Tīmeklis2024. gada 3. aug. · They validated the approach by discovering a new RBM39 molecular glue degrader, structurally similar to others previously described. … Tīmeklis2024. gada 5. sept. · The structural and kinetic studies confirm aryl sulfonamides as molecular glues in the recruitment of RBM39 and provide a framework for future efforts to utilize DCAF15 to degrade other protein of ...
Structural Basis and Kinetic Pathway of RBM39 Recruitment to
Tīmeklis2024. gada 3. aug. · Examples of molecular glues that induce proteolysis of targets include the IMiDs (immune modulatory drugs; e.g., thalidomide), which generate a novel interaction between a substrate (e.g.,... Tīmeklis2024. gada 5. nov. · Structural Basis and Kinetic Pathway of RBM39 Recruitment to DCAF15 by a Sulfonamide Molecular Glue E7820 E7820 and indisulam are two … how to work with angels pdf
Arylsulfonamide mediated RBM39 degradation causes aberrant
Tīmeklis2024. gada 1. nov. · To facilitate targeted protein degradation, molecular glues such as immunomodulatory imide drugs (IMiD, e.g., thalidomide, lenalidomide, … Whole-cell lysates were harvested using RIPA buffer with 1% HALT protease inhibitor (Sigma, UK) and quantified using the BCA protein assay (ThermoScientific Pierce) as per the manufacturer’s protocol. Cell lysates containing equal protein concentrations were loaded onto a 4–20% Mini-Protean TGX pre-cast gel (Bio … Skatīt vairāk IMR-32, BE(2)C and SK-N-AS cells cell were purchased from the American Type Culture Collection (ATCC) (Manassas, VA). KELLY and SH-SY-5Y were obtained from the German … Skatīt vairāk Cells were seeded overnight in triplicate in 96 well plates and treated with vehicle control (0.1% DMSO) or indisulam or E7820 (Sigma Aldrich, UK) at various doses for 72 h. SRB assay was performed according to the … Skatīt vairāk IMR-32 or KELLY cells were seeded overnight in 96-well plates. Cells were transfected with SMARTpool DCAF15 siRNA (L-0.31237 … Skatīt vairāk KELLY cells were transduced with Edit-R CRISPR-Cas9-TurboGFP lentiviral particles (Dharmacon #VCAS11864) in a 96 well plate, expanded and GFP positive cells sorted via FACS (total of two rounds). KELLY-Cas9 cells … Skatīt vairāk TīmeklisdCeMM1 is a RBM39 glue degrader. dCeMM1 can re-direct the activity of the CRL4DCAF15 ligase. dCeMM1 can decrease the expression levels of RBM39 in WT KBM7 cells. 体外活性: dCeMM1 (0-100 µM; 3 days) inhibited cell growth with the EC50 of 3 and 8 µ M for WT and UBE2Mmut KBM7 cells, respectively. origins headache cream