Click chemistry enables preclinical evaluation of targeted epigenetic therapies

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An electroaffinity labelling platform for chemoproteomic-based target identification

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Design of BET Inhibitor Bottlebrush Prodrugs with Superior Efficacy and Devoid of Systemic Toxicities

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Targeting BET Bromodomains in Cancer

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Radical-mediated click-clip reactions

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Injectable Catalyst-Free Poly(Propylene Fumarate) System Cross-Linked by Strain Promoted Alkyne–Azide Cycloaddition Click Chemistry for Spine Defect Filling

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Detection of cannabinoid receptor type 2 in native cells and zebrafish with a highly potent, cell-permeable fluorescent probe

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Template-Assembled Synthetic G-Quartets (TASQs): multiTASQing Molecular Tools for Investigating DNA and RNA G-Quadruplex Biology

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Click Chemistry: Novel Applications in Cell Biology and Drug Discovery

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BRD4 bimodal binding at promoters and drug-induced displacement at Pol II pause sites associates with I-BET sensitivity

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Targeting epigenetic reader domains by chemical biology

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Pharmacologic Reduction of Mitochondrial Iron Triggers a Noncanonical BAX/BAK-Dependent Cell Death

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Low-Pressure Flow Chemistry of CuAAC Click Reaction Catalyzed by Nanoporous AuCu Membrane

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Chemical Biology Tools for Protein Lysine Acylation

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Discovery of a Bromodomain and Extra Terminal Domain (BET) Inhibitor with the Selectivity for the Second Bromodomain (BD2) and the Capacity for the Treatment of Inflammatory Diseases

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Synthesis and Cellular Labeling of Caged Phosphatidylinositol Derivatives

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Progress in the development of domain selective inhibitors of the bromo and extra terminal domain family (BET) proteins

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Breaking the Silence: Regulation of HIV Transcription and Latency on the Road to a Cure

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PROTAC unleashed: Unveiling the synthetic approaches and potential therapeutic applications

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Improved methods for targeting epigenetic reader domains of acetylated and methylated lysine

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Discovery of the First BRD4 Second Bromodomain (BD2)-Selective Inhibitors

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Epigenetic BET reader inhibitor apabetalone (RVX-208) counters proinflammatory aortic gene expression in a diet induced obesity mouse model and in human endothelial cells

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Minimalist linkers suitable for irreversible inhibitors in simultaneous proteome profiling, live-cell imaging and drug screening

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Pharmacological Restriction of Genomic Binding Sites Redirects PU.1 Pioneer Transcription Factor Activity

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Fast functionalization of ultrasound microbubbles using strain promoted click chemistry

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Proteomics for cancer drug design

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Super enhancers as master gene regulators in the pathogenesis of hematologic malignancies

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Development of an N-Terminal BRD4 Bromodomain-Targeted Degrader

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Rapid conjugation of nanoparticles, proteins and siRNAs to microbubbles by strain-promoted click chemistry for ultrasound imaging and drug delivery

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Room-Temperature Cu(II) Radical-Triggered Alkyne C–H Activation

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Auto-RapTAC: A Versatile and Sustainable Platform for the Automated Rapid Synthesis and Evaluation of PROTAC

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A Photo‐responsive Small‐Molecule Approach for the Opto‐epigenetic Modulation of DNA Methylation

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Retinoblastoma protein as an intrinsic BRD4 inhibitor modulates small molecule BET inhibitor sensitivity in cancer

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Live-cell imaging and profiling of c-Jun N-terminal kinases using covalent inhibitor-derived probes

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“Clicking” Gene Therapeutics: A Successful Union of Chemistry and Biomedicine for New Solutions

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Novel Targeted Therapeutics in Acute Myeloid Leukemia: an Embarrassment of Riches

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Labelled Chemical Probes for Demonstrating Direct Target Engagement in Living Systems

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Single-cell EpiChem jointly measures drug–chromatin binding and multimodal epigenome

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Bioorthogonal “Click Chemistry” Bone Cement with Bioinspired Natural Mimicking Microstructures for Bone Repair

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The multivalent G-quadruplex (G4)-ligands MultiTASQs allow for versatile click chemistry-based investigations

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Visualization of Modified Bisarylbutadiyne-Tagged Small Molecules in Live-Cell Nuclei by Stimulated Raman Scattering Microscopy

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A gold-based inhibitor of oxidative phosphorylation is effective against triple negative breast cancer

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Biphenylation, ester-free and stepwise reaction strategy of thiol-epoxy crosslinking network for durable thermally and hygrothermally resistant electronic packaging

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BRD4 is involved in viral exacerbation of chronic obstructive pulmonary disease

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Poly-pharmacology of existing drugs: How to crack the code?

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Deciphering Drug Targets and Actions with Single-Cell and Spatial Resolution

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Brd/BET Proteins Influence the Genome-Wide Localization of the Kaposi’s Sarcoma-Associated Herpesvirus and Murine Gammaherpesvirus Major Latency Proteins

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Whole-genome mapping of small-molecule targets for cancer medicine

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Mapping cellular targets of covalent cancer drugs in the entire mammalian body

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Neue Anwendungen der Klick‐Chemie in Zellbiologie und Wirkstoffentwicklung

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Recommended Tool Compounds: Thienotriazolodiazepines-Derivatized Chemical Probes to Target BET Bromodomains

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Click chemistry enables comprehensive preclinical evaluation of targeted epigenetic therapies

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Click and discover

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Click Chemistry: Novel Applications in Cell Biology and Drug Discovery

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A Click-Chemistry Approach Reveals the BET Inhibitor Mechanism of Action

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Selective Targeting of Different Bromodomains by Small Molecules

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