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BET bromodomain inhibitors: a patent review

, MSc PhD, , BSc (Hons) PhD & , BSc (Hons) PhD

Keep up to date with the latest research on this topic with citation updates for this article.

Read on this site (6)

Ghazi Elamin, Aimen Aljoundi & Mahmoud E.S. Soliman. (2022) A synergistic multitargeted of BET and HDAC: an intra-molecular mechanism of communication in treatment of Waldenström macroglobulinemia. Molecular Simulation 48:3, pages 197-208.
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S.L. Wu, L.F. Wang, H.B. Sun, W. Wang & Y.X. Yu. (2020) Probing molecular mechanism of inhibitor bindings to bromodomain-containing protein 4 based on molecular dynamics simulations and principal component analysis. SAR and QSAR in Environmental Research 31:7, pages 547-570.
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Tian Lu, Wenchao Lu & Cheng Luo. (2020) A patent review of BRD4 inhibitors (2013-2019). Expert Opinion on Therapeutic Patents 30:1, pages 57-81.
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Utkarsh Raj, Himansu Kumar & Pritish Kumar Varadwaj. (2017) Molecular docking and dynamics simulation study of flavonoids as BET bromodomain inhibitors. Journal of Biomolecular Structure and Dynamics 35:11, pages 2351-2362.
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Thorsten Braun & Claude Gardin. (2017) Investigational BET bromodomain protein inhibitors in early stage clinical trials for acute myelogenous leukemia (AML). Expert Opinion on Investigational Drugs 26:7, pages 803-811.
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Anirban Ghoshal, D. Yugandhar & Ajay Kumar Srivastava. (2016) BET inhibitors in cancer therapeutics: a patent review. Expert Opinion on Therapeutic Patents 26:4, pages 505-522.
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Articles from other publishers (89)

Erin BradleyLucia FusaniChun-wa Chung, Peter D. CraggsEmmanuel H. DemontPhilip G. Humphreys, Darren J. MitchellAlex PhillipouInmaculada RiojaRishi R. Shah, Christopher R. Wellaway, Rab K. PrinjhaDavid S. Palmer, William J. Kerr, Marc Reid, Ian D. WallRosa Cookson. (2023) Structure-Guided Design of a Domain-Selective Bromodomain and Extra Terminal N-Terminal Bromodomain Chemical Probe. Journal of Medicinal Chemistry.
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Abhishek Wahi, Namish Manchanda, Priti Jain & Hemant R Jadhav. (2023) Targeting the epigenetic reader “BET” as a therapeutic strategy for cancer. Bioorganic Chemistry 140, pages 106833.
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Lauriane Lemelle, Tim Flaadt, Brice Fresneau, Antoine Moya-Plana, Beate Timmermann, Jelena Roganovic, Andrea Ferrari, Giulia Fichera, Ulrich M. Lauer, Tal Ben-Ami, Dominik T. Schneider, Christian Vokuhl, Stephanie Bolle, Elisabeth Fox, Steven G. DuBois, Carlos Rodriguez-Galindo, Gianni Bisogno, Aurore Surun, Ines B. Brecht & Daniel Orbach. (2023) NUT Carcinoma in Children and Adolescents: The Expert European Standard Clinical Practice Harmonized Recommendations. Journal of Pediatric Hematology/Oncology 45:4, pages 165-173.
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Carlos Gaona-López, Lenci K. Vazquez-Jimenez, Alonzo Gonzalez-Gonzalez, Timoteo Delgado-Maldonado, Eyrá Ortiz-Pérez, Benjamín Nogueda-Torres, Adriana Moreno-Rodríguez, Karina Vázquez, Emma Saavedra & Gildardo Rivera. (2023) Advances in Protozoan Epigenetic Targets and Their Inhibitors for the Development of New Potential Drugs. Pharmaceuticals 16:4, pages 543.
