-
1
-
-
84870792079
-
Perceiving the epigenetic landscape through histone readers
-
Musselman, C. A.; Lalonde, M.; Coîté, J.; Kutateladze, T. G. Perceiving the epigenetic landscape through histone readers Nat. Struct. Mol. Biol. 2012, 19, 1218-1227 10.1038/nsmb.2436
-
(2012)
Nat. Struct. Mol. Biol.
, vol.19
, pp. 1218-1227
-
-
Musselman, C.A.1
Lalonde, M.2
Coîté, J.3
Kutateladze, T.G.4
-
2
-
-
75749124332
-
Somatic mutations altering EZH2 (Tyr641) in follicular and diffuse large B-cell lymphomas of germinal-center origin
-
Morin, R. D. et al. Somatic mutations altering EZH2 (Tyr641) in follicular and diffuse large B-cell lymphomas of germinal-center origin Nat. Genet. 2010, 42, 181-185 10.1038/ng.518
-
(2010)
Nat. Genet.
, vol.42
, pp. 181-185
-
-
Morin, R.D.1
-
3
-
-
78650454078
-
Coordinated activities of wild-type plus mutant EZH2 drive tumor-associated hypertrimethylation of lysine 27 on histone H3 (H3K27) in human B-cell lymphomas
-
Sneeringer, C. J.; Porter-Scott, M.; Kuntz, K. W.; Knutson, S. K.; Pollock, R. M.; Richon, V. R.; Copeland, R. A. Coordinated activities of wild-type plus mutant EZH2 drive tumor-associated hypertrimethylation of lysine 27 on histone H3 (H3K27) in human B-cell lymphomas Proc. Natl. Acad. Sci. U. S. A. 2010, 107, 20980-20985 10.1073/pnas.1012525107
-
(2010)
Proc. Natl. Acad. Sci. U. S. A.
, vol.107
, pp. 20980-20985
-
-
Sneeringer, C.J.1
Porter-Scott, M.2
Kuntz, K.W.3
Knutson, S.K.4
Pollock, R.M.5
Richon, V.R.6
Copeland, R.A.7
-
4
-
-
77957770113
-
SET7/9 Catalytic Mutants Reveal the Role of Active Site Water Molecules in Lysine Multiple Methylation
-
Del Rizzo, P. A.; Couture, J.-F.; Dirk, L. M. A.; Strunk, B. S.; Roiko, M. S.; Brunzelle, J. S.; Houtz, R. L.; Trievel, R. C. SET7/9 Catalytic Mutants Reveal the Role of Active Site Water Molecules in Lysine Multiple Methylation J. Biol. Chem. 2010, 285, 31849-31858 10.1074/jbc.M110.114587
-
(2010)
J. Biol. Chem.
, vol.285
, pp. 31849-31858
-
-
Del Rizzo, P.A.1
Couture, J.-F.2
Dirk, L.M.A.3
Strunk, B.S.4
Roiko, M.S.5
Brunzelle, J.S.6
Houtz, R.L.7
Trievel, R.C.8
-
5
-
-
58549112187
-
Structural origins for the product specificity of SET domain protein methyltransferases
-
Couture, J.; Dirk, L. M. A.; Brunzelle, J. S.; Houtz, R. L.; Trievel, R. C. Structural origins for the product specificity of SET domain protein methyltransferases Proc. Natl. Acad. Sci. U. S. A. 2008, 105, 20659-20664 10.1073/pnas.0806712105
-
(2008)
Proc. Natl. Acad. Sci. U. S. A.
, vol.105
, pp. 20659-20664
-
-
Couture, J.1
Dirk, L.M.A.2
Brunzelle, J.S.3
Houtz, R.L.4
Trievel, R.C.5
-
6
-
-
84937397052
-
A selective inhibitor of PRMT5 with in vivo and in vitro potency in MCL models
-
Chan-Penebre, E.; Kuplast, K. G.; Majer, C. R.; Boriack-Sjodin, P. A.; Wigle, T. J.; Johnston, L. D.; Rioux, N.; Munchhof, M. J.; Jin, L.; Jacques, S. L.; West, K. A.; Lingaraj, T.; Stickland, K.; Ribich, S. A.; Raimondi, A.; Scott, M. P.; Waters, N. J.; Pollock, R. M.; Smith, J. J.; Barbash, O.; Pappalardi, M.; Ho, T. F.; Nurse, K.; Oza, K. P.; Gallagher, K. T.; Kruger, R.; Moyer, M. P.; Copeland, R. A.; Chesworth, R.; Duncan, K. W. A selective inhibitor of PRMT5 with in vivo and in vitro potency in MCL models Nat. Chem. Biol. 2015, 11, 432-437 10.1038/nchembio.1810
-
(2015)
Nat. Chem. Biol.
