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

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BIBW2992, an irreversible EGFR/HER2 inhibitor highly effective in preclinical lung cancer models

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Targeting bromodomains: epigenetic readers of lysine acetylation

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Targeting MYC dependence in cancer by inhibiting BET bromodomains

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Novel mutant-selective EGFR kinase inhibitors against EGFR T790M

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Deep proteome and transcriptome mapping of a human cancer cell line

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Developing Irreversible Inhibitors of the Protein Kinase Cysteinome

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Small Molecule Modulators of Histone Acetyltransferase p300

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Structural Bioinformatics-Based Design of Selective, Irreversible Kinase Inhibitors

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Bromodomains as therapeutic targets

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A road map to evaluate the proteome-wide selectivity of covalent kinase inhibitors

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Activity-based protein profiling for biochemical pathway discovery in cancer

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

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

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

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Cysteine Mapping in Conformationally Distinct Kinase Nucleotide Binding Sites: Application to the Design of Selective Covalent Inhibitors

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Selective Small Molecules Blocking HIV-1 Tat and Coactivator PCAF Association

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A LecA Ligand Identified from a Galactoside‐Conjugate Array Inhibits Host Cell Invasion by Pseudomonas aeruginosa

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PNA-encoded chemical libraries

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

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DNA display of fragment pairs as a tool for the discovery of novel biologically active small molecules

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DNA-templated combinatorial assembly of small molecule fragments amenable to selection/amplification cycles

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Self‐Assembled Small‐Molecule Microarrays for Protease Screening and Profiling

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Expanding the Scope of PNA‐Encoded Synthesis (PES): Mtt‐Protected PNA Fully Orthogonal to Fmoc Chemistry and a Broad Array of Robust Diversity‐Generating Reactions

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GCN5 acetylates and regulates the stability of the oncoprotein E2A-PBX1 in acute lymphoblastic leukemia

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Ethacrynic Acid Butyl-Ester Induces Apoptosis in Leukemia Cells through a Hydrogen Peroxide–Mediated Pathway Independent of GlutathioneS-Transferase P1-1 Inhibition

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Preparation of Small‐Molecule Microarrays by trans‐Cyclooctene Tetrazine Ligation and Their Application in the High‐Throughput Screening of Protein–Protein Interaction Inhibitors of Bromodomains

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Menadione and ethacrynic acid inhibit the hypoxia-inducible factor (HIF) pathway by disrupting HIF-1α interaction with p300

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A LecA Ligand Identified from a Galactoside‐Conjugate Array Inhibits Host Cell Invasion by Pseudomonas aeruginosa

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The Pleiotropic Effects of Ethacrynic Acid

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Discovery of an entropically-driven small molecule streptavidin binder from nucleic acid-encoded libraries

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Preparation of Small‐Molecule Microarrays by trans‐Cyclooctene Tetrazine Ligation and Their Application in the High‐Throughput Screening of Protein–Protein Interaction Inhibitors of Bromodomains

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Assembly of PNA-Tagged Small Molecules, Peptides, and Carbohydrates onto DNA Templates: Programming the Combinatorial Pairing and Inter-ligand Distance

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Advances in covalent drug discovery

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DNA-Encoded Chemical Libraries: A Selection System Based on Endowing Organic Compounds with Amplifiable Information

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Open-Air Alkylation Reactions in Photoredox-Catalyzed DNA-Encoded Library Synthesis

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Chemical Space of DNA-Encoded Libraries

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Covalent inhibitors: an opportunity for rational target selectivity

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DNA-encoded chemical libraries: foundations and applications in lead discovery

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Strategies for developing DNA-encoded libraries beyond binding assays

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Inhibitors of bromodomain and extra‐terminal proteins for treating multiple human diseases

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Achievements, Challenges, and Opportunities in DNA‐Encoded Library Research: An Academic Point of View