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Feng Wang, Xiang Feng, Qing He, Hua Li & Huilin Li. (2023) The Saccharomyces cerevisiae Yta7 ATPase hexamer contains a unique bromodomain tier that functions in nucleosome disassembly. Journal of Biological Chemistry 299:2, pages 102852.
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Maria Mushtaq Ali, Sehrish Naz, Sajda Ashraf, Stefan Knapp & Zaheer Ul-Haq. (2023) Epigenetic modulation by targeting bromodomain containing protein 9 (BRD9): Its therapeutic potential and selective inhibition. International Journal of Biological Macromolecules, pages 123428.
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Philip G. Humphreys, Niall A. Anderson, Paul Bamborough, Andrew BaxterChun-wa Chung, Rosa CooksonPeter D. CraggsToryn Dalton, Julie C. L. Fournier, Laurie J. GordonHeather F. Gray, Matthew W. Gray, Richard GregoryDavid J. HirstCraig Jamieson, Katherine L. Jones, Hripsimee KessedjianDavid LugoGrant McGonagleVipulkumar K. PatelChristopher PattenDarren L. PooleRab K. PrinjhaCesar Ramirez-MolinaInmaculada RiojaGail SealKayleigh A. J. StaffordRishi R. Shah, Daniel TapeNatalie H. TheodoulouLaura TomlinsonSabri UkuserIan D. WallNatalie WellawayGemma White. (2022) Identification and Optimization of a Ligand-Efficient Benzoazepinone Bromodomain and Extra Terminal (BET) Family Acetyl-Lysine Mimetic into the Oral Candidate Quality Molecule I-BET432. Journal of Medicinal Chemistry 65:22, pages 15174-15207.
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Lauriane Lemelle, Antoine Moya-Plana, Benoît Dumont, Brice Fresneau, Anne Laprie, Line Claude, Sophie Deneuve, Camille Cordero, Gaelle Pierron, Vincent Couloigner, Sophie Bernard, Liesbeth Cardoen, Hervé J. Brisse, Nina Jehanno, Lucy Metayer, Paul Fréneaux, Sylvie Helfre, Fréderic Kolb, Juliette Thariat, Yves Réguerre & Daniel Orbach. (2022) NUT carcinoma in children, adolescents and young adults. Bulletin du Cancer 109:4, pages 491-504.
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Yanzi Pei, Yujie Qian, Hao Wang & Li Tan. (2022) Epigenetic Regulation of Ferroptosis-Associated Genes and Its Implication in Cancer Therapy. Frontiers in Oncology 12.
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Yali He, Chuanhe Yang, Yinan Wang, Joshua R. Sacher, Michelle M. Sims, Lawrence M. Pfeffer & Duane D. Miller. (2022) Novel structural-related analogs of PFI-3 (SRAPs) that target the BRG1 catalytic subunit of the SWI/SNF complex increase the activity of temozolomide in glioblastoma cells. Bioorganic & Medicinal Chemistry 53, pages 116533.
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Anna M. Jermakowicz, Matthew J. Rybin, Robert K. Suter, Jann N. Sarkaria, Zane Zeier, Yangbo Feng & Nagi G. Ayad. (2021) The novel BET inhibitor UM-002 reduces glioblastoma cell proliferation and invasion. Scientific Reports 11:1.
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Negar Omidkhah, Farzin Hadizadeh & Razieh Ghodsi. (2021) Dual HDAC/BRD4 inhibitors against cancer. Medicinal Chemistry Research 30:10, pages 1822-1836.
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Ping Bai, Yu Lan, Hao Wang, Yan Liu, Robin Striar, Gengyang Yuan, Sepideh Afshar, Julia S. Zagaroli, Darcy R. Tocci, Amelia G. Langan & Changning Wang. (2021) Synthesis and Characterization of a Positron Emission Tomography Imaging Probe Selectively Targeting the Second Bromodomain of Bromodomain Protein BRD4. Bioconjugate Chemistry 32:8, pages 1711-1718.