, vol.11
, pp. 432-437
-
-
Chan-Penebre, E.1
Kuplast, K.G.2
Majer, C.R.3
Boriack-Sjodin, P.A.4
Wigle, T.J.5
Johnston, L.D.6
Rioux, N.7
Munchhof, M.J.8
Jin, L.9
Jacques, S.L.10
West, K.A.11
Lingaraj, T.12
Stickland, K.13
Ribich, S.A.14
Raimondi, A.15
Scott, M.P.16
Waters, N.J.17
Pollock, R.M.18
Smith, J.J.19
Barbash, O.20
Pappalardi, M.21
Ho, T.F.22
Nurse, K.23
Oza, K.P.24
Gallagher, K.T.25
Kruger, R.26
Moyer, M.P.27
Copeland, R.A.28
Chesworth, R.29
Duncan, K.W.30
more..
-
7
-
-
84861017386
-
Methyl Effects on Protein-Ligand Binding
-
Leung, C. S.; Leung, S. S. F.; Tirado-Rives, J.; Jorgensen, W. L. Methyl Effects on Protein-Ligand Binding J. Med. Chem. 2012, 55, 4489-4500 10.1021/jm3003697
-
(2012)
J. Med. Chem.
, vol.55
, pp. 4489-4500
-
-
Leung, C.S.1
Leung, S.S.F.2
Tirado-Rives, J.3
Jorgensen, W.L.4
-
8
-
-
80052791467
-
The Methylation Effect in Medicinal Chemistry
-
Barreiro, E. J.; Kummerle, A. E.; Fraga, C. A. M. The Methylation Effect in Medicinal Chemistry Chem. Rev. 2011, 111, 5215-5246 10.1021/cr200060g
-
(2011)
Chem. Rev.
, vol.111
, pp. 5215-5246
-
-
Barreiro, E.J.1
Kummerle, A.E.2
Fraga, C.A.M.3
-
9
-
-
84867632489
-
A Selective Inhibitor of EZH2 blocks H3K27 methylation and Kills Mutant Lymphoma Cells
-
Knutson, S. K.; Wigle, T. J.; Warholic, N. M.; Sneeringer, C. J.; Allain, C. J.; Klaus, C. R.; Sacks, J. D.; Raimondi, A.; Majer, C. R.; Song, J.; Porter-Scott, M.; Jin, L.; Smith, J. J.; Olhava, E. J.; Chesworth, R.; Moyer, M.; Richon, V. M.; Copeland, R. A.; Keilhack, H.; Pollock, R. M.; Kuntz, K. W. A Selective Inhibitor of EZH2 blocks H3K27 methylation and Kills Mutant Lymphoma Cells Nat. Chem. Biol. 2012, 8, 890-896 10.1038/nchembio.1084
-
(2012)
Nat. Chem. Biol.
, vol.8
, pp. 890-896
-
-
Knutson, S.K.1
Wigle, T.J.2
Warholic, N.M.3
Sneeringer, C.J.4
Allain, C.J.5
Klaus, C.R.6
Sacks, J.D.7
Raimondi, A.8
Majer, C.R.9
Song, J.10
Porter-Scott, M.11
Jin, L.12
Smith, J.J.13
Olhava, E.J.14
Chesworth, R.15
Moyer, M.16
Richon, V.M.17
Copeland, R.A.18
Keilhack, H.19
Pollock, R.M.20
Kuntz, K.W.21
more..
-
10
-
-
84938375449
-
Discovery, design, and synthesis of indole-based EZH2 inhibitors
-
Gehling, V. S.; Vaswani, R. G.; Nasveschuk, C. G.; Duplessis, M.; Iyer, P.; Balasubramanian, S.; Zhao, F.; Good, A. C.; Camp-bell, R.; Lee, C.; Dakin, L. A.; Cook, A. S.; Gagnon, A.; Harmange, J.; Audia, J. E.; Cummings, R. T.; Normant, E.; Trojer, P.; Albrecht, B. K. Discovery, design, and synthesis of indole-based EZH2 inhibitors Bioorg. Med. Chem. Lett. 2015, 25, 3644-3649 10.1016/j.bmcl.2015.06.056
-
(2015)
Bioorg. Med. Chem. Lett.
