4YPA
 
 | | ASH1L SET domain Q2265A mutant in complex with S-adenosyl methionine (SAM) | | 分子名称: | Histone-lysine N-methyltransferase ASH1L, S-ADENOSYLMETHIONINE, ZINC ION | | 著者 | Rogawski, D.S, Ndoj, J, Cho, H.J, Maillard, I, Grembecka, J, Cierpicki, T. | | 登録日 | 2015-03-12 | | 公開日 | 2015-09-02 | | 最終更新日 | 2023-09-27 | | 実験手法 | X-RAY DIFFRACTION (2.3 Å) | | 主引用文献 | Two Loops Undergoing Concerted Dynamics Regulate the Activity of the ASH1L Histone Methyltransferase.
Biochemistry, 54, 2015
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4YNP
 | | ASH1L SET domain S2259M mutant in complex with S-adenosyl methionine (SAM) | | 分子名称: | Histone-lysine N-methyltransferase ASH1L, S-ADENOSYLMETHIONINE, ZINC ION | | 著者 | Rogawski, D.S, Ndoj, J, Cho, H.-J, Maillard, I, Grembecka, J, Cierpicki, T. | | 登録日 | 2015-03-10 | | 公開日 | 2015-09-02 | | 最終更新日 | 2023-09-27 | | 実験手法 | X-RAY DIFFRACTION (2.9 Å) | | 主引用文献 | Two Loops Undergoing Concerted Dynamics Regulate the Activity of the ASH1L Histone Methyltransferase.
Biochemistry, 54, 2015
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4YPU
 | | ASH1L SET domain K2264L mutant in complex with S-adenosyl methionine (SAM) | | 分子名称: | Histone-lysine N-methyltransferase ASH1L, S-ADENOSYLMETHIONINE, ZINC ION | | 著者 | Rogawski, D.S, Ndoj, J, Cho, H.J, Maillard, I, Grembecka, J, Cierpicki, T. | | 登録日 | 2015-03-13 | | 公開日 | 2015-09-02 | | 最終更新日 | 2023-09-27 | | 実験手法 | X-RAY DIFFRACTION (2.6 Å) | | 主引用文献 | Two Loops Undergoing Concerted Dynamics Regulate the Activity of the ASH1L Histone Methyltransferase.
Biochemistry, 54, 2015
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4YPE
 | | ASH1L SET domain H2193F mutant in complex with S-adenosyl methionine (SAM) | | 分子名称: | Histone-lysine N-methyltransferase ASH1L, S-ADENOSYLMETHIONINE, ZINC ION | | 著者 | Rogawski, D.S, Ndoj, J, Cho, H.J, Maillard, I, Grembecka, J, Cierpicki, T. | | 登録日 | 2015-03-12 | | 公開日 | 2015-09-02 | | 最終更新日 | 2023-09-27 | | 実験手法 | X-RAY DIFFRACTION (2.2 Å) | | 主引用文献 | Two Loops Undergoing Concerted Dynamics Regulate the Activity of the ASH1L Histone Methyltransferase.
Biochemistry, 54, 2015
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4YNM
 | | ASH1L wild-type SET domain in complex with S-adenosyl methionine (SAM) | | 分子名称: | Histone-lysine N-methyltransferase ASH1L, S-ADENOSYLMETHIONINE, ZINC ION | | 著者 | Rogawski, D.S, Ndoj, J, Cho, H.-J, Maillard, I, Grembecka, J, Cierpicki, T. | | 登録日 | 2015-03-10 | | 公開日 | 2015-09-02 | | 最終更新日 | 2023-09-27 | | 実験手法 | X-RAY DIFFRACTION (2.19 Å) | | 主引用文献 | Two Loops Undergoing Concerted Dynamics Regulate the Activity of the ASH1L Histone Methyltransferase.