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Cichun Wu, Da Cheng, Yanghui Peng, Ying Li, Chunyan Fu, Ying Wang, Lei Fu, Shifang Peng & Xin Ni. (2021) Hepatic BRD4 Is Upregulated in Liver Fibrosis of Various Etiologies and Positively Correlated to Fibrotic Severity. Frontiers in Medicine 8.
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Alvina I. Khamidullina, Ekaterina A. Varlamova, Nour Alhuda Hammoud, Margarita A. Yastrebova & Alexandra V. Bruter. (2021) Gene Transcription as a Therapeutic Target in Leukemia. International Journal of Molecular Sciences 22:14, pages 7340.
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Liang Li, Wei Xie, Yu Gui & Xi‐Long Zheng. (2020) Bromodomain‐containing protein 4 and its role in cardiovascular diseases. Journal of Cellular Physiology 236:7, pages 4829-4840.
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Shiliang Wu, Lifei Wang, Lulu Zhang, Xiaoyan Xu & Juan Zhao. (2021) Molecular dynamics insights into binding selectivity of inhibitors toward BRD4 and CBP. Chemical Physics Letters 769, pages 138435.
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Ping Bai, Xiaoxia Lu, Yan Liu, Yu Lan, Hao Wang, Stephanie Fiedler, Robin Striar & Changning Wang. (2021) Discovery of a Positron Emission Tomography Radiotracer Selectively Targeting the BD1 Bromodomains of BET Proteins. ACS Medicinal Chemistry Letters 12:2, pages 282-287.
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Nanumi Han, Delnur Anwar, Naoki Hama, Takuto Kobayashi, Hidefumi Suzuki, Hidehisa Takahashi, Haruka Wada, Ryo Otsuka, Muhammad Baghdadi & Ken-ichiro Seino. (2020) Bromodomain-containing protein 4 regulates interleukin-34 expression in mouse ovarian cancer cells. Inflammation and Regeneration 40:1.
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Ping Bai, Yu Lan, Hao Wang, Zude Chen, Stephanie Fiedler, Robin Striar, Xiaoxia Lu & Changning Wang. (2020) Development of a Novel Positron Emission Tomography (PET) Radiotracer Targeting Bromodomain and Extra-Terminal Domain (BET) Family Proteins. Frontiers in Molecular Biosciences 7.
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Martin V. Nguyen, Lydia Loof & Gerald S. Falchook. (2020) Bromodomain and Extra-Terminal (BET) Domain Protein Inhibitors for Solid Tumor Cancers. Journal of Immunotherapy and Precision Oncology 3:1, pages 16-22.
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Alexander N. Phillipou, Charles S. Lay, Charlotte E. Carver, Cassie Messenger, John P. Evans, Antonia J. Lewis, Laurie J. Gordon, Mahnoor Mahmood, Luke A. Greenhough, Douglas Sammon, Aaron T. Cheng, Syandan Chakraborty, Emma J. Jones, Simon C.C. Lucas, Kelly M. Gatfield, David J. Brierley & Peter D. Craggs. (2020) Cellular Target Engagement Approaches to Monitor Epigenetic Reader Domain Interactions. SLAS Discovery 25:2, pages 163-175.
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Chun‐wa Chung & Michael M. Hann. 2020. Structural Biology in Drug Discovery. Structural Biology in Drug Discovery 479 502 .
Victoria Lucia Alonso, Luis Emilio Tavernelli, Alejandro Pezza, Pamela Cribb, Carla Ritagliati & Esteban Serra. (2019) Aim for the Readers! Bromodomains As New Targets Against Chagas’ Disease. Current Medicinal Chemistry 26:36, pages 6544-6563.
