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
|
|
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
|
|
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
|
|
7VXG
 | |
7XHQ
 | | Small-molecule Allosteric Regulation Mechanism of SHP2 | | 分子名称: | 2-[(3S,4R)-4-azanyl-3-methyl-2-oxa-8-azaspiro[4.5]decan-8-yl]-5-[2,3-bis(chloranyl)phenyl]-3-methyl-pyrrolo[2,1-f][1,2,4]triazin-4-one, Tyrosine-protein phosphatase non-receptor type 11 | | 著者 | Luo, Y, Zhu, J, Yu, K, Liu, B. | | 登録日 | 2022-04-09 | | 公開日 | 2023-02-15 | | 最終更新日 | 2023-11-29 | | 実験手法 | X-RAY DIFFRACTION (2.2 Å) | | 主引用文献 | Discovery of the SHP2 allosteric inhibitor 2-((3R,4R)-4-amino-3-methyl-2-oxa-8-azaspiro[4.5]decan-8-yl)-5-(2,3-dichlorophenyl)-3-methylpyrrolo[2,1-f][1,2,4] triazin-4(3H)-one.
J Enzyme Inhib Med Chem, 38, 2023
|
|
7Z3J
 | | Structure of crystallisable rat Phospholipase C gamma 1 in complex with inositol 1,4,5-trisphosphate | | 分子名称: | 1-phosphatidylinositol 4,5-bisphosphate phosphodiesterase gamma-1, CALCIUM ION, D-MYO-INOSITOL-1,4,5-TRIPHOSPHATE, ... | | 著者 | Pinotsis, N, Bunney, T.D, Katan, M. | | 登録日 | 2022-03-02 | | 公開日 | 2022-07-20 | | 最終更新日 | 2024-01-31 | | 実験手法 | X-RAY DIFFRACTION (2 Å) | | 主引用文献 | Characterization of the membrane interactions of phospholipase C gamma reveals key features of the active enzyme.
Sci Adv, 8, 2022
|
|
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
|
|
6JMF
 | |
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
|
|
1UUS
 | | Structure of an activated Dictyostelium STAT in its DNA-unbound form | | 分子名称: | STAT PROTEIN | | 著者 | Soler-Lopez, M, Petosa, C, Fukuzawa, M, Ravelli, R, Williams, J.G, Muller, C.W. | | 登録日 | 2004-01-09 | | 公開日 | 2004-03-26 | | 最終更新日 | 2019-10-09 | | 実験手法 | X-RAY DIFFRACTION (2.8 Å) | | 主引用文献 | Structure of an Activated Dictyostelium Stat in its DNA-Unbound Form
Mol.Cell, 13, 2004
|
|
7YQE
 | |
1UUR
 | | Structure of an activated Dictyostelium STAT in its DNA-unbound form | | 分子名称: | STATA PROTEIN | | 著者 | Soler-Lopez, M, Petosa, C, Fukuzawa, M, Ravelli, R, Williams, J.G, Muller, C.W. | | 登録日 | 2004-01-09 | | 公開日 | 2004-03-26 | | 最終更新日 | 2011-07-13 | | 実験手法 | X-RAY DIFFRACTION (2.7 Å) | | 主引用文献 | Structure of an Activated Dictyostelium Stat in its DNA-Unbound Form
Mol.Cell, 13, 2004
|
|
7ZN7
 | | Cryo-EM structure of RCMV-E E27 bound to human DDB1 (deltaBPB) and rat STAT2 CCD | | 分子名称: | B27a, DNA damage-binding protein 1, Signal transducer and activator of transcription, ... | | 著者 | Lauer, S, Spahn, C.M.T, Schwefel, D. | | 登録日 | 2022-04-20 | | 公開日 | 2022-11-09 | | 最終更新日 | 2023-03-15 | | 実験手法 | ELECTRON MICROSCOPY (3.78 Å) | | 主引用文献 | Structural mechanism of CRL4-instructed STAT2 degradation via a novel cytomegaloviral DCAF receptor.
Embo J., 42, 2023
|
|
7ZNN
 | | Cryo-EM structure of RCMV-E E27 bound to human DDB1 (deltaBPB) and full-length rat STAT2 | | 分子名称: | B27a, DNA damage-binding protein 1, Signal transducer and activator of transcription, ... | | 著者 | Lauer, S, Spahn, C.M.T, Schwefel, D. | | 登録日 | 2022-04-21 | | 公開日 | 2022-11-09 | | 最終更新日 | 2023-03-15 | | 実験手法 | ELECTRON MICROSCOPY (4.8 Å) | | 主引用文献 | Structural mechanism of CRL4-instructed STAT2 degradation via a novel cytomegaloviral DCAF receptor.
Embo J., 42, 2023
|
|
7ZLP
 | | Crystal structure of SOCS2:ElonginB:ElonginC in complex with compound 9 | | 分子名称: | Elongin-B, Elongin-C, PHOSPHATE ION, ... | | 著者 | Ramachandran, S, Ciulli, A, Makukhin, N. | | 登録日 | 2022-04-15 | | 公開日 | 2023-04-26 | | 最終更新日 | 2024-05-01 | | 実験手法 | X-RAY DIFFRACTION (1.94 Å) | | 主引用文献 | Structure-based design of a phosphotyrosine-masked covalent ligand targeting the E3 ligase SOCS2.
