3M7F
 
 | | Crystal structure of the Nedd4 C2/Grb10 SH2 complex | | 分子名称: | E3 ubiquitin-protein ligase NEDD4, Growth factor receptor-bound protein 10 | | 著者 | Huang, Q, Szebenyi, M. | | 登録日 | 2010-03-16 | | 公開日 | 2010-10-27 | | 最終更新日 | 2023-09-06 | | 実験手法 | X-RAY DIFFRACTION (2 Å) | | 主引用文献 | Structural Basis for the Interaction between the Growth Factor-binding Protein GRB10 and the E3 Ubiquitin Ligase NEDD4.
J.Biol.Chem., 285, 2010
|
|
3NHN
 | | Crystal structure of the SRC-family kinase HCK SH3-SH2-linker regulatory region | | 分子名称: | Tyrosine-protein kinase HCK | | 著者 | Alvarado, J.J, Betts, L, Moroco, J.A, Smithgall, T.E, Yeh, J.I. | | 登録日 | 2010-06-14 | | 公開日 | 2010-09-01 | | 最終更新日 | 2023-09-06 | | 実験手法 | X-RAY DIFFRACTION (2.61 Å) | | 主引用文献 | Crystal Structure of the Src Family Kinase Hck SH3-SH2 Linker Regulatory Region Supports an SH3-dominant Activation Mechanism.
J.Biol.Chem., 285, 2010
|
|
4XEY
 | |
4XZ1
 | | ZAP-70-tSH2:Compound-B adduct | | 分子名称: | 2-[(7-chloro-4-nitro-2,1,3-benzoxadiazol-5-yl)amino]ethanol, Tyrosine-protein kinase ZAP-70, doubly phosphorylated ITAM peptide | | 著者 | Barros, T, Kuriyan, J, Winger, J.A, Visperas, P.R. | | 登録日 | 2015-02-03 | | 公開日 | 2015-07-29 | | 最終更新日 | 2023-11-15 | | 実験手法 | X-RAY DIFFRACTION (2.8 Å) | | 主引用文献 | Modification by covalent reaction or oxidation of cysteine residues in the tandem-SH2 domains of ZAP-70 and Syk can block phosphopeptide binding.
Biochem. J., 465, 2015
|
|
4Y5U
 | | Transcription factor | | 分子名称: | NICKEL (II) ION, Signal transducer and activator of transcription 6 | | 著者 | Li, J, Niu, F, Ouyang, S, Liu, Z. | | 登録日 | 2015-02-12 | | 公開日 | 2016-02-17 | | 最終更新日 | 2023-11-15 | | 実験手法 | X-RAY DIFFRACTION (2.708 Å) | | 主引用文献 | Structural basis for DNA recognition by STAT6
Proc.Natl.Acad.Sci.USA, 113, 2016
|
|
4Y5W
 | | Transcription factor-DNA complex | | 分子名称: | DNA (5'-D(P*AP*TP*GP*GP*AP*TP*TP*TP*CP*CP*TP*AP*GP*GP*AP*AP*GP*AP*CP*AP*A)-3'), DNA (5'-D(P*TP*TP*GP*TP*CP*TP*TP*CP*CP*TP*AP*GP*GP*AP*AP*AP*TP*CP*CP*AP*T)-3'), Signal transducer and activator of transcription 6 | | 著者 | Li, J, Niu, F, Ouyang, S, Liu, Z. | | 登録日 | 2015-02-12 | | 公開日 | 2016-02-17 | | 最終更新日 | 2023-11-15 | | 実験手法 | X-RAY DIFFRACTION (3.104 Å) | | 主引用文献 | Structural basis for DNA recognition by STAT6
Proc.Natl.Acad.Sci.USA, 113, 2016
|
|
7TVA
 | | Stat5a Core in complex with AK2292 | | 分子名称: | DI(HYDROXYETHYL)ETHER, MALONATE ION, N-{5-[difluoro(phosphono)methyl]-1-benzothiophene-2-carbonyl}-3-methyl-L-valyl-L-prolyl-N-(5-{2-[(3R)-2,6-dioxopiperidin-3-yl]-1-oxo-2,3-dihydro-1H-isoindol-4-yl}pent-4-yn-1-yl)-N-methyl-N~3~-[4-(1,3-thiazol-2-yl)phenyl]-beta-alaninamide, ... | | 著者 | Meagher, J.L, Stuckey, J.A. | | 登録日 | 2022-02-04 | | 公開日 | 2023-02-15 | | 最終更新日 | 2024-04-03 | | 実験手法 | X-RAY DIFFRACTION (2.835 Å) | | 主引用文献 | A selective small-molecule STAT5 PROTAC degrader capable of achieving tumor regression in vivo.