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Pavel Mader, Rodrigo Mendoza-Sanchez, Aman Iqbal, Aiping Dong, Elena Dobrovetsky, Victoria B. Corless, Sean K. Liew, Scott R. Houliston, Renato Ferreira De Freitas, David Smil, Carlo C. Dela Sena, Steven Kennedy, Diego B. Diaz, Hong Wu, Ludmila Dombrovski, Abdellah Allali-Hassani, Jinrong Min, Matthieu Schapira, Masoud Vedadi, Peter J. Brown, Vijayaratnam Santhakumar, Andrei K. Yudin & Cheryl H. Arrowsmith. (2019) Identification and characterization of the first fragment hits for SETDB1 Tudor domain. Bioorganic & Medicinal Chemistry 27:17, pages 3866-3878.
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Shilei Liu, Fengnan Li, Lijia Pan, Ziyi Yang, Yijun Shu, Wenjie Lv, Ping Dong & Wei Gong. (2019) BRD4 inhibitor and histone deacetylase inhibitor synergistically inhibit the proliferation of gallbladder cancer in vitro and in vivo. Cancer Science 110:8, pages 2493-2506.
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Ping Yu, Wenjing Liu, Jinghui Ren, Yingying Wang, Yao Ning, Mingqi Huang, Xinyi Hu, Lili Wei, Min Ji & Jin Cai. (2019) Design, synthesis and biological evaluation of hypolipidemic compounds based on BRD4 inhibitor RVX-208. Bioorganic & Medicinal Chemistry Letters 29:16, pages 2168-2172.
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Beth E. Zucconi, Jessica L. Makofske, David J. Meyers, Yousang Hwang, Mingxuan Wu, Mitzi I. Kuroda & Philip A. Cole. (2019) Combination Targeting of the Bromodomain and Acetyltransferase Active Site of p300/CBP. Biochemistry 58:16, pages 2133-2143.
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Ali Alqahtani, Khalil Choucair, Mushtaq Ashraf, Danae M Hammouda, Abduraham Alloghbi, Talal Khan, Neil Senzer & John Nemunaitis. (2019) Bromodomain and extra-terminal motif inhibitors: a review of preclinical and clinical advances in cancer therapy. Future Science OA 5:3.
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Amy Donner, Heather King, Paul E. Brennan, Moses Moustakim & William J. Zuercher. 2019. Epigenetic Drug Discovery. Epigenetic Drug Discovery 133 152 .
Yan-Min Yang, Rong-Hua Shi, Chuan-Xiang Xu & Lei Li. (2018) BRD4 expression in patients with essential hypertension and its effect on blood pressure in spontaneously hypertensive rats. Journal of the American Society of Hypertension 12:12, pages e107-e117.
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Shuai Liu, Hailemichael O. Yosief, Lingling Dai, He Huang, Gagan Dhawan, Xiaofeng Zhang, Alex M. Muthengi, Justin Roberts, Dennis L. Buckley, Jennifer A. Perry, Lei Wu, James E. Bradner, Jun Qi & Wei Zhang. (2018) Structure-Guided Design and Development of Potent and Selective Dual Bromodomain 4 (BRD4)/Polo-like Kinase 1 (PLK1) Inhibitors. Journal of Medicinal Chemistry 61:17, pages 7785-7795.
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Adeena Tahir, Rima D. Alharthy, Saadia Naseem, Natasha Mahmood, Mahmood Ahmed, Khuram Shahzad, Malik Nadeem Akhtar, Abdul Hameed, Irfan Sadiq, Haq Nawaz & Muhammad Muddassar. (2018) Investigations of Structural Requirements for BRD4 Inhibitors through Ligand- and Structure-Based 3D QSAR Approaches. Molecules 23:7, pages 1527.
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Bárbara I. Díaz-Eufracio, J. Jesús Naveja & José L. Medina-Franco. 2018. Protein-Protein Interactions in Human Disease, Part A. Protein-Protein Interactions in Human Disease, Part A 65 84 .
Minjin Yoo, Miyoun Yoo, Ji Eun Kim, Heung Kyoung Lee, Chong Ock Lee, Chi Hoon Park & Kwan-Young Jung. (2017) Synthesis and biological evaluation of indazole-4,7-dione derivatives as novel BRD4 inhibitors. Archives of Pharmacal Research 41:1, pages 46-56.