Nat Commun, 14, 2023
|
|
7ZLR
 | | Crystal structure of SOCS2:ElonginB:ElonginC in complex with compound 13 | | 分子名称: | Elongin-B, Elongin-C, Suppressor of cytokine signaling 2, ... | | 著者 | Ramachandran, S, Ciulli, A, Makukhin, N. | | 登録日 | 2022-04-15 | | 公開日 | 2023-04-26 | | 最終更新日 | 2024-05-01 | | 実験手法 | X-RAY DIFFRACTION (2.01 Å) | | 主引用文献 | Structure-based design of a phosphotyrosine-masked covalent ligand targeting the E3 ligase SOCS2.
Nat Commun, 14, 2023
|
|
7ZLM
 | | Crystal structure of SOCS2:ElonginB:ElonginC in complex with compound MN551 | | 分子名称: | Elongin-B, Elongin-C, Suppressor of cytokine signaling 2, ... | | 著者 | Ramachandran, S, Ciulli, A, Makukhin, N. | | 登録日 | 2022-04-15 | | 公開日 | 2023-04-26 | | 最終更新日 | 2024-05-01 | | 実験手法 | X-RAY DIFFRACTION (1.79 Å) | | 主引用文献 | Structure-based design of a phosphotyrosine-masked covalent ligand targeting the E3 ligase SOCS2.
Nat Commun, 14, 2023
|
|
7ZLN
 | | Crystal structure of SOCS2:ElonginB:ElonginC in complex with compound 11 | | 分子名称: | Elongin-B, Elongin-C, Suppressor of cytokine signaling 2, ... | | 著者 | Ramachandran, S, Ciulli, A, Makukhin, N. | | 登録日 | 2022-04-15 | | 公開日 | 2023-04-26 | | 最終更新日 | 2024-05-01 | | 実験手法 | X-RAY DIFFRACTION (2.6 Å) | | 主引用文献 | Structure-based design of a phosphotyrosine-masked covalent ligand targeting the E3 ligase SOCS2.
Nat Commun, 14, 2023
|
|
7ZLO
 | | Crystal structure of SOCS2:ElonginB:ElonginC in complex with compound 12 | | 分子名称: | Elongin-B, Elongin-C, Suppressor of cytokine signaling 2, ... | | 著者 | Ramachandran, S, Ciulli, A, Makukhin, N. | | 登録日 | 2022-04-15 | | 公開日 | 2023-04-26 | | 最終更新日 | 2024-05-01 | | 実験手法 | X-RAY DIFFRACTION (2.22 Å) | | 主引用文献 | Structure-based design of a phosphotyrosine-masked covalent ligand targeting the E3 ligase SOCS2.
Nat Commun, 14, 2023
|
|
7ZLS
 | | co-crystal structure of SOCS2:ElonginB:ElonginC in complex with compound 13 | | 分子名称: | 1,2-ETHANEDIOL, Elongin-B, Elongin-C, ... | | 著者 | Ramachandran, S, Ciulli, A, Makukhin, N. | | 登録日 | 2022-04-15 | | 公開日 | 2023-04-26 | | 最終更新日 | 2024-05-01 | | 実験手法 | X-RAY DIFFRACTION (1.92 Å) | | 主引用文献 | Structure-based design of a phosphotyrosine-masked covalent ligand targeting the E3 ligase SOCS2.
Nat Commun, 14, 2023
|
|
8B5Y
 | | SHP2 in complex with allosteric imidazopyrazine inhibitor | | 分子名称: | (1~{S})-1'-[5-[2-(trifluoromethyl)pyridin-3-yl]sulfanyl-3~{H}-imidazo[4,5-b]pyrazin-2-yl]spiro[1,3-dihydroindene-2,4'-piperidine]-1-amine, FORMIC ACID, Tyrosine-protein phosphatase non-receptor type 11 | | 著者 | Torrente, E, Petrocchi, A. | | 登録日 | 2022-09-25 | | 公開日 | 2023-01-18 | | 最終更新日 | 2024-02-07 | | 実験手法 | X-RAY DIFFRACTION (1.83 Å) | | 主引用文献 | Discovery of a Novel Series of Imidazopyrazine Derivatives as Potent SHP2 Allosteric Inhibitors.
Acs Med.Chem.Lett., 14, 2023
|
|
4D8K
 | |
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
|
|
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
|
|
4DGP
 | | The wild-type Src homology 2 (SH2)-domain containing protein tyrosine phosphatase-2 (SHP2) | | 分子名称: | Tyrosine-protein phosphatase non-receptor type 11 | | 著者 | Yu, Z.H, Xu, J, Walls, C.D, Chen, L, Zhang, S, Wu, L, Wang, L.N, Liu, S.J, Zhang, Z.Y. | | 登録日 | 2012-01-26 | | 公開日 | 2013-03-06 | | 最終更新日 | 2024-02-28 | | 実験手法 | X-RAY DIFFRACTION (2.3 Å) | | 主引用文献 | Structural and Mechanistic Insights into LEOPARD Syndrome-Associated SHP2 Mutations.
J.Biol.Chem., 288, 2013
|
|
