Click chemistry enables preclinical evaluation of targeted epigenetic therapies
Tyler, Dean S., Vappiani, Johanna, Cañeque, Tatiana, Lam, Enid Y. N., Ward, Aoife, Gilan, Omer, Chan, Yih-Chih, Hienzsch, Antje, Rutkowska, Anna, Werner, Thilo, Wagner, Anne J., Lugo, Dave, Gregory, Richard, Ramirez Molina, Cesar, Garton, Neil, Wellaway, Christopher R., Jackson, Susan, MacPherson, Laura, Figueiredo, Margarida, Stolzenburg, Sabine, Bell, Charles C., House, Colin, Dawson, Sarah-Jane, Hawkins, Edwin D., Drewes, Gerard, Prinjha, Rab K., Rodriguez, Raphaël, Grandi, Paola, Dawson, Mark A.·2017·Science
Cited by (152)
Items 101–152 of 152
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- A Photo‐responsive Small‐Molecule Approach for the Opto‐epigenetic Modulation of DNA MethylationHa Phuong Nguyen, Sabrina K. Stewart, Mikiembo N. Kukwikila, Sioned Fôn Jones, Daniel Offenbartl‐Stiegert, Shi-Qing Mao, Shankar Balasubramanian, Stephan Beck, Stefan Howorka · 2019 · Angewandte Chemie
- Design and Characterization of 1,3-Dihydro-2 H -benzo[ d ]azepin-2-ones as Rule-of-5 Compliant Bivalent BET InhibitorsPaul Bamborough, Chun‐wa Chung, Nicole C. Goodwin, Darren J. Mitchell, Christopher E. Neipp, Alex Phillipou, Alex G. S. Preston, Rab K. Prinjha, Peter E. Soden, Robert J. Watson et al. · 2023 · ACS Medicinal Chemistry Letters
- Chemical Biology Tools for Protein Lysine AcylationYusheng Xie, Shubo Du, Zhiyang Liu, Min Liu, Zhiqiang Xu, Xiaojie Wang, Jia Xuan Kee, Fan Yi, Hongyan Sun, Shao Qin Yao · 2022 · Angewandte Chemie
- Click-cross-linked, doxorubicin-loaded hydrogels based on poly(styrene-alt-maleic anhydride)Daru Seto Bagus Anugrah, Maheshkumar Prakash Patil, Xinmeng Li, Cuong Minh Quoc Le, Kalyan Ramesh, G-D. Kim, Kyu Hyun, K. T. Lim · 2020 · eXPRESS Polymer Letters
- Subcellular localization of drug distribution by super-resolution ion beam imagingXavier Rovira‐Clavé, Sizun Jiang, Yunhao Bai, Graham L. Barlow, Salil S. Bhate, Ahmet F. Coskun, Guojun Han, Bokai Zhu, Chin‐Min Kimmy Ho, Chuck Hitzman et al. · 2019 · bioRxiv (Cold Spring Harbor Laboratory)
- Single-cell multiomics: a new frontier in drug research and developmentJian Ma, Chao Fang Dong, Aibin He, Haiqing Xiong · 2024 · Frontiers in Drug Discovery
- Proteomics approaches in the identification of cancer biomarkers and drug discoveryNasir Nisar, Suhail Ahmad Mir, Ozaifa Kareem, Faheem Hyder Pottoo · 2023 · Elsevier eBooks
- A Click Strategy for the Synthesis of Fluorescent Pyrimidinone‐Triazole Hybrids with CDK2 Selectivity in HeLa and A549 Cell LinesAranhikkal Shamsiya, Damodaran Bahulayan · 2019 · ChemistrySelect
- Macrocyclization in medicinal chemistry: updated strategies and applicationsOm Darlami, Keun-young Kim A, Dongyun Shin, Seok‐Ho Kim · 2025 · Medicinal Chemistry Research
- Apabetalone, a Clinical-Stage, Selective BET Inhibitor, Opposes DUX4 Target Gene Expression in Primary Human FSHD Muscle CellsChristopher D. Sarsons, Dean Gilham, Laura M. Tsujikawa, Sylwia Wasiak, Li Fu, Brooke D. Rakai, Stephanie C. Stotz, Agostina Carestia, Michael Sweeney, Ewelina Kulikowski · 2023 · Biomedicines
- Selectivity Mechanism of Pyrrolopyridone Analogues Targeting Bromodomain 2 of Bromodomain-Containing Protein 4 from Molecular Dynamics SimulationsMingsong Shi, Xueting Zheng, Yan Zhou, Yuan Yin, Lu Zhou, Zhiyan Zou, Yan Hu, Yuanyuan Liang, Tingting Chen, Yuhan Yang et al. · 2023 · ACS Omega