Biochemistry, 54, 2015
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6O5I
 | | Menin in complex with MI-3454 | | 分子名称: | DIMETHYL SULFOXIDE, Menin, SULFATE ION, ... | | 著者 | Linhares, B.M, Klossowski, S, Cierpicki, T, Grembecka, J. | | 登録日 | 2019-03-03 | | 公開日 | 2020-01-08 | | 最終更新日 | 2023-10-11 | | 実験手法 | X-RAY DIFFRACTION (1.24025619 Å) | | 主引用文献 | Menin inhibitor MI-3454 induces remission in MLL1-rearranged and NPM1-mutated models of leukemia.
J.Clin.Invest., 130, 2020
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6WZW
 | | Ash1L SET domain in complex with AS-85 | | 分子名称: | 4-(2-HYDROXYETHYL)-1-PIPERAZINE ETHANESULFONIC ACID, Histone-lysine N-methyltransferase ASH1L, N-{[3-(3-carbamothioylphenyl)-1-{1-[(trifluoromethyl)sulfonyl]piperidin-4-yl}-1H-indol-6-yl]methyl}azetidine-3-carboxamide, ... | | 著者 | Li, H, Deng, J, Cierpicki, T, Grembecka, J. | | 登録日 | 2020-05-14 | | 公開日 | 2021-04-07 | | 最終更新日 | 2023-10-18 | | 実験手法 | X-RAY DIFFRACTION (1.69 Å) | | 主引用文献 | Discovery of first-in-class inhibitors of ASH1L histone methyltransferase with anti-leukemic activity.
Nat Commun, 12, 2021
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6X0P
 | | Ash1L SET domain Q2265A mutant in complex with AS-5 | | 分子名称: | 3-[6-(aminomethyl)-1-(2-hydroxyethyl)-1H-indol-3-yl]benzene-1-carbothioamide, Histone-lysine N-methyltransferase ASH1L, S-ADENOSYLMETHIONINE, ... | | 著者 | Rogawski, D.S, Li, H, Borkin, D, Cierpicki, T, Grembecka, J. | | 登録日 | 2020-05-17 | | 公開日 | 2021-04-07 | | 最終更新日 | 2023-10-18 | | 実験手法 | X-RAY DIFFRACTION (1.69 Å) | | 主引用文献 | Discovery of first-in-class inhibitors of ASH1L histone methyltransferase with anti-leukemic activity.
Nat Commun, 12, 2021
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4X5Z
 | | menin in complex with MI-136 | | 分子名称: | 1,2-ETHANEDIOL, 5-[(4-{[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino}piperidin-1-yl)methyl]-1H-indole-2-carbonitrile, DIMETHYL SULFOXIDE, ... | | 著者 | Pollock, J, Borkin, D, Cierpicki, T, Grembecka, J. | | 登録日 | 2014-12-06 | | 公開日 | 2015-04-15 | | 最終更新日 | 2023-09-27 | | 実験手法 | X-RAY DIFFRACTION (1.86 Å) | | 主引用文献 | Pharmacologic Inhibition of the Menin-MLL Interaction Blocks Progression of MLL Leukemia In Vivo.
Cancer Cell, 27, 2015
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4X5Y
 | | Menin in complex with MI-503 | | 分子名称: | 1,2-ETHANEDIOL, 4-(2-HYDROXYETHYL)-1-PIPERAZINE ETHANESULFONIC ACID, 4-methyl-1-(1H-pyrazol-4-ylmethyl)-5-[(4-{[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino}piperidin-1-yl)methyl]-1H-indole-2-carbonitrile, ... | | 著者 | Pollock, J, Borkin, D, Cierpicki, T, Grembecka, J. | | 登録日 | 2014-12-06 | | 公開日 | 2015-04-15 | | 最終更新日 | 2023-12-27 | | 実験手法 | X-RAY DIFFRACTION (1.59 Å) | | 主引用文献 | Pharmacologic Inhibition of the Menin-MLL Interaction Blocks Progression of MLL Leukemia In Vivo.
Cancer Cell, 27, 2015
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