4YPA
 
 | | ASH1L SET domain Q2265A mutant in complex with S-adenosyl methionine (SAM) | | Descriptor: | Histone-lysine N-methyltransferase ASH1L, S-ADENOSYLMETHIONINE, ZINC ION | | Authors: | Rogawski, D.S, Ndoj, J, Cho, H.J, Maillard, I, Grembecka, J, Cierpicki, T. | | Deposit date: | 2015-03-12 | | Release date: | 2015-09-02 | | Last modified: | 2023-09-27 | | Method: | X-RAY DIFFRACTION (2.3 Å) | | Cite: | Two Loops Undergoing Concerted Dynamics Regulate the Activity of the ASH1L Histone Methyltransferase.
Biochemistry, 54, 2015
|
|
4YNP
 | | ASH1L SET domain S2259M mutant in complex with S-adenosyl methionine (SAM) | | Descriptor: | Histone-lysine N-methyltransferase ASH1L, S-ADENOSYLMETHIONINE, ZINC ION | | Authors: | Rogawski, D.S, Ndoj, J, Cho, H.-J, Maillard, I, Grembecka, J, Cierpicki, T. | | Deposit date: | 2015-03-10 | | Release date: | 2015-09-02 | | Last modified: | 2023-09-27 | | Method: | X-RAY DIFFRACTION (2.9 Å) | | Cite: | Two Loops Undergoing Concerted Dynamics Regulate the Activity of the ASH1L Histone Methyltransferase.
Biochemistry, 54, 2015
|
|
4YNM
 | | ASH1L wild-type SET domain in complex with S-adenosyl methionine (SAM) | | Descriptor: | Histone-lysine N-methyltransferase ASH1L, S-ADENOSYLMETHIONINE, ZINC ION | | Authors: | Rogawski, D.S, Ndoj, J, Cho, H.-J, Maillard, I, Grembecka, J, Cierpicki, T. | | Deposit date: | 2015-03-10 | | Release date: | 2015-09-02 | | Last modified: | 2023-09-27 | | Method: | X-RAY DIFFRACTION (2.19 Å) | | Cite: | Two Loops Undergoing Concerted Dynamics Regulate the Activity of the ASH1L Histone Methyltransferase.
Biochemistry, 54, 2015
|
|
4YPE
 | | ASH1L SET domain H2193F mutant in complex with S-adenosyl methionine (SAM) | | Descriptor: | Histone-lysine N-methyltransferase ASH1L, S-ADENOSYLMETHIONINE, ZINC ION | | Authors: | Rogawski, D.S, Ndoj, J, Cho, H.J, Maillard, I, Grembecka, J, Cierpicki, T. | | Deposit date: | 2015-03-12 | | Release date: | 2015-09-02 | | Last modified: | 2023-09-27 | | Method: | X-RAY DIFFRACTION (2.2 Å) | | Cite: | Two Loops Undergoing Concerted Dynamics Regulate the Activity of the ASH1L Histone Methyltransferase.
Biochemistry, 54, 2015
|
|
4YPU
 | | ASH1L SET domain K2264L mutant in complex with S-adenosyl methionine (SAM) | | Descriptor: | Histone-lysine N-methyltransferase ASH1L, S-ADENOSYLMETHIONINE, ZINC ION | | Authors: | Rogawski, D.S, Ndoj, J, Cho, H.J, Maillard, I, Grembecka, J, Cierpicki, T. | | Deposit date: | 2015-03-13 | | Release date: | 2015-09-02 | | Last modified: | 2023-09-27 | | Method: | X-RAY DIFFRACTION (2.6 Å) | | Cite: | Two Loops Undergoing Concerted Dynamics Regulate the Activity of the ASH1L Histone Methyltransferase.
Biochemistry, 54, 2015
|
|
6O5I
 | | Menin in complex with MI-3454 | | Descriptor: | DIMETHYL SULFOXIDE, Menin, SULFATE ION, ... | | Authors: | Linhares, B.M, Klossowski, S, Cierpicki, T, Grembecka, J. | | Deposit date: | 2019-03-03 | | Release date: | 2020-01-08 | | Last modified: | 2023-10-11 | | Method: | X-RAY DIFFRACTION (1.24025619 Å) | | Cite: | Menin inhibitor MI-3454 induces remission in MLL1-rearranged and NPM1-mutated models of leukemia.
J.Clin.Invest., 130, 2020
|
|
6WZW
 | | Ash1L SET domain in complex with AS-85 | | Descriptor: | 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, ... | | Authors: | Li, H, Deng, J, Cierpicki, T, Grembecka, J. | | Deposit date: | 2020-05-14 | | Release date: | 2021-04-07 | | Last modified: | 2023-10-18 | | Method: | X-RAY DIFFRACTION (1.69 Å) | | Cite: | Discovery of first-in-class inhibitors of ASH1L histone methyltransferase with anti-leukemic activity.
Nat Commun, 12, 2021
|
|
6X0P
 | | Ash1L SET domain Q2265A mutant in complex with AS-5 | | Descriptor: | 3-[6-(aminomethyl)-1-(2-hydroxyethyl)-1H-indol-3-yl]benzene-1-carbothioamide, Histone-lysine N-methyltransferase ASH1L, S-ADENOSYLMETHIONINE, ... | | Authors: | Rogawski, D.S, Li, H, Borkin, D, Cierpicki, T, Grembecka, J. | | Deposit date: | 2020-05-17 | | Release date: | 2021-04-07 | | Last modified: | 2023-10-18 | | Method: | X-RAY DIFFRACTION (1.69 Å) | | Cite: | Discovery of first-in-class inhibitors of ASH1L histone methyltransferase with anti-leukemic activity.
Nat Commun, 12, 2021
|
|
4X5Y
 | | Menin in complex with MI-503 | | Descriptor: | 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, ... | | Authors: | Pollock, J, Borkin, D, Cierpicki, T, Grembecka, J. | | Deposit date: | 2014-12-06 | | Release date: | 2015-04-15 | | Last modified: | 2023-12-27 | | Method: | X-RAY DIFFRACTION (1.59 Å) | | Cite: | Pharmacologic Inhibition of the Menin-MLL Interaction Blocks Progression of MLL Leukemia In Vivo.
Cancer Cell, 27, 2015
|
|
4X5Z
 | | menin in complex with MI-136 | | Descriptor: | 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, ... | | Authors: | Pollock, J, Borkin, D, Cierpicki, T, Grembecka, J. | | Deposit date: | 2014-12-06 | | Release date: | 2015-04-15 | | Last modified: | 2023-09-27 | | Method: | X-RAY DIFFRACTION (1.86 Å) | | Cite: | Pharmacologic Inhibition of the Menin-MLL Interaction Blocks Progression of MLL Leukemia In Vivo.
Cancer Cell, 27, 2015
|
|