, vol.25
, pp. 3644-3649
-
-
Gehling, V.S.1
Vaswani, R.G.2
Nasveschuk, C.G.3
Duplessis, M.4
Iyer, P.5
Balasubramanian, S.6
Zhao, F.7
Good, A.C.8
Camp-Bell, R.9
Lee, C.10
Dakin, L.A.11
Cook, A.S.12
Gagnon, A.13
Harmange, J.14
Audia, J.E.15
Cummings, R.T.16
Normant, E.17
Trojer, P.18
Albrecht, B.K.19
-
11
-
-
84871248432
-
Identification of Potent, Selective Cell-Active Inhibitors of the Histone Lysine Methyltransferase EZH2
-
Verma, S. K.; Tian, X.; LaFrance, L. V.; Duquenne, C.; Suarez, D. P.; Newlander, K. A.; Romeril, S. P.; Burgess, J. L.; Grant, S. W.; Brackley, J. A.; Graves, A. P.; Scherzer, D. A.; Shu, A.; Thompson, C.; Ott, H. M.; Van Aller, G. S.; Machutta, C. A.; Diaz, E.; Jiang, Y.; Johnson, N. W.; Knight, S. D.; Kruger, R. G.; McCabe, M. T.; Dhanak, D.; Tummino, P. J.; Creasy, C. L.; Miller, W. H. Identification of Potent, Selective Cell-Active Inhibitors of the Histone Lysine Methyltransferase EZH2 ACS Med. Chem. Lett. 2012, 3, 1091-1096 10.1021/ml3003346
-
(2012)
ACS Med. Chem. Lett.
, vol.3
, pp. 1091-1096
-
-
Verma, S.K.1
Tian, X.2
LaFrance, L.V.3
Duquenne, C.4
Suarez, D.P.5
Newlander, K.A.6
Romeril, S.P.7
Burgess, J.L.8
Grant, S.W.9
Brackley, J.A.10
Graves, A.P.11
Scherzer, D.A.12
Shu, A.13
Thompson, C.14
Ott, H.M.15
Van Aller, G.S.16
Machutta, C.A.17
Diaz, E.18
Jiang, Y.19
Johnson, N.W.20
Knight, S.D.21
Kruger, R.G.22
McCabe, M.T.23
Dhanak, D.24
Tummino, P.J.25
Creasy, C.L.26
Miller, W.H.27
more..
-
12
-
-
84871841675
-
Selective inhibition of EZH2 by a small molecule inhibitor blocks tumor cell proliferation
-
Qi, W.; Chan, H.; Teng, L.; Li, L.; Chuai, S.; Zhang, R.; Zeng, J.; Li, M.; Fan, H.; Lin, Y.; Gu, J.; Ardayfio, O.; Zhang, J.-H.; Yan, X.; Fang, J.; Mi, Y.; Zhang, M.; Zhou, T.; Feng, G.; Chen, Z.; Li, G.; Yang, T.; Zhao, K.; Liu, X.; Yu, Z.; Lu, C. X.; Atadja, P.; Li, E. Selective inhibition of EZH2 by a small molecule inhibitor blocks tumor cell proliferation Proc. Natl. Acad. Sci. U. S. A. 2012, 109, 21360-21365 10.1073/pnas.1210371110
-
(2012)
Proc. Natl. Acad. Sci. U. S. A.
, vol.109
, pp. 21360-21365
-
-
Qi, W.1
Chan, H.2
Teng, L.3
Li, L.4
Chuai, S.5
Zhang, R.6
Zeng, J.7
Li, M.8
Fan, H.9
Lin, Y.10
Gu, J.11
Ardayfio, O.12
Zhang, J.-H.13
Yan, X.14
Fang, J.15
Mi, Y.16
Zhang, M.17
Zhou, T.18
Feng, G.19
Chen, Z.20
Li, G.21
Yang, T.22
Zhao, K.23
Liu, X.24
Yu, Z.25
Lu, C.X.26
Atadja, P.27
Li, E.28
more..