- Macrocyclic dihydropyridine analogs as pan-BET BD2-preferred inhibitorsJiewei Jiang, Taimeng Liang, Jonathan C. Solberg, Alice Chan, Prakriti Kalra, Rui Shi, William C. K. Pomerantz, Jon E. Hawkinson, E. Schönbrunn, Gunda I. Georg · 2025 · European Journal of Medicinal Chemistry
- Bioinspired Selenium‐Nitrogen Exchange (SeNEx) Click Chemistry Suitable for Nanomole‐Scale Medicinal Chemistry and BioconjugationWei Hou, Yiyuan Zhang, Fuchao Huang, Wanting Chen, Yuang Gu, Yan Wang, Jiacheng Pang, Hewei Dong, Kangyin Pan, Shuning Zhang et al. · 2024 · Angewandte Chemie
- Click and discoverGeorge S. Vassiliou, Shankar Balasubramanian · 2017 · Nature
- Selective inhibition mechanism of three inhibitors to BRD4 uncovered by molecular docking and molecular dynamics simulationsWei Chen, L. Sang, R. Wang, D. Zou, Lin Chen · 2024 · SAR and QSAR in environmental research
- Chromatin Regulatory Targets for Anticancer TherapeuticsPaige A. Barta, Trever R. Carter, Michael A. Erb · 2025 · Chemical Reviews
- Discovery of a Photoaffinity Probe that Captures the Active Conformation of the Cannabinoid CB2 ReceptorLaura V. de Paus, Yu An, Antonius P. A. Janssen, Richard J. B. H. N. van den Berg, Laura H. Heitman, Mario van der Stelt · 2024 · ChemBioChem
- Reprogramming the chemical reactivity of iron in cancer stem cellsTatiana Cañeque, Sebastian Müller, Anne Lafon, Fabien Sindikubwabo, Antoine Versini, Lou Saier, Manon Barutaut, Christine Gaillet, Raphaël Rodriguez · 2018 · Comptes Rendus Chimie
- Place Your BETs in Combination TherapyBrian Liddicoat, Mark A. Dawson · 2020 · Molecular Cell
- Functional ProteomicsLuke N. Erber, Yue Chen · 2021 · ACS in focus
- Enzyme-free chemical DNA ligation via amine-crosslinker-mediated DNA assembly for miRNA detectionDoyeon Lim, Zeeshan Haider, Hyo-Jin Lim, Won Jin Lee, Taeseok Kang, Hyuk Soo Eun, Jin Chul Kim, Youngjun Song · 2025 · Cell Reports Physical Science
- Inert Complexes Unlock Ligand‐Accelerated Transition‐Metal Catalysis on ProteinsZhen Wang, Fengrui Xiang, XH Liao, Qingsong Wu, Jinbiao Jiao, Angzhi Bi, SiYang Maggie Liu, Dan Wang, Mengdi Wang, Zijian Guo et al. · 2026 · Angewandte Chemie International Edition
- Supramolecular nanocatalyst in water: successive click-driven assembly of click-derived rod amphiphilesInhye Kim, Eunji J. Lee · 2019 · Materials Chemistry Frontiers
- The Synthesis and Biological Evaluation of Some C-9 and C-10 Substituted Derivatives of the RNA Polymerase I Transcription Inhibitor CX-5461Madushani Amarasiri, Yen Vo, Michael G. Gardiner, Perlita Poh, Priscilla Soo, Megan Pavy, Nadine Hein, Rita Ferreira, Katherine M. Hannan, Ross D. Hannan et al. · 2021 · Australian Journal of Chemistry
- Activatable fluorescence molecular imaging and anti-tumor effects investigation of GSH-sensitive BRD4 ligandsHang Zhang, Mingliang Zhang, Yujie Zhang, Han Wang, Linnan Zhao, Hai‐Wei Xu · 2022 · Bioorganic Chemistry
- The Life Science Toolbox Provided by Chemical BiologyCarsten Schultz · 2019 · Israel Journal of Chemistry
- Selective N‐Terminal BET Bromodomain Inhibitors by Targeting Non‐Conserved Residues and Structured Water Displacement**Huarui Cui, Anand Divakaran, Anil K. Pandey, Jorden A. Johnson, Huda Zahid, Zachariah J. Hoell, Mikael O. Ellingson, Ke Shi, Hideki Aihara, Daniel A. Harki et al. · 2020 · Angewandte Chemie
- Design of BET Inhibitor Prodrugs with Superior Efficacy and Devoid of Systemic ToxicitiesFarrukh Vohidov, Jannik N. Andersen, Kyriakos D. Economides, Michail V. Shipitsin, Olga V. Burenkova, James C. Ackley, Bhavatarini Vangamudi, Nolan M. Gallagher, Peyton Shieh, Matthew R. Golder et al. · 2020 · ChemRxiv
