5LXC
 
 | | Crystal structure of DYRK2 in complex with EHT 5372 (Compound 1) | | Descriptor: | 1,2-ETHANEDIOL, Dual specificity tyrosine-phosphorylation-regulated kinase 2, methyl 9-[(2,4-dichlorophenyl)amino]-[1,3]thiazolo[5,4-f]quinazoline-2-carboximidate | | Authors: | Chaikuad, A, von Delft, F, Arrowsmith, C.H, Edwards, A, Bountra, C, Besson, T, Knapp, S, Structural Genomics Consortium (SGC) | | Deposit date: | 2016-09-20 | | Release date: | 2016-10-26 | | Last modified: | 2017-01-11 | | Method: | X-RAY DIFFRACTION (2.15 Å) | | Cite: | An Unusual Binding Model of the Methyl 9-Anilinothiazolo[5,4-f] quinazoline-2-carbimidates (EHT 1610 and EHT 5372) Confers High Selectivity for Dual-Specificity Tyrosine Phosphorylation-Regulated Kinases.
J. Med. Chem., 59, 2016
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7DH9
 | | The co-crystal structure of DYRK2 with a small molecule inhibitor 7 | | Descriptor: | Dual specificity tyrosine-phosphorylation-regulated kinase 2, [2,7-dimethoxy-9-(piperidin-4-ylmethylsulfanyl)acridin-4-yl]methanol | | Authors: | Wei, T, Xiao, J. | | Deposit date: | 2020-11-13 | | Release date: | 2021-11-17 | | Last modified: | 2023-11-29 | | Method: | X-RAY DIFFRACTION (2.194 Å) | | Cite: | Selective inhibition reveals the regulatory function of DYRK2 in protein synthesis and calcium entry.
Elife, 11, 2022
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6HDR
 | | Human DYRK2 bound to Curcumin | | Descriptor: | DITHIANE DIOL, Dual specificity tyrosine-phosphorylation-regulated kinase 2, PHOSPHATE ION, ... | | Authors: | Elkins, J.M, Soundararajan, M, Vollmar, M, Krojer, T, Bountra, C, Edwards, A.M, Arrowsmith, C, Knapp, S. | | Deposit date: | 2018-08-18 | | Release date: | 2019-08-28 | | Last modified: | 2024-01-17 | | Method: | X-RAY DIFFRACTION (2.2 Å) | | Cite: | DYRK2 bound to Curcumin
To Be Published
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3KVW
 | | Crystal Structure of dual-specificity tyrosine phosphorylation regulated kinase 2 (DYRK2) in complex with an indirubin ligand | | Descriptor: | (2Z,3E)-7'-bromo-3-(hydroxyimino)-2'-oxo-1,1',2',3-tetrahydro-2,3'-biindole-5-carboxylic acid, CHLORIDE ION, Dual specificity tyrosine-phosphorylation-regulated kinase 2 | | Authors: | Filippakopoulos, P, Myrianthopoulos, V, Kritsanida, M, Magiatis, P, Skaltsounis, A.L, Soundararajan, M, Krojer, T, Gileadi, O, Hapka, E, Fedorov, O, Berridge, G, Wang, J, Shrestha, L, Vollmar, M, von Delft, F, Arrowsmith, C.H, Edwards, A, Weigelt, J, Bountra, C, Mikros, E, Knapp, S, Structural Genomics Consortium (SGC) | | Deposit date: | 2009-11-30 | | Release date: | 2010-01-05 | | Last modified: | 2023-11-22 | | Method: | X-RAY DIFFRACTION (2.28 Å) | | Cite: | Crystal Structure of dual-specificity tyrosine phosphorylation regulated kinase 2 (DYRK2) in complex with an indirubin ligand
To be Published
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6HDP
 | | Human DYRK2 bound to Scorzodihydrostilbene A | | Descriptor: | Dual specificity tyrosine-phosphorylation-regulated kinase 2, SODIUM ION, Scorzodihydrostilbene A | | Authors: | Elkins, J.M, Soundararajan, M, Proksch, P, Meijer, L, Vollmar, M, Krojer, T, Bountra, C, Edwards, A.M, Arrowsmith, C, Knapp, S. | | Deposit date: | 2018-08-18 | | Release date: | 2019-08-28 | | Last modified: | 2024-01-17 | | Method: | X-RAY DIFFRACTION (2.3 Å) | | Cite: | DYRK2 bound to Scorzodihydrostilbene A
To Be Published
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7DH3
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7DHK
 | | The co-crystal structure of DYRK2 with a small molecule inhibitor 13 | | Descriptor: | 2-methoxy-7-phenylmethoxy-9-(piperidin-4-ylmethylsulfanyl)acridine, Dual specificity tyrosine-phosphorylation-regulated kinase 2 | | Authors: | Wei, T, Xiao, J. | | Deposit date: | 2020-11-16 | | Release date: | 2021-11-17 | | Last modified: | 2023-11-29 | | Method: | X-RAY DIFFRACTION (2.341 Å) | | Cite: | Selective inhibition reveals the regulatory function of DYRK2 in protein synthesis and calcium entry.
