[SLAS] Identify Effective Therapeutics with Simple, Quantitative Cell-Based Assays That Measure Receptor Internalization

[SLAS] Identify Effective Therapeutics with Simple, Quantitative Cell-Based Assays That Measure Receptor Internalization
Version:
21294 011322

File Name/Number:
SLAS

Year:
2022

 

Both multi- and single-pass membrane receptors constitutively exhibit complicated and dynamic membrane receptor trafficking as well as internalization induced by ligand or compound binding. Measuring how therapeutic molecule binding to membrane receptors affects receptor internalization can provide insight into drug tolerance, unwanted side effects, diseases, and ultimately help with identifying safer drugs. Additionally, antibody-based therapeutics that target specific receptors such as the immuno-oncology checkpoint receptors can induce high levels of internalization and serve as candidates for conjugation to cytotoxic compounds. These therapeutic antibody-drug conjugates (ADCs) take advantage of both antibody specificity for tumor antigens and antibody induction of receptor internalization to deliver cytotoxic drugs to cancer cells effectively.