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Conformational Adaptation Drives Potent, Selective and Durable Inhibition of the Human Protein Methyltransferase DOT1L.
Published in:
Chemical Biology & Drug Design, 2012, v. 80, n. 6, p. 971, doi. 10.1111/cbdd.12050
By:
- Basavapathruni, Aravind;
- Jin, Lei;
- Daigle, Scott R.;
- Majer, Christina R. A.;
- Therkelsen, Carly A.;
- Wigle, Tim J.;
- Kuntz, Kevin W.;
- Chesworth, Richard;
- Pollock, Roy M.;
- Scott, Margaret P.;
- Moyer, Mikel P.;
- Richon, Victoria M.;
- Copeland, Robert A.;
- Olhava, Edward J.
Publication type:
Article
Nonclinical pharmacokinetics and metabolism of EPZ-5676, a novel DOT1L histone methyltransferase inhibitor.
Published in:
Biopharmaceutics & Drug Disposition, 2014, v. 35, n. 4, p. 237, doi. 10.1002/bdd.1889
By:
- Basavapathruni, Aravind;
- Olhava, Edward J.;
- Daigle, Scott R.;
- Therkelsen, Carly A.;
- Jin, Lei;
- Boriack‐Sjodin, P. Ann;
- Allain, Christina J.;
- Klaus, Christine R.;
- Raimondi, Alejandra;
- Scott, Margaret Porter;
- Dovletoglou, Angelos;
- Richon, Victoria M.;
- Pollock, Roy M.;
- Copeland, Robert A.;
- Moyer, Mikel P.;
- Chesworth, Richard;
- Pearson, Paul G.;
- Waters, Nigel J.
Publication type:
Article
Synergistic Anti-Tumor Activity of EZH2 Inhibitors and Glucocorticoid Receptor Agonists in Models of Germinal Center Non-Hodgkin Lymphomas.
Published in:
PLoS ONE, 2014, v. 9, n. 12, p. 1, doi. 10.1371/journal.pone.0111840
By:
- Knutson, Sarah K.;
- Warholic, Natalie M.;
- Johnston, L. Danielle;
- Klaus, Christine R.;
- Wigle, Tim J.;
- Iwanowicz, Dorothy;
- Littlefield, Bruce A.;
- Porter-Scott, Margaret;
- Smith, Jesse J.;
- Moyer, Mikel P.;
- Copeland, Robert A.;
- Pollock, Roy M.;
- Kuntz, Kevin W.;
- Raimondi, Alejandra;
- Keilhack, Heike
Publication type:
Article
MLL1 and DOT1L cooperate with meningioma-1 to induce acute myeloid leukemia.
Published in:
2016
By:
- Riedel, Simone S.;
- Haladyna, Jessica N.;
- Bezzant, Matthew;
- Stevens, Brett;
- Pollyea, Daniel A.;
- Sinha, Amit U.;
- Armstrong, Scott A.;
- Qi Wei;
- Pollock, Roy M.;
- Daigle, Scott R.;
- Jordan, Craig T.;
- Ernst, Patricia;
- Neff, Tobias;
- Bernt, Kathrin M.;
- Wei, Qi
Publication type:
journal article
Metabolism and disposition of the DOT1L inhibitor, pinometostat (EPZ-5676), in rat, dog and human.
Published in:
2016
By:
- Waters, Nigel;
- Smith, Sherri;
- Olhava, Edward;
- Duncan, Kenneth;
- Burton, Richard;
- O'Neill, James;
- Rodrigue, Marie-Eve;
- Pollock, Roy;
- Moyer, Mikel;
- Chesworth, Richard;
- Waters, Nigel J;
- Smith, Sherri A;
- Olhava, Edward J;
- Duncan, Kenneth W;
- Burton, Richard D;
- Pollock, Roy M;
- Moyer, Mikel P
Publication type:
journal article
Correction: Preclinical Evidence of Anti-Tumor Activity Induced by EZH2 Inhibition in Human Models of Synovial Sarcoma.