Elife, 11, 2022
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6K0J
 | | The co-crystal structure of DYRK2 with a small molecule inhibitor | | Descriptor: | 3-(2,7-dimethoxyacridin-9-yl)sulfanylpropan-1-amine, Dual specificity tyrosine-phosphorylation-regulated kinase 2 | | Authors: | Tiantian, W, Xiao, J. | | Deposit date: | 2019-05-06 | | Release date: | 2019-11-20 | | Last modified: | 2019-12-18 | | Method: | X-RAY DIFFRACTION (2.352 Å) | | Cite: | Inhibition of dual-specificity tyrosine phosphorylation-regulated kinase 2 perturbs 26S proteasome-addicted neoplastic progression.
Proc.Natl.Acad.Sci.USA, 116, 2019
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3K2L
 | | Crystal Structure of dual-specificity tyrosine phosphorylation regulated kinase 2 (DYRK2) | | Descriptor: | CHLORIDE ION, Dual specificity tyrosine-phosphorylation-regulated kinase 2, SODIUM ION, ... | | Authors: | Filippakopoulos, P, Myrianthopoulos, V, Soundararajan, M, Krojer, T, Hapka, E, Fedorov, O, Berridge, G, Wang, J, Shrestha, L, Pike, A.C.W, Ugochukwu, E, von Delft, F, Arrowsmith, C.H, Edwards, A, Weigelt, J, Bountra, C, Mikros, E, Knapp, S, Structural Genomics Consortium (SGC) | | Deposit date: | 2009-09-30 | | Release date: | 2009-10-13 | | Last modified: | 2023-11-22 | | Method: | X-RAY DIFFRACTION (2.36 Å) | | Cite: | Structures of Down Syndrome Kinases, DYRKs, Reveal Mechanisms of Kinase Activation and Substrate Recognition.
Structure, 21, 2013
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7DHN
 | | The co-crystal structure of DYRK2 with a small molecule inhibitor 20 | | Descriptor: | 7-methoxy-2-methylsulfanyl-9-(piperidin-4-ylmethylsulfanyl)-[1,3]thiazolo[5,4-b]quinoline, Dual specificity tyrosine-phosphorylation-regulated kinase 2 | | Authors: | Wei, T, Xiao, J. | | Deposit date: | 2020-11-16 | | Release date: | 2021-11-17 | | Last modified: | 2023-11-29 | | Method: | X-RAY DIFFRACTION (2.38 Å) | | Cite: | Selective inhibition reveals the regulatory function of DYRK2 in protein synthesis and calcium entry.
Elife, 11, 2022
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7DHH
 | | The co-crystal structure of DYRK2 with a small molecule inhibitor 19 | | Descriptor: | Dual specificity tyrosine-phosphorylation-regulated kinase 2, [9-(azetidin-3-ylmethylsulfanyl)-2,7-dimethoxy-acridin-4-yl]methanol | | Authors: | Wei, T, Xiao, J. | | Deposit date: | 2020-11-14 | | Release date: | 2021-11-17 | | Last modified: | 2023-11-29 | | Method: | X-RAY DIFFRACTION (2.486 Å) | | Cite: | Selective inhibition reveals the regulatory function of DYRK2 in protein synthesis and calcium entry.
Elife, 11, 2022
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5ZTN
 | | The crystal structure of human DYRK2 in complex with Curcumin | | Descriptor: | (1Z,4Z,6E)-5-hydroxy-1,7-bis(4-hydroxy-3-methoxyphenyl)hepta-1,4,6-trien-3-one, Dual specificity tyrosine-phosphorylation-regulated kinase 2 | | Authors: | Ji, C.G, Xiao, J.Y. | | Deposit date: | 2018-05-04 | | Release date: | 2018-07-18 | | Last modified: | 2023-11-22 | | Method: | X-RAY DIFFRACTION (2.496 Å) | | Cite: | Ancient drug curcumin impedes 26S proteasome activity by direct inhibition of dual-specificity tyrosine-regulated kinase 2.