Nat.Chem.Biol., 19, 2023
|
|
7VXG
 | |
4YKN
 | | Pi3K alpha lipid kinase with Active Site Inhibitor | | 分子名称: | 3-(6-methoxypyridin-3-yl)-5-[({4-[(5-methyl-1,3,4-thiadiazol-2-yl)sulfamoyl]phenyl}amino)methyl]benzoic acid, Phosphatidylinositol 3-kinase regulatory subunit alpha,Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform fusion protein | | 著者 | Elkins, P.A. | | 登録日 | 2015-03-04 | | 公開日 | 2015-06-17 | | 最終更新日 | 2024-02-28 | | 実験手法 | X-RAY DIFFRACTION (2.9 Å) | | 主引用文献 | Discovery of a Potent Class of PI3K alpha Inhibitors with Unique Binding Mode via Encoded Library Technology (ELT).
Acs Med.Chem.Lett., 6, 2015
|
|
7UY3
 | | Crystal structure of human Fgr tyrosine kinase in complex with TL02-59 | | 分子名称: | 1,2-ETHANEDIOL, 3-[(6,7-dimethoxyquinazolin-4-yl)oxy]-N-{4-[(4-ethylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}-4-methylbenzamide, GLYCEROL, ... | | 著者 | Du, S, Alvarado, J.J, Smithgall, T.E. | | 登録日 | 2022-05-06 | | 公開日 | 2022-12-28 | | 最終更新日 | 2023-11-15 | | 実験手法 | X-RAY DIFFRACTION (2.99 Å) | | 主引用文献 | ATP-site inhibitors induce unique conformations of the acute myeloid leukemia-associated Src-family kinase, Fgr.
Structure, 30, 2022
|
|
7UY0
 | | Crystal structure of human Fgr tyrosine kinase in complex with A-419259 | | 分子名称: | 7-[trans-4-(4-methylpiperazin-1-yl)cyclohexyl]-5-(4-phenoxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine, CHLORIDE ION, GLYCEROL, ... | | 著者 | Du, S, Alvarado, J.J, Smithgall, T.E. | | 登録日 | 2022-05-06 | | 公開日 | 2022-12-28 | | 最終更新日 | 2023-11-15 | | 実験手法 | X-RAY DIFFRACTION (2.55 Å) | | 主引用文献 | ATP-site inhibitors induce unique conformations of the acute myeloid leukemia-associated Src-family kinase, Fgr.
Structure, 30, 2022
|
|
8AM0
 | | Crystal structure of human T1061E PI3Kalpha in complex with its regulatory subunit and the inhibitor GDC-0077 (Inavolisib) | | 分子名称: | (2R)-2-[[2-[(4S)-4-[bis(fluoranyl)methyl]-2-oxidanylidene-1,3-oxazolidin-3-yl]-5,6-dihydroimidazo[1,2-d][1,4]benzoxazepin-9-yl]amino]propanamide, 1,2-ETHANEDIOL, CHLORIDE ION, ... | | 著者 | Goncalves, M, Johnson, J.L, Roewer, K.M. | | 登録日 | 2022-08-02 | | 公開日 | 2023-12-13 | | 最終更新日 | 2024-01-03 | | 実験手法 | X-RAY DIFFRACTION (2.818 Å) | | 主引用文献 | Epinephrine inhibits PI3K alpha via the Hippo kinases.
Cell Rep, 42, 2023
|
|
3GQI
 | | Crystal Structure of activated receptor tyrosine kinase in complex with substrates | | 分子名称: | Basic fibroblast growth factor receptor 1, DECAVANADATE, MAGNESIUM ION, ... | | 著者 | Bae, J.H, Lew, E.D, Yuzawa, S, Tome, F, Lax, I, Schlessinger, J. | | 登録日 | 2009-03-24 | | 公開日 | 2009-08-18 | | 最終更新日 | 2023-11-22 | | 実験手法 | X-RAY DIFFRACTION (2.5 Å) | | 主引用文献 | The selectivity of receptor tyrosine kinase signaling is controlled by a secondary SH2 domain binding site.
