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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
Convergent evolution of chromatin modification by structurally distinct enzymes: comparative enzymology of histone H3 Lys<sup>27</sup> methylation by human polycomb repressive complex 2 and vSET.
Published in:
Biochemical Journal, 2013, v. 453, n. 2, p. 241, doi. 10.1042/BJ20130439
By:
- SWALM, Brooke M.;
- HALLENBECK, Kenneth K.;
- MAJER, Christina R.;
- JIN, Lei;
- SCOTT, Margaret Porter;
- MOYER, Mikel P.;
- COPELAND, Robert A.;
- WIGLE, Tim 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
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
A687V EZH2 is a gain-of-function mutation found in lymphoma patients
Published in:
FEBS Letters, 2012, v. 586, n. 19, p. 3448, doi. 10.1016/j.febslet.2012.07.066
By:
- Majer, Christina R.;
- Jin, Lei;
- Scott, Margaret Porter;
- Knutson, Sarah K.;
- Kuntz, Kevin W.;
- Keilhack, Heike;
- Smith, Jesse J.;
- Moyer, Mikel P.;
- Richon, Victoria M.;
- Copeland, Robert A.;
- Wigle, Tim J.
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

Found: 7

Conformational Adaptation Drives Potent, Selective and Durable Inhibition of the Human Protein Methyltransferase DOT1L.

Convergent evolution of chromatin modification by structurally distinct enzymes: comparative enzymology of histone H3 Lys<sup>27</sup> methylation by human polycomb repressive complex 2 and vSET.

Nonclinical pharmacokinetics and metabolism of EPZ-5676, a novel DOT1L histone methyltransferase inhibitor.

Synergistic Anti-Tumor Activity of EZH2 Inhibitors and Glucocorticoid Receptor Agonists in Models of Germinal Center Non-Hodgkin Lymphomas.

Metabolism and disposition of the DOT1L inhibitor, pinometostat (EPZ-5676), in rat, dog and human.

A687V EZH2 is a gain-of-function mutation found in lymphoma patients

A selective inhibitor of EZH2 blocks H3K27 methylation and kills mutant lymphoma cells.