6WAD
 
 | | Crystal Structure of Human Protein arginine N-methyltransferase 6 (PRMT6) in complex with MT2739 inhibitor | | 分子名称: | 5-bromo-N-(diphenylmethyl)-N-methylthiophene-2-carboxamide, Protein arginine N-methyltransferase 6, S-ADENOSYL-L-HOMOCYSTEINE | | 著者 | Halabelian, L, Zeng, H, Dong, A, Schapira, M, De Freitas, R.F, Hutchinson, A, Seitova, A, Bountra, C, Edwards, A.M, Arrowsmith, C.H, Brown, P.J, Structural Genomics Consortium (SGC) | | 登録日 | 2020-03-25 | | 公開日 | 2020-09-02 | | 最終更新日 | 2023-10-18 | | 実験手法 | X-RAY DIFFRACTION (2.45 Å) | | 主引用文献 | Crystal Structure of Human Protein arginine N-methyltransferase 6 (PRMT6) in complex with MT2739 inhibitor
to be published
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7LMT
 | | Histone-lysine N-methyltransferase NSD2-PWWP1 with compound MRT10241866a | | 分子名称: | Histone-lysine N-methyltransferase NSD2, UNKNOWN ATOM OR ION, ~{N}-cyclopropyl-3-oxidanylidene-~{N}-(thiophen-2-ylmethyl)-4~{H}-1,4-benzoxazine-7-carboxamide | | 著者 | Lei, M, Freitas, R.F, Dong, A, Schapira, M, Arrowsmith, C.H, Edwards, A.M, Min, J, Structural Genomics Consortium (SGC) | | 登録日 | 2021-02-05 | | 公開日 | 2021-03-10 | | 最終更新日 | 2023-10-18 | | 実験手法 | X-RAY DIFFRACTION (2.27 Å) | | 主引用文献 | Histone-lysine N-methyltransferase NSD2-PWWP1 with compound MRT10241866a
To Be Published
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6DXH
 | | Structure of USP5 zinc-finger ubiquitin binding domain co-crystallized with 4-(4-tert-butylphenyl)-4-oxobutanoate | | 分子名称: | 4-(4-tert-butylphenyl)-4-oxobutanoic acid, UNKNOWN ATOM OR ION, Ubiquitin carboxyl-terminal hydrolase 5, ... | | 著者 | Harding, R.J, Mann, M.K, Ravichandran, M, Ferreira de Freitas, R, Franzoni, I, Bountra, C, Edwards, A.M, Arrowsmith, C.H, Schapira, M, Structural Genomics Consortium (SGC) | | 登録日 | 2018-06-28 | | 公開日 | 2018-07-18 | | 最終更新日 | 2023-10-11 | | 実験手法 | X-RAY DIFFRACTION (2 Å) | | 主引用文献 | Discovery of Small Molecule Antagonists of the USP5 Zinc Finger Ubiquitin-Binding Domain.
J.Med.Chem., 62, 2019
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6DXT
 | | Structure of USP5 zinc-finger ubiquitin binding domain co-crystallized with 3-(5-phenyl-1,3,4-oxadiazol-2-yl)propanoate | | 分子名称: | 1,2-ETHANEDIOL, 3-(5-phenyl-1,3,4-oxadiazol-2-yl)propanoic acid, UNKNOWN ATOM OR ION, ... | | 著者 | Mann, M.K, Harding, R.J, Ravichandran, M, Ferreira de Freitas, R, Franzoni, I, Bountra, C, Edwards, A.M, Arrowsmith, C.M, Schapira, M, Structural Genomics Consortium (SGC) | | 登録日 | 2018-06-29 | | 公開日 | 2018-08-08 | | 最終更新日 | 2023-10-11 | | 実験手法 | X-RAY DIFFRACTION (1.95 Å) | | 主引用文献 | Discovery of Small Molecule Antagonists of the USP5 Zinc Finger Ubiquitin-Binding Domain.
J.Med.Chem., 62, 2019
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6UE6
 | | PWWP1 domain of NSD2 in complex with MR837 | | 分子名称: | 4-cyano-N-cyclopropyl-N-[(thiophen-2-yl)methyl]benzamide, Histone-lysine N-methyltransferase NSD2, UNKNOWN ATOM OR ION | | 著者 | Liu, Y, Tempel, W, De Freitas, R.F, Schapira, M, Brown, P.J, Bountra, C, Edwards, A.M, Arrowsmith, C.H, Min, J, Structural Genomics Consortium (SGC) | | 登録日 | 2019-09-20 | | 公開日 | 2019-11-13 | | 最終更新日 | 2023-10-11 | | 実験手法 | X-RAY DIFFRACTION (2.4 Å) | | 主引用文献 | Discovery of Small-Molecule Antagonists of the PWWP Domain of NSD2.
