High-throughput luminescence assays for ubiquitin ligases

Ubiquitin ligases (E3s) play a pivotal role in regulating protein stability and cellular signaling by catalyzing the transfer of ubiquitin to substrate proteins, marking them for degradation or functional modulation. Given their involvement in numerous diseases and targeted protein degradation modalities, E3 ligases have emerged as attractive therapeutic targets. Developing biochemical assays to measure E3 activity is essential for drug discovery and mechanistic studies. One accessible and robust approach involves luminescence-based assays that monitor ATP consumption. These assays not only provide a high-throughput means to measure E3 function, but also enable selectivity profiling across the broader family of ATP-dependent enzymes, including helicases and kinases, ensuring target specificity.

ASMS using MALDI MS and polymeric enrichment arrays (PEAs) for molecular glue discovery

The identification of small molecule binders to a distinct target is a common strategy to initiate drug discovery efforts, including for modalities that induce proximity, such as molecular glues. Affinity selection mass spectrometry, also known as ASMS, combined with polymeric enrichment arrays, offers unique benefits for identifying not only binders to virtually any target, including proteins and oligonucleotides such as RNA, but it also offers opportunities to detect proximity. Download this tech note to discovery how Peapod Bio’s innovative ASMS approach identified a small molecule binder and could also detect ternary complex formation.  

Acetyltransferase assays using MALDI MS and polymeric enrichment arrays (PEAs)

Acetyltransferase enzymes are key players implicated in gene expression regulation, DNA replication and repair, where perturbation is associated with various diseases including cancer. Traditional assays rely on labels that lack selectivity or focus on cofactor metabolism, generating indirect measurements that can lead researchers down the wrong path. Learn how Peapod Bio’s innovative mass spectrometry assay offers the ability to directly measure substrate acetylation, including multiple acetylation events, providing clear, interpretable data faster to drive projects forward.

HTS for sortase A inhibitors using MALDI MS and polymeric enrichment arrays (PEAs)

The rise of antibiotic-resistant Staphylococcus aureaus necessitates new therapeutics to combat infections. Sortase A is an essential enzyme for virulence and a promising therapeutic target. Mass spectrometry combined with polymeric enrichment arrays (PEAs) offers a label-free and high-throughput technology to measure the protease and ligase activities in a multiplexed readout. Discover how Peapod Bio utilized this innovative approach to screen 200,000 compounds in days to reveal novel sortase A inhibitors.