4I5M

Selective & Brain-Permeable Polo-like Kinase-2 (Plk-2) Inhibitors that Reduce -Synuclein Phosphorylation in Rat Brain

Summary for 4I5M

• Entry DOI: 10.2210/pdb4i5m/pdb
• Descriptor: Serine/threonine-protein kinase PLK2, 4-{[(7R)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,7,8-tetrahydropteridin-2-yl]amino}-3-methoxy-N-(1-methylpiperidin-4-yl)benzamide (3 entities in total)
• Functional Keywords: polo-like kinase-2 (plk-2), synuclein, parkinson's disease, kinase inhibitor, transferase-transferase inhibitor complex, transferase/transferase inhibitor
• Biological source: Homo sapiens (human)
• Cellular location: Cytoplasm, cytoskeleton, microtubule organizing center, centrosome, centriole : Q9NYY3
• Total number of polymer chains: 1
• Total formula weight: 36353.84

Authors

Aubele, D.L.,Hom, R.K.,Adler, M.,Galemmo Jr., R.A.,Bowers, S.,Truong, A.P.,Pan, H.,Beroza, P.,Neitz, R.J.,Yao, N.,Lin, M.,Tonn, G.,Zhang, H.,Bova, M.P.,Ren, Z.,Tam, D.,Ruslim, L.,Baker, J.,Diep, L.,Fitzgerald, K.,Hoffman, J.,Motter, R.,Fauss, D.,Tanaka, P.,Dappen, M.,Jagodzinski, J.,Chan, W.,Konradi, A.W.,Latimer, L.,Zhu, Y.L.,Artis, D.R.,Sham, H.L.,Anderson, J.P.,Bergeron, M. (deposition date: 2012-11-28, release date: 2013-12-25, Last modification date: 2024-02-28)

• Primary citation: Aubele, D.L.,Hom, R.K.,Adler, M.,Galemmo, R.A.,Bowers, S.,Truong, A.P.,Pan, H.,Beroza, P.,Neitz, R.J.,Yao, N.,Lin, M.,Tonn, G.,Zhang, H.,Bova, M.P.,Ren, Z.,Tam, D.,Ruslim, L.,Baker, J.,Diep, L.,Fitzgerald, K.,Hoffman, J.,Motter, R.,Fauss, D.,Tanaka, P.,Dappen, M.,Jagodzinski, J.,Chan, W.,Konradi, A.W.,Latimer, L.,Zhu, Y.L.,Sham, H.L.,Anderson, J.P.,Bergeron, M.,Artis, D.R.; Selective and brain-permeable polo-like kinase-2 (Plk-2) inhibitors that reduce alpha-synuclein phosphorylation in rat brain.; Chemmedchem, 8:1295-1313, 2013; PubMed: 23794260; DOI: 10.1002/cmdc.201300166

Experimental method

X-RAY DIFFRACTION (1.801 Å)