Articles - 4eqz mentioned but not cited (2)
- Mechanism of Cross-talk between H2B Ubiquitination and H3 Methylation by Dot1L. Worden EJ, Hoffmann NA, Hicks CW, Wolberger C. Cell 176 1490-1501.e12 (2019)
- Deep Neural Network Classifier for Virtual Screening Inhibitors of (S)-Adenosyl-L-Methionine (SAM)-Dependent Methyltransferase Family. Li F, Wan X, Xing J, Tan X, Li X, Wang Y, Zhao J, Wu X, Liu X, Li Z, Luo X, Lu W, Zheng M. Front Chem 7 324 (2019)
Reviews citing this publication (76)
- Histone deacetylases and their inhibitors in cancer, neurological diseases and immune disorders. Falkenberg KJ, Johnstone RW. Nat Rev Drug Discov 13 673-691 (2014)
- Chromatin proteins and modifications as drug targets. Helin K, Dhanak D. Nature 502 480-488 (2013)
- The PRMT5 arginine methyltransferase: many roles in development, cancer and beyond. Stopa N, Krebs JE, Shechter D. Cell Mol Life Sci 72 2041-2059 (2015)
- Targeting histone methyltransferases and demethylases in clinical trials for cancer therapy. Morera L, Lübbert M, Jung M. Clin Epigenetics 8 57 (2016)
- Targeting Transcription Factors for Cancer Treatment. Lambert M, Jambon S, Depauw S, David-Cordonnier MH. Molecules 23 E1479 (2018)
- Marked for death: targeting epigenetic changes in cancer. Pfister SX, Ashworth A. Nat Rev Drug Discov 16 241-263 (2017)
- Metabolic reprogramming and epigenetic modifications on the path to cancer. Sun L, Zhang H, Gao P. Protein Cell 13 877-919 (2022)
- Inhibitors of Protein Methyltransferases and Demethylases. Kaniskan HÜ, Martini ML, Jin J. Chem Rev 118 989-1068 (2018)
- Targeting histone lysine methylation in cancer. McGrath J, Trojer P. Pharmacol Ther 150 1-22 (2015)
- Targeting Epigenetics in Cancer. Bennett RL, Licht JD. Annu Rev Pharmacol Toxicol 58 187-207 (2018)
- SAM/SAH Analogs as Versatile Tools for SAM-Dependent Methyltransferases. Zhang J, Zheng YG. ACS Chem Biol 11 583-597 (2016)
- DOT1L and H3K79 Methylation in Transcription and Genomic Stability. Wood K, Tellier M, Murphy S. Biomolecules 8 E11 (2018)
- Applications of hydrogen/deuterium exchange MS from 2012 to 2014. Pirrone GF, Iacob RE, Engen JR. Anal Chem 87 99-118 (2015)
- Cancer epigenetics drug discovery and development: the challenge of hitting the mark. Campbell RM, Tummino PJ. J Clin Invest 124 64-69 (2014)
- Targeting histone methylation for cancer therapy: enzymes, inhibitors, biological activity and perspectives. Song Y, Wu F, Wu J. J Hematol Oncol 9 49 (2016)
- Metabolism, Biochemical Actions, and Chemical Synthesis of Anticancer Nucleosides, Nucleotides, and Base Analogs. Shelton J, Lu X, Hollenbaugh JA, Cho JH, Amblard F, Schinazi RF. Chem Rev 116 14379-14455 (2016)
- The emerging roles of DOT1L in leukemia and normal development. McLean CM, Karemaker ID, van Leeuwen F. Leukemia 28 2131-2138 (2014)
- Targeting DOT1L and HOX gene expression in MLL-rearranged leukemia and beyond. Chen CW, Armstrong SA. Exp Hematol 43 673-684 (2015)
- Small Molecule Inhibitors of Protein Arginine Methyltransferases. Hu H, Qian K, Ho MC, Zheng YG. Expert Opin Investig Drugs 25 335-358 (2016)
- DNA Methylation Targeting: The DNMT/HMT Crosstalk Challenge. Castillo-Aguilera O, Depreux P, Halby L, Arimondo PB, Goossens L. Biomolecules 7 E3 (2017)
- The histone methyltransferase Dot1/DOT1L as a critical regulator of the cell cycle. Kim W, Choi M, Kim JE. Cell Cycle 13 726-738 (2014)
- The upstreams and downstreams of H3K79 methylation by DOT1L. Vlaming H, van Leeuwen F. Chromosoma 125 593-605 (2016)
- Targeting the histone orthography of cancer: drugs for writers, erasers and readers. Simó-Riudalbas L, Esteller M. Br J Pharmacol 172 2716-2732 (2015)
- Recent progress toward epigenetic therapies: the example of mixed lineage leukemia. Neff T, Armstrong SA. Blood 121 4847-4853 (2013)
- A chemical probe toolbox for dissecting the cancer epigenome. Shortt J, Ott CJ, Johnstone RW, Bradner JE. Nat Rev Cancer 17 160-183 (2017)
- Epigenome-based personalized medicine in human cancer. Yan W, Herman JG, Guo M. Epigenomics 8 119-133 (2016)
- In focus: MLL-rearranged leukemia. de Boer J, Walf-Vorderwülbecke V, Williams O. Leukemia 27 1224-1228 (2013)
- Chromatin modifiers and the promise of epigenetic therapy in acute leukemia. Greenblatt SM, Nimer SD. Leukemia 28 1396-1406 (2014)
