4X61
 
 | | Crystal structure of PRMT5:MEP50 with EPZ015666 and SAM | | Descriptor: | GLYCEROL, Methylosome protein 50, N-[(2S)-3-(3,4-dihydroisoquinolin-2(1H)-yl)-2-hydroxypropyl]-6-(oxetan-3-ylamino)pyrimidine-4-carboxamide, ... | | Authors: | Boriack-Sjodin, P.A. | | Deposit date: | 2014-12-06 | | Release date: | 2015-04-22 | | Last modified: | 2024-02-28 | | Method: | X-RAY DIFFRACTION (2.85 Å) | | Cite: | A selective inhibitor of PRMT5 with in vivo and in vitro potency in MCL models.
Nat.Chem.Biol., 11, 2015
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4X60
 | | Crystal structure of PRMT5:MEP50 with EPZ015666 and sinefungin | | Descriptor: | GLYCEROL, Methylosome protein 50, N-[(2S)-3-(3,4-dihydroisoquinolin-2(1H)-yl)-2-hydroxypropyl]-6-(oxetan-3-ylamino)pyrimidine-4-carboxamide, ... | | Authors: | Boriack-Sjodin, P.A. | | Deposit date: | 2014-12-06 | | Release date: | 2015-04-22 | | Last modified: | 2024-02-28 | | Method: | X-RAY DIFFRACTION (2.35 Å) | | Cite: | A selective inhibitor of PRMT5 with in vivo and in vitro potency in MCL models.
Nat.Chem.Biol., 11, 2015
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6ARJ
 | | Crystal structure of CARM1 with EPZ022302 and SAH | | Descriptor: | GLYCEROL, Histone-arginine methyltransferase CARM1, S-ADENOSYL-L-HOMOCYSTEINE, ... | | Authors: | Boriack-Sjodin, P.A, Jin, L. | | Deposit date: | 2017-08-22 | | Release date: | 2018-02-07 | | Last modified: | 2024-03-13 | | Method: | X-RAY DIFFRACTION (1.92 Å) | | Cite: | Identification of a CARM1 Inhibitor with Potent In Vitro and In Vivo Activity in Preclinical Models of Multiple Myeloma.
Sci Rep, 7, 2017
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6ARV
 | | Crystal structure of CARM1 with Compound 2 and SAH | | Descriptor: | (2R)-1-amino-3-{3-[4-(morpholin-4-yl)-1-(propan-2-yl)-1H-pyrazolo[3,4-b]pyridin-6-yl]phenoxy}propan-2-ol, GLYCEROL, Histone-arginine methyltransferase CARM1, ... | | Authors: | Boriack-Sjodin, P.A, Jin, L. | | Deposit date: | 2017-08-23 | | Release date: | 2018-02-07 | | Last modified: | 2024-03-13 | | Method: | X-RAY DIFFRACTION (2 Å) | | Cite: | Identification of a CARM1 Inhibitor with Potent In Vitro and In Vivo Activity in Preclinical Models of Multiple Myeloma.
Sci Rep, 7, 2017
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5V3H
 | | Crystal structure of SMYD2 with SAM and EPZ033294 | | Descriptor: | 1,2-ETHANEDIOL, DI(HYDROXYETHYL)ETHER, GLYCEROL, ... | | Authors: | Boriack-Sjodin, P.A. | | Deposit date: | 2017-03-07 | | Release date: | 2018-04-25 | | Last modified: | 2024-03-06 | | Method: | X-RAY DIFFRACTION (2.69 Å) | | Cite: | Small molecule inhibitors and CRISPR/Cas9 mutagenesis demonstrate that SMYD2 and SMYD3 activity are dispensable for autonomous cancer cell proliferation.
Plos One, 13, 2018
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5V37
 | | Crystal structure of SMYD3 with SAM and EPZ028862 | | Descriptor: | 1,2-ETHANEDIOL, DI(HYDROXYETHYL)ETHER, DIMETHYL SULFOXIDE, ... | | Authors: | Boriack-Sjodin, P.A. | | Deposit date: | 2017-03-06 | | Release date: | 2018-03-07 | | Last modified: | 2024-03-06 | | Method: | X-RAY DIFFRACTION (1.42 Å) | | Cite: | Small molecule inhibitors and CRISPR/Cas9 mutagenesis demonstrate that SMYD2 and SMYD3 activity are dispensable for autonomous cancer cell proliferation.
Plos One, 13, 2018
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6E5N
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7LZF
 | | Crystal Structure of SETD2 bound to Compound 57 | | Descriptor: | 1,2-ETHANEDIOL, 4-fluoro-N-[(1R,3S)-3-{(3S)-3-[(methanesulfonyl)(methyl)amino]pyrrolidin-1-yl}cyclohexyl]-7-methyl-1H-indole-2-carboxamide, Histone-lysine N-methyltransferase SETD2, ... | | Authors: | Farrow, N.A, Boriack-Sjodin, P. | | Deposit date: | 2021-03-09 | | Release date: | 2021-09-22 | | Last modified: | 2023-10-18 | | Method: | X-RAY DIFFRACTION (2.47 Å) | | Cite: | Discovery of a First-in-Class Inhibitor of the Histone Methyltransferase SETD2 Suitable for Preclinical Studies.
Acs Med.Chem.Lett., 12, 2021
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7LZB
 | | Crystal Structure of SETD2 bound to Compound 2 | | Descriptor: | BETA-MERCAPTOETHANOL, Histone-lysine N-methyltransferase SETD2, N-[(1r,4r)-4-(beta-alanylamino)cyclohexyl]-7-methyl-1H-indole-2-carboxamide, ... | | Authors: | Farrow, N.A, Boriack-Sjodin, P. | | Deposit date: | 2021-03-09 | | Release date: | 2021-09-22 | | Last modified: | 2023-10-18 | | Method: | X-RAY DIFFRACTION (2.28 Å) | | Cite: | Discovery of a First-in-Class Inhibitor of the Histone Methyltransferase SETD2 Suitable for Preclinical Studies.
Acs Med.Chem.Lett., 12, 2021
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7LZD
 | | Crystal Structure of SETD2 bound to Compound 35 | | Descriptor: | 1,2-ETHANEDIOL, DIMETHYL SULFOXIDE, Histone-lysine N-methyltransferase SETD2, ... | | Authors: | Farrow, N.A, Boriack-Sjodin, P. | | Deposit date: | 2021-03-09 | | Release date: | 2021-09-22 | | Last modified: | 2023-10-18 | | Method: | X-RAY DIFFRACTION (1.8 Å) | | Cite: | Discovery of a First-in-Class Inhibitor of the Histone Methyltransferase SETD2 Suitable for Preclinical Studies.
Acs Med.Chem.Lett., 12, 2021
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