5VO2

DLK in complex with inhibitor 5-(1-isopropyl-5-(1-(oxetan-3-yl)piperidin-4-yl)-1H-pyrazol-3-yl)-3-(trifluoromethyl)pyridin-2-amine (compound 7)

Summary for 5VO2

• Entry DOI: 10.2210/pdb5vo2/pdb
• Related: 5VO1
• Descriptor: Mitogen-activated protein kinase kinase kinase 12, 5-{5-[1-(oxetan-3-yl)piperidin-4-yl]-1-(propan-2-yl)-1H-pyrazol-3-yl}-3-(trifluoromethyl)pyridin-2-amine (3 entities in total)
• Functional Keywords: kinase, transferase-transferase inhibitor complex, transferase/transferase inhibitor
• Biological source: Homo sapiens (Human)
• Cellular location: Cytoplasm : Q12852
• Total number of polymer chains: 1
• Total formula weight: 34427.48

Authors

HARRIS, S.F.,YIN, J. (deposition date: 2017-05-01, release date: 2017-10-04, Last modification date: 2023-10-04)

• Primary citation: Patel, S.,Meilandt, W.J.,Erickson, R.I.,Chen, J.,Deshmukh, G.,Estrada, A.A.,Fuji, R.N.,Gibbons, P.,Gustafson, A.,Harris, S.F.,Imperio, J.,Liu, W.,Liu, X.,Liu, Y.,Lyssikatos, J.P.,Ma, C.,Yin, J.,Lewcock, J.W.,Siu, M.; Selective Inhibitors of Dual Leucine Zipper Kinase (DLK, MAP3K12) with Activity in a Model of Alzheimer's Disease.; J. Med. Chem., 60:8083-8102, 2017; PubMed: 28929759; DOI: 10.1021/acs.jmedchem.7b00843

Experimental method

X-RAY DIFFRACTION (2.96 Å)