Enhancing Antiproliferative Activity and Selectivity of a FLT-3 Inhibitor by Proteolysis Targeting Chimera Conversion

Burslem, George M., Song, Jayoung, Chen, Xin, Hines, John, Crews, Craig M.·2018·Journal of the American Chemical Society
DOI 10.1021/jacs.8b10320

Cited by (188)

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  64. Synthesis and Biological Characterization of Dual-Specific Proteolysis Target Chimeras (Protacs) for the Kinases Flt3-Itd and Mapk14 with Antileukemic Activity
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  72. BindingDB Entry 50010738: Discovery of SHP2-D26 as a First, Potent, and Effective PROTAC Degrader of SHP2 Protein.
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  77. BindingDB Entry 50013059: First orally bioavailable prodrug of proteolysis targeting chimera (PROTAC) degrades cyclin-dependent kinases 2/4/6 in vivo.
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  78. BindingDB Entry 50021145: Annual review of PROTAC degraders as anticancer agents in 2022.
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  79. BindingDB Entry 50016839: VHL-based PROTACs as potential therapeutic agents: Recent progress and perspectives.
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  80. BindingDB Entry 50013984: Discovery of thalidomide-based PROTAC small molecules as the highly efficient SHP2 degraders.
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  81. BindingDB Entry 50014922: Discovery of a Brigatinib Degrader SIAIS164018 with Destroying Metastasis-Related Oncoproteins and a Reshuffling Kinome Profile.
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  82. BindingDB Entry 50021843: Structural and Physicochemical Features of Oral PROTACs.
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  83. BindingDB Entry 50013823: Discovery of selective CDK9 degraders with enhancing antiproliferative activity through PROTAC conversion.
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  85. BindingDB Entry 50017713: Structure-based discovery of receptor tyrosine kinase AXL degraders with excellent anti-tumor activity by selectively degrading AXL and inducing methuosis.
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  86. BindingDB Entry 50020717: A beginner's guide to current synthetic linker strategies towards VHL-recruiting PROTACs.
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  87. BindingDB Entry 50008708: Identification of Pyrrolo[2,3- d]pyrimidine-Based Derivatives as Potent and Orally Effective Fms-like Tyrosine Receptor Kinase 3 (FLT3) Inhibitors for Treating Acute Myelogenous Leukemia.
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