Pomalidomide - Peg2-azide is a synthetic E3 ligand -linker conjugate containing Pomalidomide based cereblon ligand and 2-unit PEG linker.
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Pomalidomide - Peg2-azide is a synthetic E3 ligand -linker conjugate containing Pomalidomide based cereblon ligand and 2-unit PEG linker. PROTAC can be synthesized to target protein degradation[1].
The IC50 value of protac compound 21[(BRD4 BD1, IC50 = 41.8 nM) composed of Pomalidomide - Peg2-azide] was 0.81 μM in inhibiting THP-1 cell line growth. At the concentration of 1 μM, compound 21 can effectively degrade BRD4 protein and inhibit c-Myc[1].
参考文献:
[1]. Zhang F, Wu Z, et,al. Discovery of a new class of PROTAC BRD4 degraders based on a dihydroquinazolinone derivative and lenalidomide/pomalidomide. Bioorg Med Chem. 2020 Jan 1;28(1):115228. doi: 10.1016/j.bmc.2019.115228. Epub 2019 Nov 30. PMID: 31813613.
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