Published in:
2017
By:
- Kawano, Satoshi;
- Grassian, Alexandra R.;
- Tsuda, Masumi;
- Knutson, Sarah K.;
- Warholic, Natalie M.;
- Kuznetsov, Galina;
- Xu, Shanqin;
- Xiao, Yonghong;
- Pollock, Roy M.;
- Smith, Jesse J.;
- Kuntz, Kevin W.;
- Ribich, Scott;
- Minoshima, Yukinori;
- Matsui, Junji;
- Copeland, Robert A.;
- Tanaka, Shinya;
- Keilhack, Heike
Publication type:
Correction Notice
Preclinical Evidence of Anti-Tumor Activity Induced by EZH2 Inhibition in Human Models of Synovial Sarcoma.
Published in:
PLoS ONE, 2016, v. 11, n. 7, p. 1, doi. 10.1371/journal.pone.0158888
By:
- Kawano, Satoshi;
- Grassian, Alexandra R.;
- Tsuda, Masumi;
- Knutson, Sarah K.;
- Warholic, Natalie M.;
- Kuznetsov, Galina;
- Xu, Shanqin;
- Xiao, Yonghong;
- Pollock, Roy M.;
- Smith, Jesse S.;
- Kuntz, Kevin K.;
- Ribich, Scott;
- Minoshima, Yukinori;
- Matsui, Junji;
- Copeland, Robert A.;
- Tanaka, Shinya;
- Keilhack, Heike
Publication type:
Article
A selective inhibitor of PRMT5 with in vivo and in vitro potency in MCL models.
Published in:
Nature Chemical Biology, 2015, v. 11, n. 6, p. 432, doi. 10.1038/nchembio.1810
By:
- Chan-Penebre, Elayne;
- Kuplast, Kristy G;
- Majer, Christina R;
- Boriack-Sjodin, P Ann;
- Wigle, Tim J;
- Johnston, L Danielle;
- Rioux, Nathalie;
- Munchhof, Michael J;
- Jin, Lei;
- Jacques, Suzanne L;
- West, Kip A;
- Lingaraj, Trupti;
- Stickland, Kimberly;
- Ribich, Scott A;
- Raimondi, Alejandra;
- Scott, Margaret Porter;
- Waters, Nigel J;
- Pollock, Roy M;
- Smith, Jesse J;
- Barbash, Olena
Publication type:
Article
The Y641C mutation of EZH2 alters substrate specificity for histone H3 lysine 27 methylation states
Published in:
FEBS Letters, 2011, v. 585, n. 19, p. 3011, doi. 10.1016/j.febslet.2011.08.018
By:
- Wigle, Tim J.;
- Knutson, Sarah K.;
- Jin, Lei;
- Kuntz, Kevin W.;
- Pollock, Roy M.;
- Richon, Victoria M.;
- Copeland, Robert A.;
- Scott, Margaret Porter
Publication type:
Article
A selective inhibitor of EZH2 blocks H3K27 methylation and kills mutant lymphoma cells.
Published in:
Nature Chemical Biology, 2012, v. 8, n. 11, p. 890, doi. 10.1038/nchembio.1084
By:
- Knutson, Sarah K;
- Wigle, Tim J;
- Warholic, Natalie M;
- Sneeringer, Christopher J;
- Allain, Christina J;
- Klaus, Christine R;
- Sacks, Joelle D;
- Raimondi, Alejandra;
- Majer, Christina R;
- Song, Jeffrey;
- Scott, Margaret Porter;
- Jin, Lei;
- Smith, Jesse J;
- Olhava, Edward J;
- Chesworth, Richard;
- Moyer, Mikel P;
- Richon, Victoria M;
- Copeland, Robert A;
- Keilhack, Heike;
- Pollock, Roy M
Publication type:
Article

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