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Phillip P. Sharp, Jean-Marc Garnier, Tamas Hatfaludi, Zhen Xu, David Segal, Kate E. Jarman, Hélène Jousset, Alexandra Garnham, John T. Feutrill, Anthony Cuzzupe, Peter Hall, Scott Taylor, Carl R. Walkley, Dean Tyler, Mark A. Dawson, Peter Czabotar, Andrew F. Wilks, Stefan Glaser, David C. S. Huang & Christopher J. Burns. (2017) Design, Synthesis, and Biological Activity of 1,2,3-Triazolobenzodiazepine BET Bromodomain Inhibitors. ACS Medicinal Chemistry Letters 8:12, pages 1298-1303.
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Tan Boon Toh, Jhin Jieh Lim & Edward Kai-Hua Chow. (2017) Epigenetics in cancer stem cells. Molecular Cancer 16:1.
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Lauriane Lemelle, Gaëlle Pierron, Paul Fréneaux, Sophie Huybrechts, Alexandra Spiegel, Dominique Plantaz, Morbize Julieron, Sophie Dumoucel, Antoine Italiano, Fréderic Millot, Christophe Le Tourneau, Guy Leverger, Pascal Chastagner, Matthieu Carton & Daniel Orbach. (2017) NUT carcinoma in children and adults: A multicenter retrospective study . Pediatric Blood & Cancer 64:12, pages e26693.
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Panpan Lu, Yinzhong Shen, He Yang, Yanan Wang, Zhengtao Jiang, Xinyi Yang, Yangcheng Zhong, Hanyu Pan, Jianqing Xu, Hongzhou Lu & Huanzhang Zhu. (2017) BET inhibitors RVX-208 and PFI-1 reactivate HIV-1 from latency. Scientific Reports 7:1.
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Michael D. Olp, Nan Zhu & Brian C. Smith. (2017) Metabolically Derived Lysine Acylations and Neighboring Modifications Tune the Binding of the BET Bromodomains to Histone H4. Biochemistry 56:41, pages 5485-5495.
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Imran Ali, Jooyun Lee, Areum Go, Gildon Choi & Kwangho Lee. (2017) Discovery of novel [1,2,4]triazolo[4,3- a ]quinoxaline aminophenyl derivatives as BET inhibitors for cancer treatment. Bioorganic & Medicinal Chemistry Letters 27:20, pages 4606-4613.
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Zhiqing Liu, Pingyuan Wang, Haiying Chen, Eric A. Wold, Bing Tian, Allan R. Brasier & Jia Zhou. (2017) Drug Discovery Targeting Bromodomain-Containing Protein 4. Journal of Medicinal Chemistry 60:11, pages 4533-4558.
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Yixin Zhu, Weijin Yang, Guangnian Ji, Nan Lin, Weihang Wu, Ping Xiong, Chenxin Zheng, Lei Yan, Peng Wan & Yu Wang. (2017) Bromodomain protein 4 is a novel predictor of survival for gastric carcinoma. Oncotarget 8:19, pages 31092-31100.
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Leilei Zhao, Yifei Yang, Yahui Guo, Lingyun Yang, Jian Zhang, Jinpei Zhou & Huibin Zhang. (2017) Design, synthesis and biological evaluation of 7-methylimidazo[1,5- a ]pyrazin-8(7 H )-one derivatives as BRD4 inhibitors. Bioorganic & Medicinal Chemistry 25:8, pages 2482-2490.
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Narayanan Balaji, Murugan Chinnapattu, Abhishek Dixit, Promod Sahu, Suresh P S & Ramesh Mullangi. (2017) Validation of an enantioselective LC-MS/MS method to quantify enantiomers of (±)-OTX015 in mice plasma: Lack of in vivo inversion of (−)-OTX015 to its antipode . Biomedical Chromatography 31:4, pages e3853.