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Discovery of a Covalent Kinase Inhibitor from a DNA-Encoded Small-Molecule Library × Protein Library Selection

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Future challenges with DNA-encoded chemical libraries in the drug discovery domain

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PNA as a Biosupramolecular Tag for Programmable Assemblies and Reactions

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A Specific and Covalent JNK‐1 Ligand Selected from an Encoded Self‐Assembling Chemical Library

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Screening for covalent inhibitors using DNA-display of small molecule libraries functionalized with cysteine reactive moieties

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An overview of DNA-encoded libraries: A versatile tool for drug discovery

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Recent advances on the encoding and selection methods of DNA-encoded chemical library

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Affinity Enhancement of Protein Ligands by Reversible Covalent Modification of Neighboring Lysine Residues

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Targeting Bromodomain-Selective Inhibitors of BET Proteins in Drug Discovery and Development

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Targeting Allosteric Control Mechanisms in Heat Shock Protein 70 (Hsp70)

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Design and Characterization of Novel Covalent Bromodomain and Extra-Terminal Domain (BET) Inhibitors Targeting a Methionine

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ABPP-CoDEL: Activity-Based Proteome Profiling-Guided Discovery of Tyrosine-Targeting Covalent Inhibitors from DNA-Encoded Libraries

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Molecular docking and dynamics simulation study of flavonoids as BET bromodomain inhibitors

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Pharmacophore Nanoarrays on DNA Origami Substrates as a Single‐Molecule Assay for Fragment‐Based Drug Discovery

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Scanning Protein Surfaces with DNA‐Encoded Libraries

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Identification of Covalent Cyclic Peptide Inhibitors in mRNA Display

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Mapping the Ligand Binding Landscape

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Applications of Reactive Cysteine Profiling

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Novel PTP1B inhibitors identified by DNA display of fragment pairs

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Development of a Selection Method for Discovering Irreversible (Covalent) Binders from a DNA-Encoded Library

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Chemical Epigenetics: The Impact of Chemical and Chemical Biology Techniques on Bromodomain Target Validation

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Integration of Lead Discovery Tactics and the Evolution of the Lead Discovery Toolbox

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Rational Design Strategies in DNA‐Encoded Libraries for Drug Discovery

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An Activity‐Based Probe Targeting Non‐Catalytic, Highly Conserved Amino Acid Residues within Bromodomains

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Covalent hits and where to find them

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Recent Advances on the Selection Methods of DNA‐Encoded Libraries

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DNA-Encoded Library Technology─A Catalyst for Covalent Ligand Discovery

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Small-Molecule Modulators of the ATPase VCP/p97 Affect Specific p97 Cellular Functions

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An mRNA Display Approach for Covalent Targeting of a Staphylococcus aureus Virulence Factor

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DNA display of glycoconjugates to emulate oligomeric interactions of glycans

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Target 2035 – an update on private sector contributions

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Opportunities and challenges for the development of covalent chemical immunomodulators

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Advancing small-molecule drug discovery by encoded dual-display technologies

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Affinity Enhancement of Protein Ligands by Reversible Covalent Modification of Neighboring Lysine Residues

Corso, A. D., Catalano, M., Schmid, A. S., Scheuermann, J., & Neri, D. (2018) · Angewandte Chemie · doi:10.1002/ange.201811650 · Cited by 19 · see citing works

The Current Toolbox for Covalent Inhibitors: From Hit Identification to Drug Discovery

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Ethacrynic Acid: A Promising Candidate for Drug Repurposing as an Anticancer Agent

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Synthesis of deoxyelephantopin analogues

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Pharmacophore Nanoarrays on DNA Origami Substrates as a Single‐Molecule Assay for Fragment‐Based Drug Discovery

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Lysine‐Targeting, Covalent Inhibitors of Bromodomain BD1 of BET Proteins in Live Cells and Animals

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Best Practices for Design and Characterization of Covalent Chemical Probes