- Mixed lineage rearranged leukaemia: pathogenesis and targeting DOT1L. Stein EM, Tallman MS. Curr Opin Hematol 22 92-96 (2015)
- A medicinal chemistry perspective for targeting histone H3 lysine-79 methyltransferase DOT1L. Anglin JL, Song Y. J Med Chem 56 8972-8983 (2013)
- Mixed-Lineage Leukemia Fusions and Chromatin in Leukemia. Krivtsov AV, Hoshii T, Armstrong SA. Cold Spring Harb Perspect Med 7 a026658 (2017)
- Targeting epigenetic regulations in cancer. Ning B, Li W, Zhao W, Wang R. Acta Biochim Biophys Sin (Shanghai) 48 97-109 (2016)
- Structural biology and chemistry of protein arginine methyltransferases. Schapira M, Ferreira de Freitas R. Medchemcomm 5 1779-1788 (2014)
- Targeting human SET1/MLL family of proteins. Vedadi M, Blazer L, Eram MS, Barsyte-Lovejoy D, Arrowsmith CH, Hajian T. Protein Sci 26 662-676 (2017)
- Epigenetic Modifications in Acute Myeloid Leukemia: Prognosis, Treatment, and Heterogeneity. Goldman SL, Hassan C, Khunte M, Soldatenko A, Jong Y, Afshinnekoo E, Mason CE. Front Genet 10 133 (2019)
- Prostate Cancer: Epigenetic Alterations, Risk Factors, and Therapy. Kgatle MM, Kalla AA, Islam MM, Sathekge M, Moorad R. Prostate Cancer 2016 5653862 (2016)
- Chemical probes of histone lysine methyltransferases. Kaniskan HÜ, Jin J. ACS Chem Biol 10 40-50 (2015)
- Targeting histone methyltransferase and demethylase in acute myeloid leukemia therapy. Castelli G, Pelosi E, Testa U. Onco Targets Ther 11 131-155 (2018)
- Epigenetic regulators and their impact on therapy in acute myeloid leukemia. Pastore F, Levine RL. Haematologica 101 269-278 (2016)
- Next-Generation Drugs and Probes for Chromatin Biology: From Targeted Protein Degradation to Phase Separation. Cermakova K, Hodges HC. Molecules 23 E1958 (2018)
- Epigenetic targets and drug discovery: part 1: histone methylation. Liu Y, Liu K, Qin S, Xu C, Min J. Pharmacol Ther 143 275-294 (2014)
- Pyrrolo[2,3-d]pyrimidine (7-deazapurine) as a privileged scaffold in design of antitumor and antiviral nucleosides. Perlíková P, Hocek M. Med Res Rev 37 1429-1460 (2017)
- Chemical Inhibition of Protein Methyltransferases. Schapira M. Cell Chem Biol 23 1067-1076 (2016)
- DOT1L: a key target in normal chromatin remodelling and in mixed-lineage leukaemia treatment. Sarno F, Nebbioso A, Altucci L. Epigenetics 15 439-453 (2020)
- Open access chemical probes for epigenetic targets. Brown PJ, Müller S. Future Med Chem 7 1901-1917 (2015)
- Inhibitors of emerging epigenetic targets for cancer therapy: a patent review (2010-2014). Tanaka M, Roberts JM, Qi J, Bradner JE. Pharm Pat Anal 4 261-284 (2015)
- Methyltransferase Inhibitors: Competing with, or Exploiting the Bound Cofactor. Ferreira de Freitas R, Ivanochko D, Schapira M. Molecules 24 E4492 (2019)
- Preclinical Pharmacokinetics and Pharmacodynamics of Pinometostat (EPZ-5676), a First-in-Class, Small Molecule S-Adenosyl Methionine Competitive Inhibitor of DOT1L. Waters NJ. Eur J Drug Metab Pharmacokinet 42 891-901 (2017)
- Small molecule epigenetic inhibitors targeted to histone lysine methyltransferases and demethylases. Wang Z, Patel DJ. Q Rev Biophys 46 349-373 (2013)
- Structure, function and inhibition of critical protein-protein interactions involving mixed lineage leukemia 1 and its fusion oncoproteins. Li X, Song Y. J Hematol Oncol 14 56 (2021)
- Direct and Indirect Targeting of HOXA9 Transcription Factor in Acute Myeloid Leukemia. Lambert M, Alioui M, Jambon S, Depauw S, Van Seuningen I, David-Cordonnier MH. Cancers (Basel) 11 E837 (2019)
- Targeting protein methylation: from chemical tools to precision medicines. Dilworth D, Barsyte-Lovejoy D. Cell Mol Life Sci 76 2967-2985 (2019)
- Epigenetic modifiers in normal and malignant hematopoiesis. Haladyna JN, Yamauchi T, Neff T, Bernt KM, Bernt KM. Epigenomics 7 301-320 (2015)
- Metabolic Fuel for Epigenetic: Nuclear Production Meets Local Consumption. Boon R. Front Genet 12 768996 (2021)
- Tackling malignant melanoma epigenetically: histone lysine methylation. Orouji E, Utikal J. Clin Epigenetics 10 145 (2018)
- Pharmacologic Targeting of Chromatin Modulators As Therapeutics of Acute Myeloid Leukemia. Lu R, Wang GG. Front Oncol 7 241 (2017)
