6H60
 
 | | pseudo-atomic structural model of the E3BP component of the human pyruvate dehydrogenase multienzyme complex | | Descriptor: | Pyruvate dehydrogenase protein X component, mitochondrial | | Authors: | Haselbach, D, Prajapati, S, Tittmann, K, Stark, H. | | Deposit date: | 2018-07-25 | | Release date: | 2019-06-05 | | Last modified: | 2019-12-11 | | Method: | ELECTRON MICROSCOPY (6 Å) | | Cite: | Structural and Functional Analyses of the Human PDH Complex Suggest a "Division-of-Labor" Mechanism by Local E1 and E3 Clusters.
Structure, 27, 2019
|
|
6H55
 | | core of the human pyruvate dehydrogenase (E2) | | Descriptor: | Dihydrolipoyllysine-residue acetyltransferase component of pyruvate dehydrogenase complex, mitochondrial | | Authors: | Haselbach, D, Prajapati, S, Tittmann, K, Stark, H. | | Deposit date: | 2018-07-23 | | Release date: | 2019-06-05 | | Last modified: | 2019-12-18 | | Method: | ELECTRON MICROSCOPY (6 Å) | | Cite: | Structural and Functional Analyses of the Human PDH Complex Suggest a "Division-of-Labor" Mechanism by Local E1 and E3 Clusters.
Structure, 27, 2019
|
|
6P69
 | |
5VND
 | | Crystal structure of FGFR1-Y563C (FGFR4 surrogate) covalently bound to H3B-6527 | | Descriptor: | 1,2-ETHANEDIOL, Fibroblast growth factor receptor 1, N-{2-[(6-{[(2,6-dichloro-3,5-dimethoxyphenyl)carbamoyl](methyl)amino}pyrimidin-4-yl)amino]-5-(4-ethylpiperazin-1-yl)phenyl}propanamide, ... | | Authors: | Tsai, J.H.C, Reynolds, D, Fekkes, P, Smith, P, Larsen, N.A. | | Deposit date: | 2017-04-30 | | Release date: | 2017-05-24 | | Last modified: | 2023-10-04 | | Method: | X-RAY DIFFRACTION (2.2 Å) | | Cite: | H3B-6527 Is a Potent and Selective Inhibitor of FGFR4 in FGF19-Driven Hepatocellular Carcinoma.
Cancer Res., 77, 2017
|
|
7LUB
 | |
7MBH
 | | Structure of Human Enolase 2 in complex with phosphoserine | | Descriptor: | 1,2-ETHANEDIOL, ACETATE ION, Gamma-enolase, ... | | Authors: | Leonard, P.G, Hicks, K.G, Rutter, J. | | Deposit date: | 2021-03-31 | | Release date: | 2022-11-09 | | Last modified: | 2023-10-25 | | Method: | X-RAY DIFFRACTION (2.1 Å) | | Cite: | Protein-metabolite interactomics of carbohydrate metabolism reveal regulation of lactate dehydrogenase.
Science, 379, 2023
|
|
6CHZ
 | | Estrogen Receptor Alpha Y537S bound to antagonist H3B-9224. | | Descriptor: | 1,2-ETHANEDIOL, 4-[(2-{4-[(1E)-1-(1H-indazol-5-yl)-2-phenylbut-1-en-1-yl]phenoxy}ethyl)amino]-N,N-dimethylbutanamide, Estrogen receptor | | Authors: | Larsen, N.A. | | Deposit date: | 2018-02-23 | | Release date: | 2018-03-21 | | Last modified: | 2024-03-13 | | Method: | X-RAY DIFFRACTION (1.68 Å) | | Cite: | Discovery of Selective Estrogen Receptor Covalent Antagonists for the Treatment of ER alphaWTand ER alphaMUTBreast Cancer.
Cancer Discov, 8, 2018
|
|
6CHW
 | | Estrogen Receptor Alpha Y537S covalently bound to antagonist H3B-5942. | | Descriptor: | 1,2-ETHANEDIOL, 4-[(2-{4-[(1E)-1-(1H-indazol-5-yl)-2-phenylbut-1-en-1-yl]phenoxy}ethyl)amino]-N,N-dimethylbutanamide, DIMETHYL SULFOXIDE, ... | | Authors: | Larsen, N.A. | | Deposit date: | 2018-02-23 | | Release date: | 2018-03-21 | | Last modified: | 2020-02-26 | | Method: | X-RAY DIFFRACTION (1.89 Å) | | Cite: | Discovery of Selective Estrogen Receptor Covalent Antagonists for the Treatment of ER alphaWTand ER alphaMUTBreast Cancer.
Cancer Discov, 8, 2018
|
|
5SYB
 | | Crystal structure of human PHF5A | | Descriptor: | 1,2-ETHANEDIOL, PHD finger-like domain-containing protein 5A, ZINC ION | | Authors: | Tsai, J.H.C, Teng, T, Zhu, P, Fekkes, P, Larsen, N.A. | | Deposit date: | 2016-08-10 | | Release date: | 2016-09-07 | | Last modified: | 2024-03-06 | | Method: | X-RAY DIFFRACTION (1.82 Å) | | Cite: | Splicing modulators act at the branch point adenosine binding pocket defined by the PHF5A-SF3b complex.
Nat Commun, 8, 2017
|
|
7KIA
 | | Crystal structure of FGFR2 kinase domain gatekeeper mutant V564F in complex with covalent compound 19 | | Descriptor: | 1-[4-(4-{4-(4-methylpiperazin-1-yl)-6-[(3-methyl-1H-pyrazol-5-yl)amino]pyrimidin-2-yl}phenyl)piperidin-1-yl]prop-2-en-1-one, CITRATE ANION, Fibroblast growth factor receptor 2, ... | | Authors: | Ke, J, Wibowo, A.S, Carter, J.J, Larsen, N.A. | | Deposit date: | 2020-10-23 | | Release date: | 2021-02-10 | | Last modified: | 2023-10-18 | | Method: | X-RAY DIFFRACTION (2.22 Å) | | Cite: | Discovery of Aminopyrazole Derivatives as Potent Inhibitors of Wild-Type and Gatekeeper Mutant FGFR2 and 3.
Acs Med.Chem.Lett., 12, 2021
|
|
7KIE
 | | Crystal structure of FGFR2 kinase domain gatekeeper mutant V564F in complex with covalent compound 3 | | Descriptor: | CITRATE ANION, Fibroblast growth factor receptor 2, GLYCEROL, ... | | Authors: | Ke, J, Wibowo, A.S, Carter, J.J, Larsen, N.A. | | Deposit date: | 2020-10-23 | | Release date: | 2021-02-10 | | Last modified: | 2023-10-18 | | Method: | X-RAY DIFFRACTION (2.47 Å) | | Cite: | Discovery of Aminopyrazole Derivatives as Potent Inhibitors of Wild-Type and Gatekeeper Mutant FGFR2 and 3.
Acs Med.Chem.Lett., 12, 2021
|
|
