3FC2

PLK1 in complex with BI6727

Summary for 3FC2

• Entry DOI: 10.2210/pdb3fc2/pdb
• Descriptor: Serine/threonine-protein kinase PLK1, N-{trans-4-[4-(cyclopropylmethyl)piperazin-1-yl]cyclohexyl}-4-{[(7R)-7-ethyl-5-methyl-8-(1-methylethyl)-6-oxo-5,6,7,8-tetrahydropteridin-2-yl]amino}-3-methoxybenzamide, 1,2-ETHANEDIOL, ... (8 entities in total)
• Functional Keywords: protein kinase, atp-binding, cell cycle, cell division, kinase, mitosis, nucleotide-binding, nucleus, phosphoprotein, serine/threonine-protein kinase, transferase
• Biological source: Homo sapiens (Human)
• Cellular location: Nucleus: P53350
• Total number of polymer chains: 1
• Total formula weight: 38883.58

Authors

Bader, G. (deposition date: 2008-11-21, release date: 2009-05-12, Last modification date: 2023-12-27)

Primary citation

Rudolph, D.,Steegmaier, M.,Hoffmann, M.,Grauert, M.,Baum, A.,Quant, J.,Haslinger, C.,Garin-Chesa, P.,Adolf, G.R.
BI 6727, A Polo-like Kinase Inhibitor with Improved Pharmacokinetic Profile and Broad Antitumor Activity.
Clin.Cancer Res., 15:3094-3102, 2009

PubMed Abstract: Antimitotic chemotherapy remains a cornerstone of multimodality treatment for locally advanced and metastatic cancers. To identify novel mitosis-specific agents with higher selectivity than approved tubulin-binding agents (taxanes, Vinca alkaloids), we have generated inhibitors of Polo-like kinase 1, a target that functions predominantly in mitosis.

PubMed: 19383823
DOI: 10.1158/1078-0432.CCR-08-2445

Experimental method

X-RAY DIFFRACTION (2.45 Å)