- An Update of Epigenetic Drugs for the Treatment of Cancers and Brain Diseases: A Comprehensive Review. Sahafnejad Z, Ramazi S, Allahverdi A. Genes (Basel) 14 873 (2023)
- Chemical probes targeting epigenetic proteins: Applications beyond oncology. Ackloo S, Brown PJ, Müller S. Epigenetics 12 378-400 (2017)
- Epigenetic pathway targets for the treatment of disease: accelerating progress in the development of pharmacological tools: IUPHAR Review 11. Tough DF, Lewis HD, Rioja I, Lindon MJ, Prinjha RK. Br J Pharmacol 171 4981-5010 (2014)
- Inhibitors of protein methyltransferases as chemical tools. Luo M. Epigenomics 7 1327-1338 (2015)
- Methyltransferase inhibitors for modulation of the epigenome and beyond. Schapira M, Arrowsmith CH. Curr Opin Chem Biol 33 81-87 (2016)
- Aberrant Activity of Histone-Lysine N-Methyltransferase 2 (KMT2) Complexes in Oncogenesis. Poreba E, Lesniewicz K, Durzynska J. Int J Mol Sci 21 E9340 (2020)
- Disturbing the histone code in leukemia: translocations and mutations affecting histone methyl transferases. Chopra M, Bohlander SK. Cancer Genet 208 192-205 (2015)
- Importance of epigenetic changes in cancer etiology, pathogenesis, clinical profiling, and treatment: what can be learned from hematologic malignancies? Vecchio L, Seke Etet PF, Kipanyula MJ, Krampera M, Nwabo Kamdje AH. Biochim Biophys Acta 1836 90-104 (2013)
- Mutations in epigenetic modifiers in acute myeloid leukemia and their clinical utility. Hou HA, Tien HF. Expert Rev Hematol 9 447-469 (2016)
- Cell-based assays to support the profiling of small molecules with histone methyltransferase and demethylase modulatory activity. Martinez NJ, Simeonov A. Drug Discov Today Technol 18 9-17 (2015)
- Connecting the DOTs on Cell Identity. Wille CK, Sridharan R. Front Cell Dev Biol 10 906713 (2022)
- Exploring Methods of Targeting Histone Methyltransferases and Their Applications in Cancer Therapeutics. Wang MY, Liow P, Guzman MIT, Qi J. ACS Chem Biol 17 744-755 (2022)
- Chemogenomics for drug discovery: clinical molecules from open access chemical probes. Quinlan RBA, Brennan PE. RSC Chem Biol 2 759-795 (2021)
- Synthesis of lysine methyltransferase inhibitors. Hui C, Ye T. Front Chem 3 44 (2015)
- Role of HOXA9 in solid tumors: mechanistic insights and therapeutic potential. Tang L, Peng L, Tan C, Liu H, Chen P, Wang H. Cancer Cell Int 22 349 (2022)
- Cell fate conversion-from the viewpoint of small molecules and lineage specifiers. Zhao T, Li Y, Deng H. Diabetes Obes Metab 18 Suppl 1 3-9 (2016)
- Novel insights into histone lysine methyltransferases in cancer therapy: From epigenetic regulation to selective drugs. Liao Q, Yang J, Ge S, Chai P, Fan J, Jia R. J Pharm Anal 13 127-141 (2023)
- Collateral Victim or Rescue Worker?-The Role of Histone Methyltransferases in DNA Damage Repair and Their Targeting for Therapeutic Opportunities in Cancer. He L, Lomberk G. Front Cell Dev Biol 9 735107 (2021)
- Epimutations and Their Effect on Chromatin Organization: Exciting Avenues for Cancer Treatment. Mohammad A, Jha S. Cancers (Basel) 15 215 (2022)
- Novel approaches to pediatric leukemia treatment. Thomas X. Expert Rev Anticancer Ther 15 811-828 (2015)
Articles citing this publication (91)
- Potent inhibition of DOT1L as treatment of MLL-fusion leukemia. Daigle SR, Olhava EJ, Therkelsen CA, Basavapathruni A, Jin L, Boriack-Sjodin PA, Allain CJ, Klaus CR, Raimondi A, Scott MP, Waters NJ, Chesworth R, Moyer MP, Copeland RA, Richon VM, Pollock RM. Blood 122 1017-1025 (2013)
- An orally bioavailable chemical probe of the Lysine Methyltransferases EZH2 and EZH1. Konze KD, Ma A, Li F, Barsyte-Lovejoy D, Parton T, Macnevin CJ, Liu F, Gao C, Huang XP, Kuznetsova E, Rougie M, Jiang A, Pattenden SG, Norris JL, James LI, Roth BL, Brown PJ, Frye SV, Arrowsmith CH, Hahn KM, Wang GG, Vedadi M, Jin J. ACS Chem Biol 8 1324-1334 (2013)
- IL-22(+)CD4(+) T cells promote colorectal cancer stemness via STAT3 transcription factor activation and induction of the methyltransferase DOT1L. Kryczek I, Lin Y, Nagarsheth N, Peng D, Zhao L, Zhao E, Vatan L, Szeliga W, Dou Y, Owens S, Zgodzinski W, Majewski M, Wallner G, Fang J, Huang E, Zou W. Immunity 40 772-784 (2014)
