6VHG
Crystal structure of phosphorylated RET tyrosine kinase domain complexed with a pyrazolo[1,5-a]pyrimidine inhibitor
Summary for 6VHG
Entry DOI | 10.2210/pdb6vhg/pdb |
Descriptor | Proto-oncogene tyrosine-protein kinase receptor Ret, 3-(3,4-dimethoxyphenyl)-N~5~-(1-methylpiperidin-4-yl)-6-phenylpyrazolo[1,5-a]pyrimidine-5,7-diamine, SULFATE ION, ... (6 entities in total) |
Functional Keywords | inhibitor, complex, tyrosine kinase, catalytic domain, transferase-transferase inhibitor complex, transferase/transferase inhibitor |
Biological source | Homo sapiens (Human) |
Total number of polymer chains | 1 |
Total formula weight | 36501.53 |
Authors | Lee, C.C.,Spraggon, G. (deposition date: 2020-01-09, release date: 2020-02-26, Last modification date: 2023-11-15) |
Primary citation | Mathison, C.J.N.,Chianelli, D.,Rucker, P.V.,Nelson, J.,Roland, J.,Huang, Z.,Yang, Y.,Jiang, J.,Xie, Y.F.,Epple, R.,Bursulaya, B.,Lee, C.,Gao, M.Y.,Shaffer, J.,Briones, S.,Sarkisova, Y.,Galkin, A.,Li, L.,Li, N.,Li, C.,Hua, S.,Kasibhatla, S.,Kinyamu-Akunda, J.,Kikkawa, R.,Molteni, V.,Tellew, J.E. Efficacy and Tolerability of Pyrazolo[1,5-a]pyrimidine RET Kinase Inhibitors for the Treatment of Lung Adenocarcinoma. Acs Med.Chem.Lett., 11:558-565, 2020 Cited by PubMed: 32292564DOI: 10.1021/acsmedchemlett.0c00015 PDB entries with the same primary citation |
Experimental method | X-RAY DIFFRACTION (2.303 Å) |
Structure validation
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