- Single-cell profiling of small molecule-genomic interactions and epigenetic statesChao Dong, Xiaoxuan Meng, Tong Zhang, Zhifang Guo, Yaxi Liu, Peihuang Wu, Shiwei Chen, Fanqi Zhou, Yanni Ma, Shaokun Shu et al. · 2024 · Research Square
- Association of MiR-29b/BRD4 with Airway Dysbiosis in Chronic Obstructive Pulmonary Disease after Smoking CessationSiyi Zhou, Yu-xin Zeng, Tao Yu, Jianmiao Wang · 2025 · Current Medical Science
- Additional file 1 of BRD4 is involved in viral exacerbation of chronic obstructive pulmonary diseaseDuan, Yifei, Zhou, Siyi, Wang, Jianmiao · 2023 · Figshare
- Inert Complexes Unlock Ligand‐Accelerated Transition‐Metal Catalysis on ProteinsZhen Wang, Fengrui Xiang, XH Liao, Qingsong Wu, Jinbiao Jiao, Angzhi Bi, SiYang Maggie Liu, Dan Wang, Mengdi Wang, Zijian Guo et al. · 2026 · Angewandte Chemie
- Des inhibiteurs de méthyltransférases de l'ADN au développement de sondes chimiques pour l'identification de modulateurs épigénétiques dérégulés dans les cancersDany Pechalrieu · 2017 · theses.fr (ABES)
- Validation de nouvelles cibles thérapeutiques dans le glioblastome par une approche de pharmacologie fonctionnelleJérémy Ariey-Bonnet · 2020 · theses.fr (ABES)
- Advancements in green click chemistry: Sustainable catalytic methods for the synthesis of 1,2,3-triazole derivativesSahil Jindal, Rakesh Kumar, Chetan Sharma, Man Vir Singh, A Suresh Kumar, Yogesh Kumar · 2026 · Next research.
- Reversible Click Reactions in Water: A Robust and Customizable Synthetic ToolY.R. Shen, Yijian Zong, Huacheng Yu, Jiang‐Fei Xu, Mei‐Xiang Wang, Xi Zhang · 2026 · Angewandte Chemie International Edition
- Reversible Click Reactions in Water: A Robust and Customizable Synthetic ToolY.R. Shen, Yijian Zong, Huacheng Yu, Jiang‐Fei Xu, Mei‐Xiang Wang, Xi Zhang · 2026 · Angewandte Chemie
- BindingDB Entry 50007698: Discovery ofBindingDB · 2021 · UC San Diego
- BindingDB Entry 50019895: 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.BindingDB · 2024 · UC San Diego
- BindingDB Entry 50011062: Structure-Based Design of a Bromodomain and Extraterminal Domain (BET) Inhibitor Selective for the N-Terminal Bromodomains That Retains an Anti-inflammatory and Antiproliferative Phenotype.BindingDB · 2021 · UC San Diego
- BindingDB Entry 50016263: Targeting Bromodomain-Selective Inhibitors of BET Proteins in Drug Discovery and Development.BindingDB · 2023 · UC San Diego
- BindingDB Entry 50010598: Application of Atypical Acetyl-lysine Methyl Mimetics in the Development of Selective Inhibitors of the Bromodomain-Containing Protein 7 (BRD7)/Bromodomain-Containing Protein 9 (BRD9) Bromodomains.BindingDB · 2021 · UC San Diego
- BindingDB Entry 50023478: PROTAC unleashed: Unveiling the synthetic approaches and potential therapeutic applications.BindingDB · 2026 · UC San Diego
- BindingDB Entry 50022868: Discovery of the First BRD4 Second Bromodomain (BD2)-Selective Inhibitors.BindingDB · 2026 · UC San Diego
- BindingDB Entry 50023737: Macrocyclic dihydropyridine analogs as pan-BET BD2-preferred inhibitors.BindingDB · 2026 · UC San Diego
- BindingDB Entry 50016017: Development of an N-Terminal BRD4 Bromodomain-Targeted Degrader.BindingDB · 2023 · UC San Diego
- BindingDB Entry 50018669: Progress in the development of domain selective inhibitors of the bromo and extra terminal domain family (BET) proteins.BindingDB · 2024 · UC San Diego