2015
HaloPROTACS: Use of Small Molecule PROTACs to Induce Degradation of HaloTag Fusion Proteins
Buckley DL, Raina K, Darricarrere N, Hines J, Gustafson JL, Smith IE, Miah AH, Harling JD, Crews CM. HaloPROTACS: Use of Small Molecule PROTACs to Induce Degradation of HaloTag Fusion Proteins. ACS Chemical Biology 2015, 10: 1831-1837. PMID: 26070106, PMCID: PMC4629848, DOI: 10.1021/acschembio.5b00442.Peer-Reviewed Original ResearchConceptsChemical probesMore drug-like propertiesFusion proteinSmall-molecule PROTACsProtein degradationDrug-like propertiesE3 ligase ligandChemical genetic toolsSpecific E3 ligasesProtein of interestVHL ligandsHaloTag fusion proteinsE3 ligasesGenetic toolsHeterobifunctional moleculesNumerous proteinsHaloPROTACLigandsPROTACsProteinNovel classAttractive strategyDegradationProbeLigases
2011
Small-molecule hydrophobic tagging–induced degradation of HaloTag fusion proteins
Neklesa TK, Tae HS, Schneekloth AR, Stulberg MJ, Corson TW, Sundberg TB, Raina K, Holley SA, Crews CM. Small-molecule hydrophobic tagging–induced degradation of HaloTag fusion proteins. Nature Chemical Biology 2011, 7: 538-543. PMID: 21725302, PMCID: PMC3139752, DOI: 10.1038/nchembio.597.Peer-Reviewed Original ResearchConceptsFusion proteinHaloTag fusion proteinsProtein functionTransmembrane proteinProteinNew toolChemical spaceDegradationTags