- Pharmacological targeting of the Wdr5-MLL interaction in C/EBPα N-terminal leukemia. Grebien F, Vedadi M, Getlik M, Giambruno R, Grover A, Avellino R, Skucha A, Vittori S, Kuznetsova E, Smil D, Barsyte-Lovejoy D, Li F, Poda G, Schapira M, Wu H, Dong A, Senisterra G, Stukalov A, Huber KVM, Schönegger A, Marcellus R, Bilban M, Bock C, Brown PJ, Zuber J, Bennett KL, Al-Awar R, Delwel R, Nerlov C, Arrowsmith CH, Superti-Furga G. Nat Chem Biol 11 571-578 (2015)
- DOT1L inhibits SIRT1-mediated epigenetic silencing to maintain leukemic gene expression in MLL-rearranged leukemia. Chen CW, Koche RP, Sinha AU, Deshpande AJ, Zhu N, Eng R, Doench JG, Xu H, Chu SH, Qi J, Wang X, Delaney C, Bernt KM, Bernt KM, Root DE, Hahn WC, Bradner JE, Armstrong SA. Nat Med 21 335-343 (2015)
- Discovery of an in vivo chemical probe of the lysine methyltransferases G9a and GLP. Liu F, Barsyte-Lovejoy D, Li F, Xiong Y, Korboukh V, Huang XP, Allali-Hassani A, Janzen WP, Roth BL, Frye SV, Arrowsmith CH, Brown PJ, Vedadi M, Jin J. J Med Chem 56 8931-8942 (2013)
- Structural Basis of Dot1L Stimulation by Histone H2B Lysine 120 Ubiquitination. Valencia-Sánchez MI, De Ioannes P, Wang M, Vasilyev N, Chen R, Nudler E, Armache JP, Armache KJ. Mol Cell 74 1010-1019.e6 (2019)
- Functional interdependence of BRD4 and DOT1L in MLL leukemia. Gilan O, Lam EY, Becher I, Lugo D, Cannizzaro E, Joberty G, Ward A, Wiese M, Fong CY, Ftouni S, Tyler D, Stanley K, MacPherson L, Weng CF, Chan YC, Ghisi M, Smil D, Carpenter C, Brown P, Garton N, Blewitt ME, Bannister AJ, Kouzarides T, Huntly BJ, Johnstone RW, Drewes G, Dawson SJ, Arrowsmith CH, Grandi P, Prinjha RK, Dawson MA. Nat Struct Mol Biol 23 673-681 (2016)
- Selective inhibitors of protein methyltransferases. Kaniskan HÜ, Konze KD, Jin J. J Med Chem 58 1596-1629 (2015)
- LLY-283, a Potent and Selective Inhibitor of Arginine Methyltransferase 5, PRMT5, with Antitumor Activity. Bonday ZQ, Cortez GS, Grogan MJ, Antonysamy S, Weichert K, Bocchinfuso WP, Li F, Kennedy S, Li B, Mader MM, Arrowsmith CH, Brown PJ, Eram MS, Szewczyk MM, Barsyte-Lovejoy D, Vedadi M, Guccione E, Campbell RM. ACS Med Chem Lett 9 612-617 (2018)
- Pharmacological inhibition of LSD1 for the treatment of MLL-rearranged leukemia. Feng Z, Yao Y, Zhou C, Chen F, Wu F, Wei L, Liu W, Dong S, Redell M, Mo Q, Song Y. J Hematol Oncol 9 24 (2016)
- C/EBPβ enhances platinum resistance of ovarian cancer cells by reprogramming H3K79 methylation. Liu D, Zhang XX, Li MC, Cao CH, Wan DY, Xi BX, Tan JH, Wang J, Yang ZY, Feng XX, Ye F, Chen G, Wu P, Xi L, Wang H, Zhou JF, Feng ZH, Ma D, Gao QL. Nat Commun 9 1739 (2018)
- Complementary activities of DOT1L and Menin inhibitors in MLL-rearranged leukemia. Dafflon C, Craig VJ, Méreau H, Gräsel J, Schacher Engstler B, Hoffman G, Nigsch F, Gaulis S, Barys L, Ito M, Aguadé-Gorgorió J, Bornhauser B, Bourquin JP, Proske A, Stork-Fux C, Murakami M, Sellers WR, Hofmann F, Schwaller J, Tiedt R. Leukemia 31 1269-1277 (2017)
- A chemical biology toolbox to study protein methyltransferases and epigenetic signaling. Scheer S, Ackloo S, Medina TS, Schapira M, Li F, Ward JA, Lewis AM, Northrop JP, Richardson PL, Kaniskan HÜ, Shen Y, Liu J, Smil D, McLeod D, Zepeda-Velazquez CA, Luo M, Jin J, Barsyte-Lovejoy D, Huber KVM, De Carvalho DD, Vedadi M, Zaph C, Brown PJ, Arrowsmith CH. Nat Commun 10 19 (2019)
- Inhibition of histone methyltransferase DOT1L silences ERα gene and blocks proliferation of antiestrogen-resistant breast cancer cells. Nassa G, Salvati A, Tarallo R, Gigantino V, Alexandrova E, Memoli D, Sellitto A, Rizzo F, Malanga D, Mirante T, Morelli E, Nees M, Åkerfelt M, Kangaspeska S, Nyman TA, Milanesi L, Giurato G, Weisz A. Sci Adv 5 eaav5590 (2019)
- Discovery of a Dual PRMT5-PRMT7 Inhibitor. Smil D, Eram MS, Li F, Kennedy S, Szewczyk MM, Brown PJ, Barsyte-Lovejoy D, Arrowsmith CH, Vedadi M, Schapira M. ACS Med Chem Lett 6 408-412 (2015)
- Inhibition of histone H3K79 methylation selectively inhibits proliferation, self-renewal and metastatic potential of breast cancer. Zhang L, Deng L, Chen F, Yao Y, Wu B, Wei L, Mo Q, Song Y. Oncotarget 5 10665-10677 (2014)
- Discovery of a selective, substrate-competitive inhibitor of the lysine methyltransferase SETD8. Ma A, Yu W, Li F, Bleich RM, Herold JM, Butler KV, Norris JL, Korboukh V, Tripathy A, Janzen WP, Arrowsmith CH, Frye SV, Vedadi M, Brown PJ, Jin J. J Med Chem 57 6822-6833 (2014)