Cell(Cambridge,Mass.), 138, 2009
|
|
1X27
 | | Crystal Structure of Lck SH2-SH3 with SH2 binding site of p130Cas | | 分子名称: | CRK-associated substrate, Proto-oncogene tyrosine-protein kinase LCK, SODIUM ION | | 著者 | Nasertorabi, F, Tars, K, Becherer, K, Kodandapani, R, Liljas, L, Vuori, K, Ely, K.R. | | 登録日 | 2005-04-20 | | 公開日 | 2006-02-07 | | 最終更新日 | 2023-11-15 | | 実験手法 | X-RAY DIFFRACTION (2.7 Å) | | 主引用文献 | Molecular basis for regulation of Src by the docking protein p130Cas
J.MOL.RECOG., 19, 2006
|
|
4OHI
 | | LEOPARD Syndrome-Associated SHP2/Q510E mutant | | 分子名称: | Tyrosine-protein phosphatase non-receptor type 11 | | 著者 | Yu, Z.H, Zhang, R.Y, Walls, C.D, Chen, L, Zhang, S, Wu, L, Wang, L, Liu, S, Zhang, Z.Y. | | 登録日 | 2014-01-17 | | 公開日 | 2014-09-24 | | 最終更新日 | 2023-09-20 | | 実験手法 | X-RAY DIFFRACTION (2.2 Å) | | 主引用文献 | Molecular basis of gain-of-function LEOPARD syndrome-associated SHP2 mutations.
Biochemistry, 53, 2014
|
|
4OHL
 | | LEOPARD Syndrome-Associated SHP2/T468M mutant | | 分子名称: | Tyrosine-protein phosphatase non-receptor type 11 | | 著者 | Yu, Z.H, Zhang, R.Y, Walls, C.D, Chen, L, Zhang, S, Wu, L, Wang, L, Liu, S, Zhang, Z.Y. | | 登録日 | 2014-01-17 | | 公開日 | 2014-09-24 | | 最終更新日 | 2023-09-20 | | 実験手法 | X-RAY DIFFRACTION (2.4 Å) | | 主引用文献 | Molecular basis of gain-of-function LEOPARD syndrome-associated SHP2 mutations.
Biochemistry, 53, 2014
|
|
7RCT
 | |
4OHH
 | | LEOPARD Syndrome-Associated SHP2/Q506P mutant | | 分子名称: | Tyrosine-protein phosphatase non-receptor type 11 | | 著者 | Yu, Z.H, Zhang, R.Y, Walls, C.D, Chen, L, Zhang, S, Wu, L, Wang, L, Liu, S, Zhang, Z.Y. | | 登録日 | 2014-01-17 | | 公開日 | 2014-09-24 | | 最終更新日 | 2023-09-20 | | 実験手法 | X-RAY DIFFRACTION (2.7 Å) | | 主引用文献 | Molecular basis of gain-of-function LEOPARD syndrome-associated SHP2 mutations.
Biochemistry, 53, 2014
|
|
4GWF
 | | Crystal structure of the tyrosine phosphatase SHP-2 with Y279C mutation | | 分子名称: | 1,2-ETHANEDIOL, DI(HYDROXYETHYL)ETHER, GLYCEROL, ... | | 著者 | Qiu, W, Lin, A, Hutchinson, A, Romanov, V, Ruzanov, M, Thompson, C, Lam, K, Kisselman, G, Battaile, K, Chirgadze, N.Y. | | 登録日 | 2012-09-03 | | 公開日 | 2013-09-04 | | 最終更新日 | 2023-09-13 | | 実験手法 | X-RAY DIFFRACTION (2.1 Å) | | 主引用文献 | Crystal structure of the tyrosine phosphatase SHP-2 with Y279C mutation
TO BE PUBLISHED
|
|
3HIZ
 | | Crystal structure of p110alpha H1047R mutant in complex with niSH2 of p85alpha | | 分子名称: | Phosphatidylinositol 3-kinase regulatory subunit alpha, Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha isoform | | 著者 | Amzel, L.M, Vogelstein, B, Gabelli, S.B, Mandelker, D. | | 登録日 | 2009-05-20 | | 公開日 | 2009-09-29 | | 最終更新日 | 2023-09-06 | | 実験手法 | X-RAY DIFFRACTION (3.3 Å) | | 主引用文献 | A frequent kinase domain mutation that changes the interaction between PI3K{alpha} and the membrane.
Proc.Natl.Acad.Sci.USA, 106, 2009
|
|
7R75
 | | Structure of human SHP2 in complex with compound 16 | | 分子名称: | 6-(4-amino-4-methylpiperidin-1-yl)-3-(3-chlorophenyl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one, Tyrosine-protein phosphatase non-receptor type 11 | | 著者 | Leonard, P.G, Cross, J. | | 登録日 | 2021-06-24 | | 公開日 | 2021-10-27 | | 最終更新日 | 2023-10-18 | | 実験手法 | X-RAY DIFFRACTION (2.83 Å) | | 主引用文献 | Discovery of 6-[(3 S ,4 S )-4-Amino-3-methyl-2-oxa-8-azaspiro[4.5]decan-8-yl]-3-(2,3-dichlorophenyl)-2-methyl-3,4-dihydropyrimidin-4-one (IACS-15414), a Potent and Orally Bioavailable SHP2 Inhibitor.
