grant
Optimizing PepTAC structure and amphiphilicity for enhanced target protein degradation
NIHUS FederalResearch GrantFY202520S Catalytic Proteasome20S Core Proteasome20S Proteasome20S Proteosome26 S proteasome complex26S ATP-Dependent Protease26S ATP-Dependent Proteasome26S Proteasome Complex26S Proteosome26S protease26S proteasomeAPF-1ATP-Dependent Proteolysis Factor 1AddressAreaAssayAttentionBindingBioassayBiodistributionBiological AssayBiologyBlood SerumCell BodyCellsChemicalsCirculationComplexDNA Molecular BiologyDataDevelopmentDevelopment and ResearchDoseDrugsE3 LigaseE3 Ubiquitin LigaseEffectivenessEncapsulatedEndosomesEsteroproteasesFaceFormulationGoalsHMG-20High Mobility Protein 20Intracellular TransportInvestigationLigandsLigaseLigase GeneLiteratureLocationMacropainMacroxyproteinaseMeasuresMediatingMedicationMetabolic Protein DegradationMethodsMiceMice MammalsModalityMolecularMolecular BiologyMolecular InteractionMulticatalytic ProteinaseMurineMusOutcomePathway interactionsPenetrationPeptidasesPeptide HydrolasesPeptidesPerformancePermeabilityPharmaceutical PreparationsPositionPositioning AttributeProsomeProtacProtease GeneProteasesProteasomeProteasome Endopeptidase ComplexProtein TurnoverProteinasesProteinsProteolysis targeting chimericProteolytic EnzymesProteosomeR & DR&DReceptosomesRegulatory Protein DegradationReportingResearchSerumSpecificityStructureStructure-Activity RelationshipSurfaceSynthetasesSystemTailTherapeuticThermodynamicThermodynamicsToxic effectToxicitiesUbiquitilationUbiquitinUbiquitin Protein LigaseUbiquitin-Protein Ligase ComplexesUbiquitin-Protein Ligase E3UbiquitinationUbiquitinoylationVariantVariationamphiphilicityassess effectivenesschemical structure functiondesigndesigningdetermine effectivenessdevelopmentaldrug/agenteffectiveness assessmenteffectiveness evaluationevaluate effectivenessexamine effectivenessfacesfacialimprovedin vivointerestlipid based nanoparticlelipid nanoparticlelipophilicitymanufacturabilitymanufacturemulticatalytic endopeptidase complexnano particle deliverynano-molarnanomolarnanoparticle deliverednanoparticle deliverynovelpathwayprecision medicineprecision-based medicineprotein degradationprotein protein interactionproteolysis targeting chimaeraproteolysis targeting chimerarecruitresearch and developmentsmall moleculestructure function relationshiptherapeutic agent developmenttherapeutic developmenttoolubiquinationubiquitin conjugationubiquitin-protein ligaseuptake
Description preview
Project Summary
This study seeks to advance heterobifunctional degraders that induce targeted protein degradation through
the ubiquitin proteasome pathway. Typically, molecular degraders involve a ligand that recruits an E3
ubiquitin ligase and another that targets a protein of interest (POI), forming an E3:Degrader:POI ternary
complex, leading to…
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