2021
Targeted degradation of transcription factors by TRAFTACs: TRAnscription Factor TArgeting Chimeras
Samarasinghe KTG, Jaime-Figueroa S, Burgess M, Nalawansha DA, Dai K, Hu Z, Bebenek A, Holley SA, Crews CM. Targeted degradation of transcription factors by TRAFTACs: TRAnscription Factor TArgeting Chimeras. Cell Chemical Biology 2021, 28: 648-661.e5. PMID: 33836141, PMCID: PMC8524358, DOI: 10.1016/j.chembiol.2021.03.011.Peer-Reviewed Original ResearchConceptsTranscription factorsTargeted degradationTranscription factor degradationDNA-binding proteinsMultiple signaling pathwaysGeneralizable strategyDCas9 proteinProtein familyLigandable sitesProteasomal pathwaySignaling pathwaysOverexpression of oncoproteinsAberrant activationChimeric oligonucleotideProteinChimerasFactor degradationNF-κBPathwayHaloTagDegradationBrachyuryOverexpressionOncoproteinOligonucleotide
2001
The anti-inflammatory natural product parthenolide from the medicinal herb Feverfew directly binds to and inhibits IκB kinase
Kwok B, Koh B, Ndubuisi M, Elofsson M, Crews C. The anti-inflammatory natural product parthenolide from the medicinal herb Feverfew directly binds to and inhibits IκB kinase. Cell Chemical Biology 2001, 8: 759-766. PMID: 11514225, DOI: 10.1016/s1074-5521(01)00049-7.Peer-Reviewed Original ResearchConceptsAnti-inflammatory activityHerb feverfewPro-inflammatory signaling pathwaysDirect molecular targetVivo anti-inflammatory activityAnti-inflammatory propertiesAnti-inflammatory agentsCytokine-mediated stimulationCytokine-mediated signalingIkappaB kinase betaSesquiterpene lactone parthenolidePharmaceutical interventionsIκB kinaseMolecular targetsNatural product parthenolideKinase betaParthenolideCysteine 179Signaling pathwaysPossible molecular basisIntracellular signaling processesAttractive targetIKK complexMolecular mechanismsAlpha-methylene gamma-lactone moiety