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; PubMed: 32292564; DOI: 10.1021/acsmedchemlett.0c00015

Experimental method

X-RAY DIFFRACTION (2.303 Å)