ReviewFuture medicinal chemistry2016
Selectivity on-target of bromodomain chemical probes by structure-guided medicinal chemistry and chemical biology.
Review in Future medicinal chemistry, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 22 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
22 citing papers in PubMed, 59 citations in OpenAlex.
- Fragment-Based Discovery of BRD4-BD2 Selective Binders: Biophysical Validation and Structural Insights for Domain-Selective Inhibitor Design.ACS omega · 2026Article
- Eyes Toward the Clinic: Selective Inhibition and Degradation Approaches to Bromodomain-Containing Proteins.Chembiochem : a European journal of chemical biology · 2026Review
- Identifying a non-conserved site for achieving allosteric covalent inhibition of CECR2.Acta pharmacologica Sinica · 2025Article
- Histone Modifications in the Anoxic Northern Crayfish, Faxonius virilis.Marine biotechnology (New York, N.Y.) · 2024Article
- An Update of Epigenetic Drugs for the Treatment of Cancers and Brain Diseases: A Comprehensive Review.Genes · 2023Review
- Improved methods for targeting epigenetic reader domains of acetylated and methylated lysine.Current opinion in chemical biology · 2021Review
- Chemogenomics for drug discovery: clinical molecules from open access chemical probes.RSC chemical biology · 2021Review
- Development of Dimethylisoxazole-Attached Imidazo[1,2-Journal of medicinal chemistry · 2021Article
- Identification of dual histone modification-binding protein interaction by combining mass spectrometry and isothermal titration calorimetric analysis.Journal of advanced research · 2020Article
- EpiHope for the Treatment of Pulmonary Arterial Hypertension: Selective versus Nonselective BET Inhibition.American journal of respiratory and critical care medicine · 2019Article
- BET bromodomain inhibitors: fragment-based in silico design using multi-target QSAR models.Molecular diversity · 2019Article
- BRD4 bimodal binding at promoters and drug-induced displacement at Pol II pause sites associates with I-BET sensitivity.Epigenetics & chromatin · 2019Article
- BETting on Novel Treatments for Asthma: Bromodomain 4 Inhibitors.American journal of respiratory cell and molecular biology · 2019Article
- Flavonoids as Putative Epi-Modulators: Insight into Their Binding Mode with BRD4 Bromodomains Using Molecular Docking and Dynamics.Biomolecules · 2018Article
- Optimization of a "bump-and-hole" approach to allele-selective BET bromodomain inhibition.Chemical science · 2018Article
- Impact of Target Warhead and Linkage Vector on Inducing Protein Degradation: Comparison of Bromodomain and Extra-Terminal (BET) Degraders Derived from Triazolodiazepine (JQ1) and Tetrahydroquinoline (I-BET726) BET Inhibitor Scaffolds.Journal of medicinal chemistry · 2018Article
- Selective inhibition mechanism of RVX-208 to the second bromodomain of bromo and extraterminal proteins: insight from microsecond molecular dynamics simulations.Scientific reports · 2017Article
- Chemical modulators for epigenome reader domains as emerging epigenetic therapies for cancer and inflammation.Current opinion in chemical biology · 2017Review
- Drug Discovery Targeting Bromodomain-Containing Protein 4.Journal of medicinal chemistry · 2017Review
- Structural basis of molecular recognition of helical histone H3 tail by PHD finger domains.The Biochemical journal · 2017Article
Corrections and comments
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Authors and funding
2 authors at 2 institutions in 2 countries.
Funding
Abstract
Targeting epigenetic proteins is a rapidly growing area for medicinal chemistry and drug discovery. Recent years have seen an explosion of interest in developing small molecules binding to bromodomains, the readers of acetyl-lysine modifications. A plethora of co-crystal structures has motivated focused fragment-based design and optimization programs within both industry and academia. These efforts have yielded several compounds entering the clinic, and many more are increasingly being used as chemical probes to interrogate bromodomain biology. High selectivity of chemical probes is necessary to ensure biological activity is due to an on-target effect. Here, we review the state-of-the-art of bromodomain-targeting compounds, focusing on the structural basis for their on-target selectivity or lack thereof. We also highlight chemical biology approaches to enhance on-target selectivity.
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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.