Identifying Fragments for Covalent Drug Discovery by Combining Intact Ms Analysis on Recombinant Proteins with Cellular Chemoproteomics Approaches
Time: 9:30 am
day: Conference Day 2
Details:
- Discussing the approach of using both intact MS analysis for the high throughput screening of covalent fragments against recombinant proteins, with lower throughput chemoproteomics approaches – in cell competition between compound and desthiobiotin iodoacetamide (DBIA) – to determine target engagement and selectivity against native proteins
- Evaluating in-cell DBIA results to identify protein degraders and stabilizers
- Understanding the “ligandibility” of Cysteine residues to identify optimal cysteine residues that can be leveraged for drug development