-
14
-
-
77950571108
-
New substructure filters for removal of pan assay interference compounds (PAINS) from screening libraries and for their exclusion in bioassays
-
Baell, J. B.; Holloway, G. A. New substructure filters for removal of pan assay interference compounds (PAINS) from screening libraries and for their exclusion in bioassays J. Med. Chem. 2010, 53, 2719-2740 10.1021/jm901137j
-
(2010)
J. Med. Chem.
, vol.53
, pp. 2719-2740
-
-
Baell, J.B.1
Holloway, G.A.2
-
15
-
-
34548351239
-
A simple assay for detection of small-molecule redox activity
-
Lor, L. A.; Schneck, J.; McNulty, D. E.; Diaz, E.; Brandt, M.; Thrall, S. H.; Schwartz, B. A simple assay for detection of small-molecule redox activity J. Biomol. Screening 2007, 12, 881-890 10.1177/1087057107304113
-
(2007)
J. Biomol. Screening
, vol.12
, pp. 881-890
-
-
Lor, L.A.1
Schneck, J.2
McNulty, D.E.3
Diaz, E.4
Brandt, M.5
Thrall, S.H.6
Schwartz, B.7
-
16
-
-
77952545106
-
Apparent Activity in High-Throughput Screening: Origins of Compound-Dependent Assay Interference
-
Thorne, N.; Auld, D. S.; Inglese, J. Apparent Activity in High-Throughput Screening: Origins of Compound-Dependent Assay Interference Curr. Opin. Chem. Biol. 2010, 14, 315-324 10.1016/j.cbpa.2010.03.020
-
(2010)
Curr. Opin. Chem. Biol.
, vol.14
, pp. 315-324
-
-
Thorne, N.1
Auld, D.S.2
Inglese, J.3
-
17
-
-
84959325956
-
Aryl-or heteroaryl-substituted benzamide compounds as anticancer agents and their preparation
-
October 18
-
Kuntz, K. W.; Chesworth, R.; Duncan, K. W.; Keilhack, H.; Warholic, N.; Klaus, C.; Zheng, W.; Seki, M.; Shirotori, S.; Ka-wano, S. Aryl-or heteroaryl-substituted benzamide compounds as anticancer agents and their preparation. WO 2012142504 A1, October 18, 2012.
-
(2012)
-
-
Kuntz, K.W.1
Chesworth, R.2
Duncan, K.W.3
Keilhack, H.4
Warholic, N.5
Klaus, C.6
Zheng, W.7
Seki, M.8
Shirotori, S.9
Ka-Wano, S.10
-
18
-
-
84959387958
-
Aryl and heteroaryl fused lactams
-
June 26
-
Edwards, M. P.; Kumpf, R. A.; Kung, P.; Mcalpine, I. J.; Ninkovic, S.; Rui, E. Y.; Sutton, S. C.; Tatlock, J. H.; Wythes, M. J.; Zehnder, L. R. Aryl and heteroaryl fused lactams. WO 2014/097041 A1, June 26, 2014.
-
(2014)
-
-
Edwards, M.P.1
Kumpf, R.A.2
Kung, P.3
McAlpine, I.J.4
Ninkovic, S.5
Rui, E.Y.6
Sutton, S.C.7
Tatlock, J.H.8
Wythes, M.J.9
Zehnder, L.R.10
-
19
-
-
84921318899
-
Selective Inhibition of EZH2 by EPZ-6438 Leads to Potent Antitumor Activity in EZH2-Mutant Non-Hodgkin Lymphoma
-
Knutson, S. K.; Kawano, S.; Minoshima, Y.; Warholic, N. M.; Huang, K.; Xiao, Y.; Kadowaki, T.; Uesugi, M.; Kuznetsov, G.; Kumar, N.; Wigle, T. J.; Klaus, C. R.; Allain, C. J.; Raimondi, A.; Waters, N. J.; Smith, J. J.; Porter-Scott, M.; Chesworth, R.; Moyer, M. P.; Copeland, R. A.; Richon, V. M.; Uenaka, T.; Pollock, R. M.; Kuntz, K. W.; Yokoi, A.; Keilhack, H. Selective Inhibition of EZH2 by EPZ-6438 Leads to Potent Antitumor Activity in EZH2-Mutant Non-Hodgkin Lymphoma Mol. Cancer Ther. 2014, 13, 842-854 10.1158/1535-7163.MCT-13-0773
-
(2014)
Mol. Cancer Ther.