- Pharmacological inhibition of PRMT7 links arginine monomethylation to the cellular stress response. Szewczyk MM, Ishikawa Y, Organ S, Sakai N, Li F, Halabelian L, Ackloo S, Couzens AL, Eram M, Dilworth D, Fukushi H, Harding R, Dela Seña CC, Sugo T, Hayashi K, McLeod D, Zepeda C, Aman A, Sánchez-Osuna M, Bonneil E, Takagi S, Al-Awar R, Tyers M, Richard S, Takizawa M, Gingras AC, Arrowsmith CH, Vedadi M, Brown PJ, Nara H, Barsyte-Lovejoy D. Nat Commun 11 2396 (2020)
- Nucleosome Turnover Regulates Histone Methylation Patterns over the Genome. Chory EJ, Calarco JP, Hathaway NA, Bell O, Neel DS, Crabtree GR. Mol Cell 73 61-72.e3 (2019)
- Probing the SAM Binding Site of SARS-CoV-2 Nsp14 In Vitro Using SAM Competitive Inhibitors Guides Developing Selective Bisubstrate Inhibitors. Devkota K, Schapira M, Perveen S, Khalili Yazdi A, Li F, Chau I, Ghiabi P, Hajian T, Loppnau P, Bolotokova A, Satchell KJF, Wang K, Li D, Liu J, Smil D, Luo M, Jin J, Fish PV, Brown PJ, Vedadi M. SLAS Discov 26 1200-1211 (2021)
- MLL leukemia induction by genome editing of human CD34+ hematopoietic cells. Buechele C, Breese EH, Schneidawind D, Lin CH, Jeong J, Duque-Afonso J, Wong SH, Smith KS, Negrin RS, Porteus M, Cleary ML. Blood 126 1683-1694 (2015)
- Bromo-deaza-SAH: a potent and selective DOT1L inhibitor. Yu W, Smil D, Li F, Tempel W, Fedorov O, Nguyen KT, Bolshan Y, Al-Awar R, Knapp S, Arrowsmith CH, Vedadi M, Brown PJ, Schapira M. Bioorg Med Chem 21 1787-1794 (2013)
- Small-molecule ligands of methyl-lysine binding proteins: optimization of selectivity for L3MBTL3. James LI, Korboukh VK, Krichevsky L, Baughman BM, Herold JM, Norris JL, Jin J, Kireev DB, Janzen WP, Arrowsmith CH, Frye SV. J Med Chem 56 7358-7371 (2013)
- The histone methyltransferase DOT1L: regulatory functions and a cancer therapy target. Wong M, Polly P, Liu T. Am J Cancer Res 5 2823-2837 (2015)
- 3-(Piperidin-4-ylmethoxy)pyridine Containing Compounds Are Potent Inhibitors of Lysine Specific Demethylase 1. Wu F, Zhou C, Yao Y, Wei L, Feng Z, Deng L, Song Y. J Med Chem 59 253-263 (2016)
- Discovery of Novel Dot1L Inhibitors through a Structure-Based Fragmentation Approach. Chen C, Zhu H, Stauffer F, Caravatti G, Vollmer S, Machauer R, Holzer P, Möbitz H, Scheufler C, Klumpp M, Tiedt R, Beyer KS, Calkins K, Guthy D, Kiffe M, Zhang J, Gaul C. ACS Med Chem Lett 7 735-740 (2016)
- Crystal structures of the human histone H4K20 methyltransferases SUV420H1 and SUV420H2. Wu H, Siarheyeva A, Zeng H, Lam R, Dong A, Wu XH, Li Y, Schapira M, Vedadi M, Min J. FEBS Lett 587 3859-3868 (2013)
- Mll-AF4 Confers Enhanced Self-Renewal and Lymphoid Potential during a Restricted Window in Development. Barrett NA, Malouf C, Kapeni C, Bacon WA, Giotopoulos G, Jacobsen SEW, Huntly BJ, Ottersbach K. Cell Rep 16 1039-1054 (2016)
- DOT1L Activity Promotes Proliferation and Protects Cortical Neural Stem Cells from Activation of ATF4-DDIT3-Mediated ER Stress In Vitro. Roidl D, Hellbach N, Bovio PP, Villarreal A, Heidrich S, Nestel S, Grüning BA, Boenisch U, Vogel T. Stem Cells 34 233-245 (2016)
- Silencing or inhibition of H3K79 methyltransferase DOT1L induces cell cycle arrest by epigenetically modulating c-Myc expression in colorectal cancer. Yang L, Lei Q, Li L, Yang J, Dong Z, Cui H. Clin Epigenetics 11 199 (2019)
- Synthesis, Activity and Metabolic Stability of Non-Ribose Containing Inhibitors of Histone Methyltransferase DOT1L. Deng L, Zhang L, Yao Y, Wang C, Redell MS, Dong S, Song Y. Medchemcomm 4 822-826 (2013)
- Th22 cells control colon tumorigenesis through STAT3 and Polycomb Repression complex 2 signaling. Sun D, Lin Y, Hong J, Chen H, Nagarsheth N, Peng D, Wei S, Huang E, Fang J, Kryczek I, Zou W. Oncoimmunology 5 e1082704 (2016)
- Functional interrogation of HOXA9 regulome in MLLr leukemia via reporter-based CRISPR/Cas9 screen. Zhang H, Zhang Y, Zhou X, Wright S, Hyle J, Zhao L, An J, Zhao X, Shao Y, Xu B, Lee HM, Chen T, Zhou Y, Chen X, Lu R, Li C. Elife 9 e57858 (2020)
- Loss of Histone H3 K79 Methyltransferase Dot1l Facilitates Kidney Fibrosis by Upregulating Endothelin 1 through Histone Deacetylase 2. Zhang L, Chen L, Gao C, Chen E, Lightle AR, Foulke L, Zhao B, Higgins PJ, Zhang W. J Am Soc Nephrol 31 337-349 (2020)