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Moses Moustakim, Peter G. K. Clark, Laura Trulli, Angel L. Fuentes de Arriba, Matthias T. Ehebauer, Apirat Chaikuad, Emma J. Murphy, Jacqui Mendez‐Johnson, Danette Daniels, Chun‐Feng D. Hou, Yu‐Hui Lin, John R. Walker, Raymond Hui, Hongbing Yang, Lucy Dorrell, Catherine M. Rogers, Octovia P. Monteiro, Oleg Fedorov, Kilian V. M. Huber, Stefan Knapp, Jag Heer, Darren J. Dixon & Paul E. Brennan. (2016) Discovery of a PCAF Bromodomain Chemical Probe. Angewandte Chemie International Edition 56:3, pages 827-831.
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Moses Moustakim, Peter G. K. Clark, Laura Trulli, Angel L. Fuentes de Arriba, Matthias T. Ehebauer, Apirat Chaikuad, Emma J. Murphy, Jacqui Mendez‐Johnson, Danette Daniels, Chun‐Feng D. Hou, Yu‐Hui Lin, John R. Walker, Raymond Hui, Hongbing Yang, Lucy Dorrell, Catherine M. Rogers, Octovia P. Monteiro, Oleg Fedorov, Kilian V. M. Huber, Stefan Knapp, Jag Heer, Darren J. Dixon & Paul E. Brennan. (2016) Discovery of a PCAF Bromodomain Chemical Probe. Angewandte Chemie 129:3, pages 845-849.
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Tomomi Noguchi-Yachide, Seika Amemiya, Takao Yamaguchi & Yuichi Hashimoto. (2017) Development of N6-(Heteroarylcarbonyl)adenines as BRD4 Inhibitors. HETEROCYCLES 94:6, pages 1107.
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Jie Li, Peiqi Wang, Bihui Zhou, Jianyou Shi, Jie Liu, Xiangrong Li, Limei Fan, Yaxin Zheng & Liang Ouyang. (2016) Development of 4,5-dihydro-benzodiazepinone derivatives as a new chemical series of BRD4 inhibitors. European Journal of Medicinal Chemistry 121, pages 294-299.
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Narayanan Balaji, Ramesh Mullangi & A. Siva Kumar. (2016) Development and Validation of a Chiral Liquid Chromatographic Method for Quantitative Determination of (+)-OTX015 in (−)-OTX015. Chromatographia 79:19-20, pages 1317-1323.
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Natalie H Theodoulou, Nicholas CO Tomkinson, Rab K Prinjha & Philip G Humphreys. (2016) Clinical progress and pharmacology of small molecule bromodomain inhibitors. Current Opinion in Chemical Biology 33, pages 58-66.
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Paul Bamborough, Heather A. Barnett, Isabelle Becher, Mark J. Bird, Chun-wa Chung, Peter D. Craggs, Emmanuel H. Demont, Hawa Diallo, David J. FallonLaurie J. Gordon, Paola Grandi, Clare I. Hobbs, Edward Hooper-Greenhill, Emma J. Jones, Robert P. LawArmelle Le Gall, David Lugo, Anne-Marie Michon, Darren J. Mitchell, Rab K. Prinjha, Robert J. Sheppard, Allan J. B. WatsonRobert J. Watson. (2016) GSK6853, a Chemical Probe for Inhibition of the BRPF1 Bromodomain. ACS Medicinal Chemistry Letters 7:6, pages 552-557.
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Terry D. Crawford, Vickie Tsui, E. Megan Flynn, Shumei Wang, Alexander M. Taylor, Alexandre Côté, James E. Audia, Maureen H. Beresini, Daniel J. Burdick, Richard Cummings, Les A. Dakin, Martin Duplessis, Andrew C. Good, Michael C. Hewitt, Hon-Ren Huang, Hariharan Jayaram, James R. Kiefer, Ying Jiang, Jeremy Murray, Christopher G. Nasveschuk, Eneida Pardo, Florence Poy, F. Anthony Romero, Yong Tang, Jian Wang, Zhaowu Xu, Laura E. Zawadzke, Xiaoyu Zhu, Brian K. Albrecht, Steven R. Magnuson, Steve Bellon & Andrea G. Cochran. (2016) Diving into the Water: Inducible Binding Conformations for BRD4, TAF1(2), BRD9, and CECR2 Bromodomains. Journal of Medicinal Chemistry 59:11, pages 5391-5402.
