Methylarginine targeting chimeras for lysosomal degradation of intracellular proteins
Seabrook L, Franco C, Loy C, Osman J, Fredlender C, Zimak J, Campos M, Nguyen S, Watson R, Levine S, Khalil M, Sumigray K, Trader D, Albrecht L. Methylarginine targeting chimeras for lysosomal degradation of intracellular proteins. Nature Chemical Biology 2024, 20: 1566-1576. PMID: 39414979, DOI: 10.1038/s41589-024-01741-y.Peer-Reviewed Original ResearchProtein arginine methyltransferasesTarget proteinsLoss-of-function phenotypesDegradation of intracellular proteinsUbiquitin-proteasome pathwayHistone deacetylase 6Bromodomain-containing protein 4Discovery of small moleculesTargeted Protein DegradationDegrade target proteinsTargeting chimerasArginine methylationArginine methyltransferasesProtein methylationPathogenic proteinsLysosomal deliveryLysosomal pathwayIntracellular proteinsLysosomal degradationHeterobifunctional small moleculesProtein degradationSmall-molecule degradersLysosomal proteolysisSubstrate degradationSmall moleculesRegulated induced proximity targeting chimeras—RIPTACs—A heterobifunctional small molecule strategy for cancer selective therapies
Raina K, Forbes C, Stronk R, Rappi J, Eastman K, Zaware N, Yu X, Li H, Bhardwaj A, Gerritz S, Forgione M, Hundt A, King M, Posner Z, Correia A, McGovern A, Puleo D, Chenard R, Mousseau J, Vergara J, Garvin E, Macaluso J, Martin M, Bassoli K, Jones K, Garcia M, Howard K, Yaggi M, Smith L, Chen J, Mayfield A, De Leon C, Hines J, Kayser-Bricker K, Crews C. Regulated induced proximity targeting chimeras—RIPTACs—A heterobifunctional small molecule strategy for cancer selective therapies. Cell Chemical Biology 2024, 31: 1490-1502.e42. PMID: 39116881, PMCID: PMC11371387, DOI: 10.1016/j.chembiol.2024.07.005.Peer-Reviewed Original ResearchProtein-protein interactionsTarget proteinsTernary complexChemical biology studiesExpressed intracellular proteinStable ternary complexAnti-proliferative responseEssential proteinsProtein proximityEffector ligandsIntracellular proteinsCDK inhibitorsTarget-expressing cellsHeterobifunctional small moleculesSmall moleculesCell survivalTumor cellsTherapeutic modalitiesProteinSelective therapySmall molecule strategiesLigandBiological studies
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