- Crystal structure of arginine methyltransferase 6 from Trypanosoma brucei. Wang C, Zhu Y, Chen J, Li X, Peng J, Chen J, Zou Y, Zhang Z, Jin H, Yang P, Wu J, Niu L, Gong Q, Teng M, Shi Y. PLoS One 9 e87267 (2014)
- Mitotic accumulation of dimethylated lysine 79 of histone H3 is important for maintaining genome integrity during mitosis in human cells. Guppy BJ, McManus KJ. Genetics 199 423-433 (2015)
- DOT1L complex regulates transcriptional initiation in human erythroleukemic cells. Wu A, Zhi J, Tian T, Cihan A, Cevher MA, Liu Z, David Y, Muir TW, Roeder RG, Yu M. Proc Natl Acad Sci U S A 118 e2106148118 (2021)
- HEDD: the human epigenetic drug database. Qi Y, Wang D, Wang D, Jin T, Yang L, Wu H, Li Y, Zhao J, Du F, Song M, Wang R. Database (Oxford) 2016 baw159 (2016)
- RE-IIBP Methylates H3K79 and Induces MEIS1-mediated Apoptosis via H2BK120 Ubiquitination by RNF20. Woo Park J, Kim KB, Kim JY, Chae YC, Jeong OS, Seo SB. Sci Rep 5 12485 (2015)
- A critical role for CRM1 in regulating HOXA gene transcription in CALM-AF10 leukemias. Conway AE, Haldeman JM, Wechsler DS, Lavau CP. Leukemia 29 423-432 (2015)
- DOT1L inhibition blocks multiple myeloma cell proliferation by suppressing IRF4-MYC signaling. Ishiguro K, Kitajima H, Niinuma T, Ishida T, Maruyama R, Ikeda H, Hayashi T, Sasaki H, Wakasugi H, Nishiyama K, Shindo T, Yamamoto E, Kai M, Sasaki Y, Tokino T, Nakase H, Suzuki H. Haematologica 104 155-165 (2019)
- Discovery of Potent, Selective, and Structurally Novel Dot1L Inhibitors by a Fragment Linking Approach. Möbitz H, Machauer R, Holzer P, Vaupel A, Stauffer F, Ragot C, Caravatti G, Scheufler C, Fernandez C, Hommel U, Tiedt R, Beyer KS, Chen C, Zhu H, Gaul C. ACS Med Chem Lett 8 338-343 (2017)
- DOT1L inhibition attenuates graft-versus-host disease by allogeneic T cells in adoptive immunotherapy models. Kagoya Y, Nakatsugawa M, Saso K, Guo T, Anczurowski M, Wang CH, Butler MO, Arrowsmith CH, Hirano N. Nat Commun 9 1915 (2018)
- High-resolution characterization of gene function using single-cell CRISPR tiling screen. Yang L, Chan AKN, Miyashita K, Delaney CD, Wang X, Li H, Pokharel SP, Li S, Li M, Xu X, Lu W, Liu Q, Mattson N, Chen KY, Wang J, Yuan YC, Horne D, Rosen ST, Soto-Feliciano Y, Feng Z, Hoshii T, Xiao G, Müschen M, Chen J, Armstrong SA, Chen CW. Nat Commun 12 4063 (2021)
- Prevalence and architecture of posttranscriptionally impaired synonymous mutations in 8,320 genomes across 22 cancer types. Teng H, Wei W, Li Q, Xue M, Shi X, Li X, Mao F, Sun Z. Nucleic Acids Res 48 1192-1205 (2020)
- Structure-activity relationship studies of SETD8 inhibitors. Ma A, Yu W, Xiong Y, Butler KV, Brown PJ, Jin J. Medchemcomm 5 1892-1898 (2014)
- Metabolism and disposition of the DOT1L inhibitor, pinometostat (EPZ-5676), in rat, dog and human. Waters NJ, Smith SA, Olhava EJ, Duncan KW, Burton RD, O'Neill J, Rodrigue ME, Pollock RM, Moyer MP, Chesworth R. Cancer Chemother Pharmacol 77 43-62 (2016)
- Discovery of SARS-CoV-2 Nsp14 and Nsp16 Methyltransferase Inhibitors by High-Throughput Virtual Screening. Bobrovs R, Kanepe I, Narvaiss N, Patetko L, Kalnins G, Sisovs M, Bula AL, Grinberga S, Boroduskis M, Ramata-Stunda A, Rostoks N, Jirgensons A, Tars K, Jaudzems K. Pharmaceuticals (Basel) 14 1243 (2021)
- Structure-guided DOT1L probe optimization by label-free ligand displacement. Yi JS, Federation AJ, Qi J, Dhe-Paganon S, Hadler M, Xu X, St Pierre R, Varca AC, Wu L, Marineau JJ, Smith WB, Souza A, Chory EJ, Armstrong SA, Bradner JE. ACS Chem Biol 10 667-674 (2015)
- Targeted drug discovery for pediatric leukemia. Napper AD, Watson VG. Front Oncol 3 170 (2013)
- Dot1 histone methyltransferases share a distributive mechanism but have highly diverged catalytic properties. Stulemeijer IJ, De Vos D, van Harten K, Joshi OK, Blomberg O, van Welsem T, Terweij M, Vlaming H, de Graaf EL, Altelaar AF, Bakker BM, van Leeuwen F. Sci Rep 5 9824 (2015)
- Emerging Epigenetic Therapeutic Targets in Acute Myeloid Leukemia. Wingelhofer B, Somervaille TCP. Front Oncol 9 850 (2019)