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Dual Bcl-XL /Bcl-2 inhibitors discovered from DNA-encoded libraries using a fragment pairing strategy

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Recent advances in DNA-encoded libraries: From covalent targeting to protein profiling

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Covalent fragment libraries in drug discovery—Design, synthesis, and screening methods

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An Activity‐Based Probe Targeting Non‐Catalytic, Highly Conserved Amino Acid Residues within Bromodomains

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Applied Biophysics for Bromodomain Drug Discovery

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Covalent chemistry in targeted protein degradation

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Seven-Membered Rings

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Universal and Quantitative Method To Evaluate Inhibitor Potency for Cysteinome Proteins Using a Nonspecific Activity-Based Protein Profiling Probe

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Chemische Epigenetik: der Einfluss chemischer und chemo‐biologischer Techniken auf die Zielstruktur‐Validierung von Bromodomänen

Schiedel, M., Moroglu, M., Ascough, D. M. H., Chamberlain, A. E. R., Kamps, J. J. A. G., Sekirnik, A. R., & Conway, S. J. (2019) · Angewandte Chemie · doi:10.1002/ange.201812164 · Cited by 3 · see citing works

Systematic Evaluation of Electrophile Reactivity and Stability for Covalent DNA‐Encoded Libraries

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Rational Design Strategies in DNA‐Encoded Libraries for Drug Discovery

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Covalent Modification of Bromodomain Proteins by Peptides Containing a DNA Damage‐Induced, Histone Post‐Translational Modification

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Lysine‐Targeting, Covalent Inhibitors of Bromodomain BD1 of BET Proteins in Live Cells and Animals

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Selection Strategies in DNA-Encoded Libraries

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High Throughput Screening Methods for PPI Inhibitor Discovery

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PNA-Encoded Synthesis (PES) and DNA Display of Small Molecule Libraries

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Application of DELs for E3 Ligase Ligand Discovery and Targeted Protein Degradation

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BindingDB Entry 50013495: Dual Bcl-X

BindingDB (2022) · UC San Diego · doi:10.7270/q2t157dk

BindingDB Entry 50016263: Targeting Bromodomain-Selective Inhibitors of BET Proteins in Drug Discovery and Development.

BindingDB (2023) · UC San Diego · doi:10.7270/q2v98d2c

BindingDB Entry 50012499: Novel PTP1B inhibitors identified by DNA display of fragment pairs.

BindingDB (2022) · UC San Diego · doi:10.7270/q2kk9ghp

BindingDB Entry 50002865: Design and Characterization of Novel Covalent Bromodomain and Extra-Terminal Domain (BET) Inhibitors Targeting a Methionine.

BindingDB (2020) · UC San Diego · doi:10.7270/q2f76g6t

BindingDB Entry 50009804: Chemical Space of DNA-Encoded Libraries.

BindingDB (2021) · UC San Diego · doi:10.7270/q2n58qv5

Identifizierung von niedermolekularen kovalenten Bromodomäne‐Bindern aus einer DNA‐kodierten Bibliothek

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An Activity‐Based Probe Targeting Non‐Catalytic, Highly Conserved Amino Acid Residues within Bromodomains

D’Ascenzio, M., Pugh, K., Konietzny, R., Berridge, G., Tallant, C., Hashem, S., Monteiro, O., Thomas, J. R., Schirle, M., Knapp, S., et al. (2018) · Angewandte Chemie · doi:10.1002/ange.201807825 · Cited by 6 · see citing works

Bromodomain biology and drug discovery

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A Chemical Biology Platform to Develop Small Molecule Probes for Bromodomains

Shaw, K. L. (2017) · Digital Access to Scholarship at Harvard (DASH) (Harvard University)

Abstract 4238: BROMOscan - a high throughput, quantitative ligand binding platform identifies best-in-class bromodomain inhibitors from a screen of mature compounds targeting other protein classes.

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