A BRET biosensor for measuring uncompetitive engagement of PRMT5 complexes in cells
- kilianhuber
- 14 minutes ago
- 1 min read
New in Nature Communications: a live-cell BRET biosensor to study how PRMT5 inhibitors engage their target in a tumour-context cellular environment
We investigated the PRMT5 inhibitor GSK3326595 and developed CBH-002, a BRET probe that binds a genetically encoded PRMT5-NanoLuc biosensor and senses changes in SAM/MTA. This enabled us to determine EC50 values in MTAP wild-type and MTAP-deleted cells, quantifying inhibitor potency in a cell-context-dependent way - adding another layer of personalised medicine
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