ADC Payload Screening and Profiling

Our Payload Screening and Profiling service identifies and evaluates cytotoxic agents for antibody-drug conjugates (ADCs). We screen a broad range of payloads, including DNA-damaging agents, tubulin inhibitors, protein degraders, and immune modulators, to support efficacy and safety assessment for targeted cancer therapies.

Topoisomerase I (Topo I) is a crucial enzyme in DNA replication and transcription. It alleviates torsional strain in the DNA helix by inducing single-strand breaks and re-ligation.

This assay assesses the ability of an ADC payload to inhibit Topo I and prevent DNA-strand re-ligation, helping determine payload potency and effectiveness as a Topo I inhibitor.

We offer absorbance-based and fluorescence-based tubulin polymerization assays to evaluate how ADC payloads disrupt microtubule dynamics and to provide mechanistic insight into their potential as anticancer agents.

Cell-cycle arrest assays evaluate how a cytotoxic payload affects cancer-cell proliferation by disrupting normal cell-cycle progression.

The resulting arrest can occur at phases including G1, S, or G2/M, depending on the payload mechanism of action, and can prevent cell division and contribute to cell death.

Flow-cytometry analysis quantifies apoptotic cells according to changes in cell size, complexity, and membrane asymmetry.

Annexin V FITC-A and PI-PE-A are used as apoptosis markers. Annexin V binds phosphatidylserine after its early-apoptosis translocation to the outer plasma membrane leaflet, while propidium iodide stains late apoptotic or dead cells but not live cells or early apoptotic cells.

Application Notes

                           

Dual Payload Pairs Screening Identifies Broad Synergy of DDR Inhibitors with TOPO1 ADC Payloads in Resistant and Wild-Type Cancer Models ↗