5TA8
Crystal structure of PLK1 in complex with a novel 5,6-dihydroimidazolo[1,5-f]pteridine inhibitor
Summary for 5TA8
Entry DOI | 10.2210/pdb5ta8/pdb |
Related | 5TA6 |
Descriptor | Serine/threonine-protein kinase PLK1, ZINC ION, 4-[(9-cyclopentyl-7,7-difluoro-5-methyl-6-oxo-6,7,8,9-tetrahydro-5H-pyrimido[4,5-b][1,4]diazepin-2-yl)amino]-3-methoxy-N-(1-methylpiperidin-4-yl)benzamide, ... (4 entities in total) |
Functional Keywords | plk1 inhibitor, kinase, structure-based drug design, antitumor activity, transferase-transferase inhibitor complex, transferase/transferase inhibitor |
Biological source | Homo sapiens (Human) |
Cellular location | Nucleus: P53350 |
Total number of polymer chains | 1 |
Total formula weight | 41191.92 |
Authors | Skene, R.J.,Hosfield, D.J. (deposition date: 2016-09-09, release date: 2017-02-22, Last modification date: 2024-03-06) |
Primary citation | Kiryanov, A.,Natala, S.,Jones, B.,McBride, C.,Feher, V.,Lam, B.,Liu, Y.,Honda, K.,Uchiyama, N.,Kawamoto, T.,Hikichi, Y.,Zhang, L.,Hosfield, D.,Skene, R.,Zou, H.,Stafford, J.,Cao, X.,Ichikawa, T. Structure-based design and SAR development of 5,6-dihydroimidazolo[1,5-f]pteridine derivatives as novel Polo-like kinase-1 inhibitors. Bioorg. Med. Chem. Lett., 27:1311-1315, 2017 Cited by PubMed: 28169164DOI: 10.1016/j.bmcl.2016.10.009 PDB entries with the same primary citation |
Experimental method | X-RAY DIFFRACTION (2.6 Å) |
Structure validation
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