J.Med.Chem., 64, 2021
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6NFT
 | | Structure of USP5 zinc-finger ubiquitin binding domain co-crystallized with (4-oxoquinazolin-3(4H)-yl)acetic acid | | 分子名称: | (4-oxoquinazolin-3(4H)-yl)acetic acid, 1,2-ETHANEDIOL, UNKNOWN ATOM OR ION, ... | | 著者 | Harding, R.J, Mann, M.K, Tempel, W, Bountra, C, Arrowmsmith, C.M, Edwards, A.M, Schapira, M, Structural Genomics Consortium (SGC) | | 登録日 | 2018-12-20 | | 公開日 | 2019-01-02 | | 最終更新日 | 2021-06-09 | | 実験手法 | X-RAY DIFFRACTION (1.65 Å) | | 主引用文献 | Discovery of Small Molecule Antagonists of the USP5 Zinc Finger Ubiquitin-Binding Domain.
J.Med.Chem., 62, 2019
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5U4X
 | | Coactivator-associated arginine methyltransferase 1 with TP-064 | | 分子名称: | Histone-arginine methyltransferase CARM1, N-methyl-N-[(2-{1-[2-(methylamino)ethyl]piperidin-4-yl}pyridin-4-yl)methyl]-3-phenoxybenzamide, S-ADENOSYL-L-HOMOCYSTEINE, ... | | 著者 | DONG, A, ZENG, H, Saikatendu, K.S, STONE, H, WALKER, J.R, Seitova, A, Hutchinson, A, Bountra, C, Arrowsmith, C.H, Edwards, A.M, BROWN, P.J, WU, H, Structural Genomics Consortium (SGC) | | 登録日 | 2016-12-06 | | 公開日 | 2016-12-21 | | 最終更新日 | 2023-10-04 | | 実験手法 | X-RAY DIFFRACTION (1.88 Å) | | 主引用文献 | TP-064, a potent and selective small molecule inhibitor of PRMT4 for multiple myeloma.
Oncotarget, 9, 2018
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6AU2
 | | Crystal structure of SETDB1 Tudor domain with aryl triazole fragments | | 分子名称: | 1,2-ETHANEDIOL, 1-methyl-4H,6H-[1,2,4]triazolo[4,3-a][4,1]benzoxazepine, BETA-MERCAPTOETHANOL, ... | | 著者 | MADER, P, Mendoza-Sanchez, R, IQBAL, A, DONG, A, DOBROVETSKY, E, CORLESS, V.B, LIEW, S.K, TEMPEL, W, SMIL, D, DELA SENA, C.C, KENNEDY, S, DIAZ, D, HOLOWNIA, A, VEDADI, M, BROWN, P.J, SANTHAKUMAR, V, Bountra, C, Edwards, A.M, YUDIN, A.K, Arrowsmith, C.H, Structural Genomics Consortium (SGC) | | 登録日 | 2017-08-30 | | 公開日 | 2017-10-11 | | 最終更新日 | 2019-10-16 | | 実験手法 | X-RAY DIFFRACTION (1.63 Å) | | 主引用文献 | Identification and characterization of the first fragment hits for SETDB1 Tudor domain.
Bioorg.Med.Chem., 27, 2019
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7MDN
 | | Histone-lysine N-methyltransferase NSD2-PWWP1 with compound MRT10241866a | | 分子名称: | Histone-lysine N-methyltransferase NSD2, UNKNOWN ATOM OR ION, ~{N}-cyclopropyl-3-oxidanylidene-~{N}-(thiophen-2-ylmethyl)-4~{H}-1,4-benzoxazine-7-carboxamide | | 著者 | Lei, M, Freitas, R.F, Dong, A, Schapira, M, Arrowsmith, C.H, Edwards, A.M, Min, J, Structural Genomics Consortium (SGC) | | 登録日 | 2021-04-05 | | 公開日 | 2021-05-05 | | 最終更新日 | 2023-10-18 | | 実験手法 | X-RAY DIFFRACTION (2.42 Å) | | 主引用文献 | A chemical probe targeting the PWWP domain alters NSD2 nucleolar localization.
Nat.Chem.Biol., 18, 2022
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6P9G
 | | Structure of USP5 zinc-finger ubiquitin binding domain co-crystallized with 2-(4-oxoquinazolin-3(4H)-yl)propanoic acid | | 分子名称: | (2R)-2-(4-oxoquinazolin-3(4H)-yl)propanoic acid, UNKNOWN ATOM OR ION, Ubiquitin carboxyl-terminal hydrolase 5, ... | | 著者 | Tempel, W, Mann, M.K, Harding, R.J, Bountra, C, Arrowsmith, C.H, Edwards, A.M, Schapira, M, Structural Genomics Consortium (SGC) | | 登録日 | 2019-06-10 | | 公開日 | 2019-09-18 | | 最終更新日 | 2023-10-11 | | 実験手法 | X-RAY DIFFRACTION (2.1 Å) | | 主引用文献 | Discovery of Small Molecule Antagonists of the USP5 Zinc Finger Ubiquitin-Binding Domain.
J.Med.Chem., 62, 2019
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