection.Biomolecules · 2021Review
- Functional Roles of Bromodomain Proteins in Cancer.Cancers · 2021Review
- Are BET Inhibitors yet Promising Latency-Reversing Agents for HIV-1 Reactivation in AIDS Therapy?Viruses · 2021Review
- The bromodomains of BET family proteins can recognize diacetylated histone H2A.Z.Protein science : a publication of the Protein Society · 2021Article
2 more citing papers are in PubMed but not listed here.
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Authors and funding
6 authors at 3 institutions in 3 countries.
Funding
Abstract
Recent data demonstrate that small synthetic compounds specifically targeting bromodomain proteins can modulate the expression of cancer-related or inflammatory genes. Although these studies have focused on the ability of bromodomains to recognize acetylated histones, it is increasingly becoming clear that histone-like modifications exist on other important proteins, such as transcription factors. However, our understanding of the molecular mechanisms through which these modifications modulate protein function is far from complete. The transcription factor GATA1 can be acetylated at lysine residues adjacent to the zinc finger domains, and this acetylation is essential for the normal chromatin occupancy of GATA1. We have recently identified the bromodomain-containing protein Brd3 as a cofactor that interacts with acetylated GATA1 and shown that this interaction is essential for the targeting of GATA1 to chromatin. Here we describe the structural basis for this interaction. Our data reveal for the first time the molecular details of an interaction between a transcription factor bearing multiple acetylation modifications and its cognate recognition module. We also show that this interaction can be inhibited by an acetyllysine mimic, highlighting the importance of further increasing the specificity of compounds that target bromodomain and extraterminal (BET) bromodomains in order to fully realize their therapeutic potential.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.