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Dong U. Lee, Paula Katavolos, Gopinath Palanisamy, Arna Katewa, Charly Sioson, Janice Corpuz, Jodie Pang, Kevin DeMent, Edna Choo, Nico Ghilardi, Dolores Diaz & Dimitry M. Danilenko. (2016) Nonselective inhibition of the epigenetic transcriptional regulator BET induces marked lymphoid and hematopoietic toxicity in mice. Toxicology and Applied Pharmacology 300, pages 47-54.
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Brian S. Gerstenberger, John D. Trzupek, Cynthia Tallant, Oleg Fedorov, Panagis Filippakopoulos, Paul E. Brennan, Vita Fedele, Sarah Martin, Sarah Picaud, Catherine Rogers, Mihir Parikh, Alexandria Taylor, Brian Samas, Alison O’Mahony, Ellen Berg, Gabriel Pallares, Adam D. Torrey, Daniel K. Treiber, Ivan J. Samardjiev, Brian T. Nasipak, Teresita Padilla-Benavides, Qiong Wu, Anthony N. Imbalzano, Jeffrey A. Nickerson, Mark E. Bunnage, Susanne Müller, Stefan Knapp & Dafydd R. Owen. (2016) Identification of a Chemical Probe for Family VIII Bromodomains through Optimization of a Fragment Hit. Journal of Medicinal Chemistry 59:10, pages 4800-4811.
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Laetitia J. Martin, Manfred Koegl, Gerd Bader, Xiao-Ling Cockcroft, Oleg Fedorov, Dennis Fiegen, Thomas Gerstberger, Marco H. Hofmann, Anja F. Hohmann, Dirk Kessler, Stefan Knapp, Petr Knesl, Stefan Kornigg, Susanne Müller, Herbert Nar, Catherine Rogers, Klaus Rumpel, Otmar Schaaf, Steffen Steurer, Cynthia Tallant, Christopher R. Vakoc, Markus Zeeb, Andreas Zoephel, Mark Pearson, Guido Boehmelt & Darryl McConnell. (2016) Structure-Based Design of an in Vivo Active Selective BRD9 Inhibitor. Journal of Medicinal Chemistry 59:10, pages 4462-4475.
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Panpan Lu, Xiying Qu, Yinzhong Shen, Zhengtao Jiang, Pengfei Wang, Hanxian Zeng, Haiyan Ji, Junxiao Deng, Xinyi Yang, Xian Li, Hongzhou Lu & Huanzhang Zhu. (2016) The BET inhibitor OTX015 reactivates latent HIV-1 through P-TEFb. Scientific Reports 6:1.
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Elena Ferri, Carlo Petosa & Charles E. McKenna. (2016) Bromodomains: Structure, function and pharmacology of inhibition. Biochemical Pharmacology 106, pages 1-18.
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Steven G. Smith & Ming-Ming Zhou. (2015) The Bromodomain: A New Target in Emerging Epigenetic Medicine. ACS Chemical Biology 11:3, pages 598-608.
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Natalie H. Theodoulou, Nicholas C. O. Tomkinson, Rab K. Prinjha & Philip G. Humphreys. (2016) Progress in the Development of non-BET Bromodomain Chemical Probes. ChemMedChem 11:5, pages 477-487.