, vol.13
, pp. 842-854
-
-
Knutson, S.K.1
Kawano, S.2
Minoshima, Y.3
Warholic, N.M.4
Huang, K.5
Xiao, Y.6
Kadowaki, T.7
Uesugi, M.8
Kuznetsov, G.9
Kumar, N.10
Wigle, T.J.11
Klaus, C.R.12
Allain, C.J.13
Raimondi, A.14
Waters, N.J.15
Smith, J.J.16
Porter-Scott, M.17
Chesworth, R.18
Moyer, M.P.19
Copeland, R.A.20
Richon, V.M.21
Uenaka, T.22
Pollock, R.M.23
Kuntz, K.W.24
Yokoi, A.25
Keilhack, H.26
more..
-
20
-
-
84916881910
-
Synergistic Anti-Tumor Activity of EZH2 Inhibitors and Glucocorticoid Receptor Agonists in Models of Germinal Center Non-Hodgkin Lymphomas
-
Knutson, S. K.; Warholic, N. M.; Johnston, L. D.; Klaus, C. R.; Wigle, T. J.; Iwanowicz, D.; Littlefield, B. A.; Porter-Scott, M.; Smith, J.; Moyer, M. P.; Copeland, R. A.; Pollock, R. M.; Kuntz, K. W.; Raimondi, A.; Keilhack, H. Synergistic Anti-Tumor Activity of EZH2 Inhibitors and Glucocorticoid Receptor Agonists in Models of Germinal Center Non-Hodgkin Lymphomas PLoS One 2014, 9, e111840 10.1371/journal.pone.0111840
-
(2014)
PLoS One
, vol.9
-
-
Knutson, S.K.1
Warholic, N.M.2
Johnston, L.D.3
Klaus, C.R.4
Wigle, T.J.5
Iwanowicz, D.6
Littlefield, B.A.7
Porter-Scott, M.8
Smith, J.9
Moyer, M.P.10
Copeland, R.A.11
Pollock, R.M.12
Kuntz, K.W.13
Raimondi, A.14
Keilhack, H.15
-
21
-
-
84877324084
-
Durable Tumor Regression in Genetically Altered Malignant Rhabdoid Tumors by Inhibition of Methyltransferase EZH2
-
Knutson, S. K.; Warholic, N. M.; Wigle, T. J.; Klaus, C. R.; Allain, C. J.; Raimondi, A.; Porter-Scott, M.; Chesworth, R.; Moyer, M. P.; Copeland, R. A.; Richon, V. M.; Pollock, R. M.; Kuntz, K. W.; Keilhack, H. Durable Tumor Regression in Genetically Altered Malignant Rhabdoid Tumors by Inhibition of Methyltransferase EZH2 Proc. Natl. Acad. Sci. U. S. A. 2013, 110, 7922-7927 10.1073/pnas.1303800110
-
(2013)
Proc. Natl. Acad. Sci. U. S. A.
, vol.110
, pp. 7922-7927
-
-
Knutson, S.K.1
Warholic, N.M.2
Wigle, T.J.3
Klaus, C.R.4
Allain, C.J.5
Raimondi, A.6
Porter-Scott, M.7
Chesworth, R.8
Moyer, M.P.9
Copeland, R.A.10
Richon, V.M.11
Pollock, R.M.12
Kuntz, K.W.13
Keilhack, H.14
-
22
-
-
84964728083
-
Phase 1 Study of E7438 (EPZ-6438), an Enhancer of Zeste-Homolog 2 (EZH2) Inhibitor: Dose Determination and Preliminary Activity in Non-Hodgkin Lymphoma
-
Ribrag, V.; Soria, J.; Reyderman, L.; Kraljevic, S.; Chen, R.; Salazar, P.; Kuznetsov, G.; Keilhack, H.; Waters, N.; Hedrick, E.; Ottesen, L. H.; Italiano, A. Phase 1 Study of E7438 (EPZ-6438), an Enhancer of Zeste-Homolog 2 (EZH2) Inhibitor: Dose Determination and Preliminary Activity in Non-Hodgkin Lymphoma Hematol. Oncol. 2015, 33, 179
-
(2015)
Hematol. Oncol.
, vol.33
, pp. 179
-
-
Ribrag, V.1
Soria, J.2
Reyderman, L.3
Kraljevic, S.4
Chen, R.5
Salazar, P.6
Kuznetsov, G.7
Keilhack, H.8
Waters, N.9
Hedrick, E.10
Ottesen, L.H.11
Italiano, A.12
|