- Hydrogen deuterium exchange defines catalytically linked regions of protein flexibility in the catechol O-methyltransferase reaction. Zhang J, Balsbaugh JL, Gao S, Ahn NG, Klinman JP. Proc Natl Acad Sci U S A 117 10797-10805 (2020)
- Structural Insights into Substrate Recognition and Catalysis in Outer Membrane Protein B (OmpB) by Protein-lysine Methyltransferases from Rickettsia. Abeykoon AH, Noinaj N, Choi BE, Wise L, He Y, Chao CC, Wang G, Gucek M, Ching WM, Chock PB, Buchanan SK, Yang DC. J Biol Chem 291 19962-19974 (2016)
- In Situ Proteome Profiling and Bioimaging Applications of Small-Molecule Affinity-Based Probes Derived From DOT1L Inhibitors. Zhu B, Zhang H, Pan S, Wang C, Ge J, Lee JS, Yao SQ. Chemistry 22 7824-7836 (2016)
- Open access target validation is a more efficient way to accelerate drug discovery. Lee WH. PLoS Biol 13 e1002164 (2015)
- Analogs of S-Adenosyl-L-Methionine in Studies of Methyltransferases. Rudenko AY, Mariasina SS, Sergiev PV, Polshakov VI. Mol Biol 56 229-250 (2022)
- Non-canonical H3K79me2-dependent pathways promote the survival of MLL-rearranged leukemia. Richter WF, Shah RN, Ruthenburg AJ. Elife 10 e64960 (2021)
- Editorial Challenges in developing novel DNA methyltransferases inhibitors for cancer therapy. Guianvarc'h D, Arimondo PB. Future Med Chem 6 1237-1240 (2014)
- DOT1L inhibition is lethal for multiple myeloma due to perturbation of the endoplasmic reticulum stress pathway. Dafflon C, Gaulis S, Barys L, Kapur K, Cornacchione V, Schukur L, Bergling S, Traggiai E, Jansky S, Hellmann L, Engstler BS, Kerr G, de Weck A, Ruddy DA, Naumann U, Stauffer F, Gaul C, Lin Y, Billy E, Weiss A, Hofmann F, Ito M, Tiedt R. Oncotarget 11 956-968 (2020)
- Disruptor of telomeric silencing 1-like (DOT1L): disclosing a new class of non-nucleoside inhibitors by means of ligand-based and structure-based approaches. Sabatino M, Rotili D, Patsilinakos A, Forgione M, Tomaselli D, Alby F, Arimondo PB, Mai A, Ragno R. J Comput Aided Mol Des 32 435-458 (2018)
- Disruptor of telomeric silencing 1-like promotes ovarian cancer tumor growth by stimulating pro-tumorigenic metabolic pathways and blocking apoptosis. Chava S, Bugide S, Edwards YJK, Gupta R. Oncogenesis 10 48 (2021)
- Identification of a peptide inhibitor for the histone methyltransferase WHSC1. Morrison MJ, Boriack-Sjodin PA, Swinger KK, Wigle TJ, Sadalge D, Kuntz KW, Scott MP, Janzen WP, Chesworth R, Duncan KW, Harvey DM, Lampe JW, Mitchell LH, Copeland RA. PLoS One 13 e0197082 (2018)
- The Cks1/Cks2 axis fine-tunes Mll1 expression and is crucial for MLL-rearranged leukaemia cell viability. Grey W, Ivey A, Milne TA, Haferlach T, Grimwade D, Uhlmann F, Voisset E, Yu V. Biochim Biophys Acta Mol Cell Res 1865 105-116 (2018)
- DOT1L inhibition enhances pluripotency beyond acquisition of epithelial identity and without immediate suppression of the somatic transcriptome. Wille CK, Sridharan R. Stem Cell Reports 17 384-396 (2022)
- Elucidating the Importance of DOT1L Recruitment in MLL-AF9 Leukemia and Hematopoiesis. Grigsby SM, Friedman A, Chase J, Waas B, Ropa J, Serio J, Shen C, Muntean AG, Maillard I, Nikolovska-Coleska Z. Cancers (Basel) 13 642 (2021)
- Identification of DOT1L inhibitors by structure-based virtual screening adapted from a nucleoside-focused library. Gibbons GS, Chakraborty A, Grigsby SM, Umeano AC, Liao C, Moukha-Chafiq O, Pathak V, Mathew B, Lee YT, Dou Y, Schürer SC, Reynolds RC, Snowden TS, Nikolovska-Coleska Z. Eur J Med Chem 189 112023 (2020)
- Turning a Substrate Peptide into a Potent Inhibitor for the Histone Methyltransferase SETD8. Judge RA, Zhu H, Upadhyay AK, Bodelle PM, Hutchins CW, Torrent M, Marin VL, Yu W, Vedadi M, Li F, Brown PJ, Pappano WN, Sun C, Petros AM. ACS Med Chem Lett 7 1102-1106 (2016)
- Antecedent chromatin organization determines cGAS recruitment to ruptured micronuclei. MacDonald KM, Nicholson-Puthenveedu S, Tageldein MM, Khasnis S, Arrowsmith CH, Harding SM. Nat Commun 14 556 (2023)
- Repurposing epigenetic inhibitors to target the Clostridioides difficile-specific DNA adenine methyltransferase and sporulation regulator CamA. Zhou J, Horton JR, Yu D, Ren R, Blumenthal RM, Zhang X, Cheng X. Epigenetics 17 970-981 (2022)
- Transcription factor MEF2D is required for the maintenance of MLL-rearranged acute myeloid leukemia. Zhao L, Zhang P, Galbo PM, Zhou X, Aryal S, Qiu S, Zhang H, Zhou Y, Li C, Zheng D, Bhatia R, Lu R. Blood Adv 5 4727-4740 (2021)