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Wylie S. Palmer, Guillaume Poncet-Montange, Gang Liu, Alessia Petrocchi, Naphtali Reyna, Govindan Subramanian, Jay Theroff, Anne Yau, Maria Kost-Alimova, Jennifer P. Bardenhagen, Elisabetta Leo, Hannah E. Shepard, Trang N. Tieu, Xi Shi, Yanai Zhan, Shuping Zhao, Michelle C. Barton, Giulio Draetta, Carlo Toniatti, Philip Jones, Mary Geck Do & Jannik N. Andersen. (2015) Structure-Guided Design of IACS-9571, a Selective High-Affinity Dual TRIM24-BRPF1 Bromodomain Inhibitor. Journal of Medicinal Chemistry 59:4, pages 1440-1454.
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Natalie H. TheodoulouPaul BamboroughAndrew J. BannisterIsabelle Becher, Rino A. BitKa Hing CheChun-wa ChungAntje Dittmann, Gerard Drewes, David H. Drewry, Laurie GordonPaola Grandi, Melanie LeveridgeMatthew LindonAnne-Marie Michon, Judit MolnarSamuel C. RobsonNicholas C. O. TomkinsonTony KouzaridesRab K. PrinjhaPhilip G. Humphreys. (2015) Discovery of I-BRD9, a Selective Cell Active Chemical Probe for Bromodomain Containing Protein 9 Inhibition. Journal of Medicinal Chemistry 59:4, pages 1425-1439.
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Peiling Chen, Apirat Chaikuad, Paul Bamborough, Marcus Bantscheff, Chas Bountra, Chun-wa Chung, Oleg Fedorov, Paola Grandi, David Jung, Robert Lesniak, Matthew Lindon, Susanne Müller, Martin Philpott, Rab Prinjha, Catherine Rogers, Carolyn Selenski, Cynthia Tallant, Thilo Werner, Timothy M. Willson, Stefan Knapp & David H. Drewry. (2015) Discovery and Characterization of GSK2801, a Selective Chemical Probe for the Bromodomains BAZ2A and BAZ2B. Journal of Medicinal Chemistry 59:4, pages 1410-1424.
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Natalia Milosevich, Michael C. Gignac, James McFarlane, Chakravarthi Simhadri, Shanti Horvath, Kevin D. Daze, Caitlin S. Croft, Aman Dheri, Taylor T. H. Quon, Sarah F. Douglas, Jeremy E. Wulff, Irina Paci & Fraser Hof. (2015) Selective Inhibition of CBX6: A Methyllysine Reader Protein in the Polycomb Family. ACS Medicinal Chemistry Letters 7:2, pages 139-144.
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Moses Moustakim, Peter G. K. Clark, Duncan A. Hay, Darren J. Dixon & Paul E. Brennan. (2016) Chemical probes and inhibitors of bromodomains outside the BET family. MedChemComm 7:12, pages 2246-2264.
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Yanai Zhan, Maria Kost-Alimova, Xi Shi, Elisabetta Leo, Jennifer P. Bardenhagen, Hannah E. Shepard, Srikanth Appikonda, Bhavatarini Vangamudi, Shuping Zhao, Trang N. Tieu, Shiming Jiang, Timothy P. Heffernan, Joseph R. Marszalek, Carlo Toniatti, Giulio Draetta, Jessica Tyler, Michelle Barton, Philip Jones, Wylie S. Palmer, Mary K. Geck Do & Jannik N. Andersen. (2015) Development of novel cellular histone-binding and chromatin-displacement assays for bromodomain drug discovery. Epigenetics & Chromatin 8:1.
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Rosaria Benedetti, Mariarosaria Conte, Concetta Iside & Lucia Altucci. (2015) Epigenetic-based therapy: From single- to multi-target approaches. The International Journal of Biochemistry & Cell Biology 69, pages 121-131.
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Paul Butler, Michael Lawton, Robert E. Chapin, Brett D. Hollingshead, Karen Leach, Prashant R. Nambiar, Mathew Pletcher & Amy H. Yang. 2015. Epigenetics for Drug Discovery. Epigenetics for Drug Discovery 288 315 .
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