Proc. Natl. Acad. Sci. U.S.A., 115, 2018
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7DJO
 | | The co-crystal structure of DYRK2 with a small molecule inhibitor 17 | | Descriptor: | Dual specificity tyrosine-phosphorylation-regulated kinase 2, [2,7-dimethoxy-9-[[(3S)-pyrrolidin-3-yl]methylsulfanyl]acridin-4-yl]methanol | | Authors: | Wei, T, Xiao, J. | | Deposit date: | 2020-11-20 | | Release date: | 2021-11-24 | | Last modified: | 2023-11-29 | | Method: | X-RAY DIFFRACTION (2.499 Å) | | Cite: | Selective inhibition reveals the regulatory function of DYRK2 in protein synthesis and calcium entry.
Elife, 11, 2022
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7EJV
 | | The co-crystal structure of DYRK2 with YK-2-69 | | Descriptor: | Dual specificity tyrosine-phosphorylation-regulated kinase 2, [6-[[4-[2-(dimethylamino)-1,3-benzothiazol-6-yl]-5-fluoranyl-pyrimidin-2-yl]amino]pyridin-3-yl]-(4-ethylpiperazin-1-yl)methanone | | Authors: | Li, Z, Xiao, Y, Yuan, K, Kuang, W, Xiuquan, Y, Yang, P. | | Deposit date: | 2021-04-02 | | Release date: | 2022-04-06 | | Last modified: | 2023-11-29 | | Method: | X-RAY DIFFRACTION (2.5 Å) | | Cite: | Targeting dual-specificity tyrosine phosphorylation-regulated kinase 2 with a highly selective inhibitor for the treatment of prostate cancer.
Nat Commun, 13, 2022
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4AZF
 | | Human DYRK2 in complex with Leucettine L41 | | Descriptor: | 1,2-ETHANEDIOL, 5-(1,3-benzodioxol-5-ylmethyl)-2-(phenylamino)-4H-imidazol-4-one, DYRK2 DUAL-SPECIFICITY TYROSINE-PHOSPHORYLATION REGULATED KINASE 2, ... | | Authors: | Elkins, J.M, Soundararajan, M, Muniz, J.R.C, Tahtouh, T, Burgy, G, Durieu, E, Lozach, O, Cochet, C, Schmid, R.S, Lo, D.C, Delhommel, F, Carreaux, F, Bazureau, J.P, Meijer, L, Edwards, A, Bountra, C, Knapp, S. | | Deposit date: | 2012-06-25 | | Release date: | 2012-09-05 | | Last modified: | 2023-12-20 | | Method: | X-RAY DIFFRACTION (2.55 Å) | | Cite: | Selectivity, Co-Crystal Structures and Neuroprotective Properties of Leucettines, a Family of Protein Kinase Inhibitors Derived from the Marine Sponge Alkaloid Leucettamine B.
J.Med.Chem., 55, 2012
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5LXD
 | | Crystal structure of DYRK2 in complex with EHT 1610 (compound 2) | | Descriptor: | 1,2-ETHANEDIOL, Dual specificity tyrosine-phosphorylation-regulated kinase 2, methyl 9-[(2-fluoranyl-4-methoxy-phenyl)amino]-[1,3]thiazolo[5,4-f]quinazoline-2-carboximidate | | Authors: | Chaikuad, A, von Delft, F, Arrowsmith, C.H, Edwards, A, Bountra, C, Besson, T, Knapp, S, Structural Genomics Consortium (SGC) | | Deposit date: | 2016-09-20 | | Release date: | 2016-10-26 | | Last modified: | 2017-01-11 | | Method: | X-RAY DIFFRACTION (2.58 Å) | | Cite: | An Unusual Binding Model of the Methyl 9-Anilinothiazolo[5,4-f] quinazoline-2-carbimidates (EHT 1610 and EHT 5372) Confers High Selectivity for Dual-Specificity Tyrosine Phosphorylation-Regulated Kinases.
J. Med. Chem., 59, 2016
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7DG4
 | | The co-crystal structure of DYRK2 with a small molecule inhibitor 6 | | Descriptor: | 2,7-dimethoxy-9-(piperidin-4-ylmethylsulfanyl)acridine, Dual specificity tyrosine-phosphorylation-regulated kinase 2 | | Authors: | Wei, T, Xiao, J. | | Deposit date: | 2020-11-10 | | Release date: | 2021-11-10 | | Last modified: | 2023-11-29 | | Method: | X-RAY DIFFRACTION (2.58 Å) | | Cite: | Selective inhibition reveals the regulatory function of DYRK2 in protein synthesis and calcium entry.
Elife, 11, 2022
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7DHC
 | | The co-crystal structure of DYRK2 with a small molecule inhibitor 10 | | Descriptor: | 4-[bis(fluoranyl)methyl]-2,7-dimethoxy-9-(piperidin-4-ylmethylsulfanyl)acridine, Dual specificity tyrosine-phosphorylation-regulated kinase 2 | | Authors: | Wei, T, Xiao, J. | | Deposit date: | 2020-11-13 | | Release date: | 2021-11-17 | | Last modified: | 2023-11-29 | | Method: | X-RAY DIFFRACTION (2.592 Å) | | Cite: | Selective inhibition reveals the regulatory function of DYRK2 in protein synthesis and calcium entry.
