Search results for "Polo-like kinase"

showing 3 items of 3 documents

MCC1019, a selective inhibitor of the Polo-box domain of Polo-like kinase 1 as novel, potent anticancer candidate

2019

Polo-like kinase (PLK1) has been identified as a potential target for cancer treatment. Although a number of small molecules have been investigated as PLK1 inhibitors, many of which showed limited selectivity. PLK1 harbors a regulatory domain, the Polo box domain (PBD), which has a key regulatory function for kinase activity and substrate recognition. We report on 3-bromomethyl-benzofuran-2-carboxylic acid ethyl ester (designated: MCC1019) as selective PLK1 inhibitor targeting PLK1 PBD. Cytotoxicity and fluorescence polarization-based screening were applied to a library of 1162 drug-like compounds to identify potential inhibitors of PLK1 PBD. The activity of compound MC1019 against the PLK1…

PBD Polo box domainMTD maximal tolerance doseCDC25 cell division cycle 25HIF-1α hypoxia-inducible factor 1 αMST microscale thermophoresisIC50 50% inhibition concentrationMFP M phase promoting factorPARP-1 poly(ADP-ribose) polymerase-10302 clinical medicineFOXO forkhead box ONec-1 necrostatin 1CDC2 cell division cycle protein 2 homologGeneral Pharmacology Toxicology and PharmaceuticsMitotic catastropheCDK cyclin-dependent kinase0303 health sciencesChemistryPolo-like kinaseMono-targeted therapyCell cycleBUBR1 budding uninhibited by benzimidazole-related 1Polo box domain030220 oncology & carcinogenesisPLK1 Polo-like kinaseNecroptosisSpindle damagePLK1IHC immunohistochemistryOriginal articleNecroptosisCell cyclePLK1APC/C anaphase-promoting complex/cyclosomePLK3ABC avidin-biotin complexPI propidium iodide03 medical and health sciencesFBS fetal bovine serumPDB Protein Data BankKd the dissociation constantKinase activity030304 developmental biologyAkt/PKB signaling pathwayCell growthlcsh:RM1-950LC3 light chain 3lcsh:Therapeutics. PharmacologyCancer researchDAPKs death-associated protein kinase3-MA 3-methyladenineDAPI 4′6-diamidino-2-phenylindoleSAC spindle assembly checkpointActa Pharmaceutica Sinica B
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Polo-like kinase 1 as a target for human cytomegalovirus pp65 lower matrix protein

1999

ABSTRACT Human cytomegalovirus (HCMV) pp65 protein is the major constituent of viral dense bodies but is dispensable for viral growth in vitro. pp65 copurifies with a S/T kinase activity and has been implicated in phosphorylation of HCMV IE1 immediate-early protein and its escape from major histocompatibility complex 1 presentation. Furthermore, the presence of pp65 correlates with a virion-associated kinase activity. To clarify the role of pp65, yeast two-hybrid system (THS) screening was performed to identify pp65 cellular partners. A total of 18 out of 48 yeast clones harboring cDNAs for putative pp65 binding proteins encoded the Polo-like kinase 1 (Plk1) C-terminal domain. Plk1 behaved …

Human cytomegalovirusvirusesRecombinant Fusion ProteinsImmunologyCytomegalovirusCell Cycle ProteinsPolo-like kinaseBiologyProtein Serine-Threonine KinasesMicrobiologyDNA-binding proteinPLK1Cell LineViral Matrix ProteinsVirologyProto-Oncogene ProteinsmedicineAnimalsHumansKinase activityViral matrix proteinKinasevirus diseasesmedicine.diseasePhosphoproteinsMolecular biologyVirus-Cell Interactionssurgical procedures operativeInsect ScienceCOS CellsPhosphorylationProtein KinasesHeLa Cells
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A selective inhibitor of the Polo-box domain of Polo-like kinase 1 identified by virtual screening

2018

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0301 basic medicineLK Polo-like kinasePolo-like kinaseCell cycleIC50 50% inhibition concentrationVirtual drug screeningPLK103 medical and health sciences0302 clinical medicineNeoplasmsTargeted chemotherapylcsh:Science (General)MitosisComputingMethodologies_COMPUTERGRAPHICSCDK cyclin-dependent kinasePBD Polo-box domainPyRxNatural productslcsh:R5-920MultidisciplinaryMicroscale thermophoresisKinaseChemistryCell cycleCell biology030104 developmental biology030220 oncology & carcinogenesisCancer cellOriginal ArticleCAMKK2 calcium/calmodulin-dependent protein kinase kinase 2PC Polo-box caplcsh:Medicine (General)Multipolar spindleslcsh:Q1-390Journal of Advanced Research
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