J.Med.Chem., 64, 2021
|
|
7R7D
 | | Structure of human SHP2 in complex with compound 22 | | 分子名称: | 4-[6-(4-amino-4-methylpiperidin-1-yl)-1H-pyrazolo[3,4-b]pyrazin-3-yl]-3-chloro-N-methylpyridin-2-amine, TETRAETHYLENE GLYCOL, Tyrosine-protein phosphatase non-receptor type 11 | | 著者 | Leonard, P.G, Cross, J. | | 登録日 | 2021-06-24 | | 公開日 | 2021-10-27 | | 最終更新日 | 2023-10-18 | | 実験手法 | X-RAY DIFFRACTION (2.6 Å) | | 主引用文献 | Discovery of 6-[(3 S ,4 S )-4-Amino-3-methyl-2-oxa-8-azaspiro[4.5]decan-8-yl]-3-(2,3-dichlorophenyl)-2-methyl-3,4-dihydropyrimidin-4-one (IACS-15414), a Potent and Orally Bioavailable SHP2 Inhibitor.
J.Med.Chem., 64, 2021
|
|
3HHM
 | | Crystal structure of p110alpha H1047R mutant in complex with niSH2 of p85alpha and the drug wortmannin | | 分子名称: | (1S,6BR,9AS,11R,11BR)-9A,11B-DIMETHYL-1-[(METHYLOXY)METHYL]-3,6,9-TRIOXO-1,6,6B,7,8,9,9A,10,11,11B-DECAHYDRO-3H-FURO[4, 3,2-DE]INDENO[4,5-H][2]BENZOPYRAN-11-YL ACETATE, Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha isoform, ... | | 著者 | Amzel, L.M, Vogelstein, B, Gabelli, S.B, Mandelker, D. | | 登録日 | 2009-05-15 | | 公開日 | 2009-09-29 | | 最終更新日 | 2023-09-06 | | 実験手法 | X-RAY DIFFRACTION (2.8 Å) | | 主引用文献 | A frequent kinase domain mutation that changes the interaction between PI3K{alpha} and the membrane.
Proc.Natl.Acad.Sci.USA, 106, 2009
|
|
7R7L
 | | Structure of human SHP2 in complex with compound 30 | | 分子名称: | 6-[(3S,4S)-4-amino-3-methyl-2-oxa-8-azaspiro[4.5]decan-8-yl]-3-(2,3-dichlorophenyl)-2-methylpyrimidin-4(3H)-one, Tyrosine-protein phosphatase non-receptor type 11 | | 著者 | Leonard, P.G, Cross, J. | | 登録日 | 2021-06-24 | | 公開日 | 2021-10-27 | | 最終更新日 | 2023-10-18 | | 実験手法 | X-RAY DIFFRACTION (3 Å) | | 主引用文献 | Discovery of 6-[(3 S ,4 S )-4-Amino-3-methyl-2-oxa-8-azaspiro[4.5]decan-8-yl]-3-(2,3-dichlorophenyl)-2-methyl-3,4-dihydropyrimidin-4-one (IACS-15414), a Potent and Orally Bioavailable SHP2 Inhibitor.
J.Med.Chem., 64, 2021
|
|
7R7I
 | | Structure of human SHP2 in complex with compound 27 | | 分子名称: | Tyrosine-protein phosphatase non-receptor type 11, [3-(4-amino-4-methylpiperidin-1-yl)-6-(2,3-dichlorophenyl)-5-methylpyrazin-2-yl]methanol | | 著者 | Leonard, P.G, Cross, J. | | 登録日 | 2021-06-24 | | 公開日 | 2021-10-27 | | 最終更新日 | 2023-10-18 | | 実験手法 | X-RAY DIFFRACTION (2.85 Å) | | 主引用文献 | Discovery of 6-[(3 S ,4 S )-4-Amino-3-methyl-2-oxa-8-azaspiro[4.5]decan-8-yl]-3-(2,3-dichlorophenyl)-2-methyl-3,4-dihydropyrimidin-4-one (IACS-15414), a Potent and Orally Bioavailable SHP2 Inhibitor.
J.Med.Chem., 64, 2021
|
|