Elife, 11, 2022
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7AKF
 | | Structure of DYRK2 in complex with compound 50 | | Descriptor: | 4-(2,3-dimethyl-1-benzofuran-5-yl)pyridine-2,6-diamine, CHLORIDE ION, Dual specificity tyrosine-phosphorylation-regulated kinase 2 | | Authors: | Dokurno, P, Surgenor, A.E, Kotschy, A. | | Deposit date: | 2020-09-30 | | Release date: | 2021-05-26 | | Last modified: | 2024-01-31 | | Method: | X-RAY DIFFRACTION (2.6 Å) | | Cite: | Structure-Guided Discovery of Potent and Selective DYRK1A Inhibitors.
J.Med.Chem., 64, 2021
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7DL6
 | | The co-crystal structure of DYRK2 with a small molecule inhibitor 18 | | Descriptor: | Dual specificity tyrosine-phosphorylation-regulated kinase 2, [2,7-dimethoxy-9-[[(3R)-pyrrolidin-3-yl]methylsulfanyl]acridin-4-yl]methanol | | Authors: | Wei, T, Xiao, J. | | Deposit date: | 2020-11-26 | | Release date: | 2021-12-01 | | Last modified: | 2023-11-29 | | Method: | X-RAY DIFFRACTION (2.648 Å) | | Cite: | Selective inhibition reveals the regulatory function of DYRK2 in protein synthesis and calcium entry.
Elife, 11, 2022
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7DHV
 | | The co-crystal structure of DYRK2 with a small molecule inhibitor 8 | | Descriptor: | 2,7-dimethoxy-9-(piperidin-4-ylmethylsulfanyl)acridine-4-carboxylic acid, Dual specificity tyrosine-phosphorylation-regulated kinase 2 | | Authors: | Wei, T, Xiao, J. | | Deposit date: | 2020-11-17 | | Release date: | 2021-11-17 | | Last modified: | 2023-11-29 | | Method: | X-RAY DIFFRACTION (2.679 Å) | | Cite: | Selective inhibition reveals the regulatory function of DYRK2 in protein synthesis and calcium entry.
Elife, 11, 2022
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8HLT
 | | The co-crystal structure of DYRK2 with YK-2-99B | | Descriptor: | (6-{[(4P)-4-(1,3-benzothiazol-5-yl)-5-fluoropyrimidin-2-yl]amino}pyridin-3-yl)(piperazin-1-yl)methanone, Dual specificity tyrosine-phosphorylation-regulated kinase 2 | | Authors: | Shen, H.T, Xiao, Y.B, Yuan, K, Yang, P, Li, Q.N. | | Deposit date: | 2022-12-01 | | Release date: | 2023-12-13 | | Method: | X-RAY DIFFRACTION (2.8 Å) | | Cite: | Discovery of Potent DYRK2 Inhibitors with High Selectivity, Great Solubility, and Excellent Safety Properties for the Treatment of Prostate Cancer.
J.Med.Chem., 66, 2023
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7AKH
 | | Structure of DYRK2 in complex with compound 58 | | Descriptor: | 4-[3-[(2~{S})-2-(6-bromanylpyridin-2-yl)oxypropyl]-2-methyl-imidazo[4,5-b]pyridin-5-yl]pyridine-2,6-diamine, CHLORIDE ION, Dual specificity tyrosine-phosphorylation-regulated kinase 2 | | Authors: | Dokurno, P, Surgenor, A.E, Kotschy, A. | | Deposit date: | 2020-10-01 | | Release date: | 2021-05-26 | | Last modified: | 2024-01-31 | | Method: | X-RAY DIFFRACTION (2.85 Å) | | Cite: | Structure-Guided Discovery of Potent and Selective DYRK1A Inhibitors.
J.Med.Chem., 64, 2021
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7DHO
 | | The co-crystal structure of DYRK2 with a small molecule inhibitor 14 | | Descriptor: | 2-methoxy-9-(piperidin-4-ylmethylsulfanyl)-7-propan-2-yloxy-acridine, Dual specificity tyrosine-phosphorylation-regulated kinase 2 | | Authors: | Wei, T, Xiao, J. | | Deposit date: | 2020-11-16 | | Release date: | 2021-11-17 | | Last modified: | 2023-11-29 | | Method: | X-RAY DIFFRACTION (3.29 Å) | | Cite: | Selective inhibition reveals the regulatory function of DYRK2 in protein synthesis and calcium entry.
Elife, 11, 2022
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