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4MQ2

The crystal structure of DYRK1a with a bound pyrido[2,3-d]pyrimidine inhibitor

Summary for 4MQ2
Entry DOI10.2210/pdb4mq2/pdb
Related2vx3 4MQ1
DescriptorDual specificity tyrosine-phosphorylation-regulated kinase 1A, methyl 4-chloro-3-{[(2-methoxy-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidin-6-yl)carbonyl]amino}benzoate, PENTAETHYLENE GLYCOL, ... (5 entities in total)
Functional Keywordsdyrk1a, dyrk1b, kinase, transferase-transferase inhibitor complex, transferase/transferase inhibitor
Biological sourceHomo sapiens (human)
Cellular locationNucleus speckle: Q13627
Total number of polymer chains4
Total formula weight171791.17
Authors
Lukacs, C.M.,Janson, C.A.,Garvie, C.,Liang, L. (deposition date: 2013-09-15, release date: 2013-12-11, Last modification date: 2023-12-06)
Primary citationAnderson, K.,Chen, Y.,Chen, Z.,Dominique, R.,Glenn, K.,He, Y.,Janson, C.,Luk, K.C.,Lukacs, C.,Polonskaia, A.,Qiao, Q.,Railkar, A.,Rossman, P.,Sun, H.,Xiang, Q.,Vilenchik, M.,Wovkulich, P.,Zhang, X.
Pyrido[2,3-d]pyrimidines: Discovery and preliminary SAR of a novel series of DYRK1B and DYRK1A inhibitors.
Bioorg.Med.Chem.Lett., 23:6610-6615, 2013
Cited by
PubMed: 24239188
DOI: 10.1016/j.bmcl.2013.10.055
PDB entries with the same primary citation
Experimental method
X-RAY DIFFRACTION (2.8 Å)
Structure validation

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