grant
Inhibitors of Tyrosine Kinase-Dependent Signaling as Anti-Cancer Agents
Organization DIVISION OF BASIC SCIENCES - NCILocation UNITED STATES
NIHUS FederalResearch GrantFY20255-IsothiocyanatofluoresceinActive Follow-upAffinityAlkynesAnti-Cancer AgentsAntibiotic AgentsAntibiotic DrugsAntibioticsAntineoplastic AgentsAntineoplastic DrugsAntineoplasticsAssayAzidesAzolesBindingBioassayBiologicalBiological AssayC-terminalCancer DrugCancersCell Communication and SignalingCell CycleCell Division CycleCell SignalingCephalosporinsComplexComputer softwareCopperCu elementDNADNA Nicking-Closing ProteinDNA Relaxing EnzymeDNA Relaxing ProteinDNA Repair EnzymesDNA Topoisomerase IDNA TopoisomerasesDNA Type 1 TopoisomeraseDNA Untwisting EnzymeDNA Untwisting ProteinDeoxyribonucleic AcidDigitDigit structureDockingE3 LigaseE3 Ubiquitin LigaseELISAEnzyme-Linked Immunosorbent AssayFITCFamilyFluoresceinFluorescein-5-isothiocyanateFluorescenceFluorescence PolarizationFluorescent ProbesFoundationsGelH-bondHistidineHydrogen BondingIntracellular Communication and SignalingKinasesL-SerineL-ThreonineLabelLeadLecithinase DLengthLibrariesLigand BindingLigandsMalignant NeoplasmsMalignant TumorMeasuresMiscellaneous AntibioticModelingModificationMolecular InteractionMolecular TargetN-terminalNH2-terminalNeoplastic Disease Chemotherapeutic AgentsNitrogenPLK GenePLK1PLK1 genePTK InhibitorsParentsPb elementPenicillin-Binding ProteinsPeptidesPhosphatesPhosphatidylcholine PhosphohydrolasePhospholipase DPhosphorylserinePhosphoserinePhosphothreoninePhosphotransferase GenePhosphotransferasesPolo-Box DomainPolo-Like KinaseProtacProtein Tyrosine Kinase InhibitorsProteinsProteolysis targeting chimericReactionReportingSTPK13SeriesSerineSerine PhosphateSerine/Threonine Protein Kinase 13Seryl PhosphateSideSignal TransductionSignal Transduction SystemsSignalingSoftwareStructureSurface Plasmon ResonanceTK InhibitorsThreonineThreonine PhosphateTopoisomeraseTopoisomerase ITopoisomerase InhibitorsTransphosphorylasesTumor-Specific Treatment AgentsType I DNA TopoisomerasesTyr-DNA phosphodiesteraseTyrosineTyrosine Kinase InhibitorUbiquitin Protein LigaseUbiquitin-Protein Ligase ComplexesUbiquitin-Protein Ligase E3Workactive followupanti-canceranti-cancer drugbeta lactam antibioticbeta-Lactamsbiologicbiological signal transductioncovalent bondcycloadditiondesigndesigningenzyme linked immunoassayflexibilityflexiblefollow upfollow-upfollowed upfollowupheavy metal Pbheavy metal leadimprovedinhibitorinorganic phosphatelipophosphodiesterase IImalignancymemberneoplasm/cancernew drug treatmentsnew drugsnew pharmacological therapeuticnew therapeuticsnew therapynext generation therapeuticsnicking closing enzymenovel drug treatmentsnovel drugsnovel pharmaco-therapeuticnovel pharmacological therapeuticnovel therapeuticsnovel therapyoverexpressoverexpressionparentpharmacophorephosphatidylcholine phosphatidohydrolasephosphodiesterpolo-like kinase 1protein protein interactionproteolysis targeting chimaeraproteolysis targeting chimerarelaxing enzymesmall moleculespatial and temporalspatial temporalspatiotemporalswivelasetumortyrosyl-DNA phosphodiesteraseubiquitin-protein ligaseuntwisting enzymeuptakevirtualwortmanninβ lactam antibioticβ-Lactams
Description preview
Objective One: Plk1 is composed of an N-terminal catalytic kinase domain (KD) and a C-terminal polo-box domain (PBD). The PBD recognizes phosphoserine (pS) and phosphothreonine (pT)-containing sequences, facilitating protein-protein interactions (PPIs). The KD is tethered to the PBD by means of a flexible interdomain linker. Intramolecular…
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