- Structural diversity of the epigenetics pocketome. Cabaye A, Nguyen KT, Liu L, Pande V, Schapira M. Proteins 83 1316-1326 (2015)
- Synthesis and Biological Activity of a Cytostatic Inhibitor of MLLr Leukemia Targeting the DOT1L Protein. Bon C, Si Y, Pernak M, Barbachowska M, Levi-Acobas E, Cadet Daniel V, Jallet C, Ruzic D, Djokovic N, Djikić T, Nikolic K, Halby L, Arimondo PB. Molecules 26 5300 (2021)
- Synthesis of a 3'-C-ethynyl-β-d-ribofuranose purine nucleoside library: Discovery of C7-deazapurine analogs as potent antiproliferative nucleosides. Hulpia F, Noppen S, Schols D, Andrei G, Snoeck R, Liekens S, Vervaeke P, Van Calenbergh S. Eur J Med Chem 157 248-267 (2018)
- Antiproliferative and Antimigration Activities of Fluoro-Neplanocin A via Inhibition of Histone H3 Methylation in Triple-Negative Breast Cancer. Byun WS, Kim WK, Yoon JS, Jarhad DB, Jeong LS, Lee SK. Biomolecules 10 E530 (2020)
- DOT1L bridges transcription and heterochromatin formation at mammalian pericentromeres. Malla AB, Yu H, Farris D, Kadimi S, Lam TT, Cox AL, Smith ZD, Lesch BJ. EMBO Rep 24 e56492 (2023)
- The mechanism of MYB transcriptional regulation by MLL-AF9 oncoprotein. Cao L, Mitra P, Gonda TJ. Sci Rep 9 20084 (2019)
- Combining small molecules for cell reprogramming through an interatomic analysis. Feltes BC, Bonatto D, Bonatto D. Mol Biosyst 9 2741-2763 (2013)
- Epigenetic drug library screening reveals targeting DOT1L abrogates NAD+ synthesis by reprogramming H3K79 methylation in uveal melanoma. Gu X, Hua Y, Yu J, Yang L, Ge S, Jia R, Chai P, Zhuang A, Fan X. J Pharm Anal 13 24-38 (2023)
- Histone Methyltransferase DOT1L is Involved in Larval Molting and Second Stage Nymphal Feeding in Ornithodoros Moubata. Gobl J, Kumar Sinha D, Sima R, Perner J, Kopáček P, Valdés JJ, Rego ROM, Cabezas-Cruz A. Vaccines (Basel) 8 E157 (2020)
- An efficient method for the synthesis of selenium modified nucleosides: its application in the synthesis of Se-adenosyl-L-selenomethionine (SeAM). Kogami M, Koketsu M. Org Biomol Chem 13 9405-9417 (2015)
- DOT1L is a barrier to histone acetylation during reprogramming to pluripotency. Wille CK, Zhang X, Haws SA, Denu JM, Sridharan R. Sci Adv 9 eadf3980 (2023)
- DOT1L promotes cell proliferation and invasion by epigenetically regulating STAT5B in renal cell carcinoma. Hou Y, Huang S, Liu J, Wang L, Yuan Y, Liu H, Weng X, Chen Z, Hu J, Liu X. Am J Cancer Res 13 276-292 (2023)
- Mechanistic basis of the increased methylation activity of the SETD2 protein lysine methyltransferase towards a designed super-substrate peptide. Schnee P, Choudalakis M, Weirich S, Khella MS, Carvalho H, Pleiss J, Jeltsch A. Commun Chem 5 139 (2022)
- A unique binding pocket induced by a noncanonical SAH mimic to develop potent and selective PRMT inhibitors. Deng Y, Song X, Iyamu ID, Dong A, Min J, Huang R. Acta Pharm Sin B 13 4893-4905 (2023)
- Comparative Study of Adenosine Analogs as Inhibitors of Protein Arginine Methyltransferases and a Clostridioides difficile-Specific DNA Adenine Methyltransferase. Zhou J, Deng Y, Iyamu ID, Horton JR, Yu D, Hajian T, Vedadi M, Rotili D, Mai A, Blumenthal RM, Zhang X, Huang R, Cheng X. ACS Chem Biol 18 734-745 (2023)
- DOT1L interaction partner AF10 controls patterning of H3K79 methylation and RNA polymerase II to maintain cell identity. Wille CK, Neumann EN, Deshpande AJ, Sridharan R. Stem Cell Reports 18 2451-2463 (2023)
- DOT1L regulates lung developmental epithelial cell fate and adult alveolar stem cell differentiation after acute injury. Li S, Liberti D, Zhou S, Ying Y, Kong J, Basil MC, Cardenas-Diaz FL, Shiraishi K, Morley MP, Morrisey EE. Stem Cell Reports 18 1841-1853 (2023)
- Discovery of Cofactor Competitive Inhibitors against the Human Methyltransferase Fibrillarin. Shi Y, El-Deeb IM, Masic V, Hartley-Tassell L, Maggioni A, Itzstein MV, Ve T. Pharmaceuticals (Basel) 15 26 (2021)
- Structures of SARS-CoV-2 N7-methyltransferase with DOT1L and PRMT7 inhibitors provide a platform for new antivirals. Kottur J, White KM, Rodriguez ML, Rechkoblit O, Quintana-Feliciano R, Nayar A, García-Sastre A, Aggarwal AK. PLoS Pathog 19 e1011546 (2023)