In this white paper, we describe the development of Octet® Bio-Layer Interferometry (BLI) assays that validate and characterize bi-functional small molecule CIR target binding and covalent reaction kinetics.
We demonstrate how the Octet® system can be employed to efficiently characterize CIR binding affinities against both a prostate tumor antigen and human serum antibodies, as well as measure the selective covalent recruitment of these antibodies to the tumor antigen. These assays can accelerate the advancement of lead compounds to in vivo validation studies, and have additional utility in characterizing emerging classes of covalent inhibitor drugs.
Eden Kapcan, Zi Yang, Benjamin Lake, Anthony F. Rullo Department of Pathology and Molecular Medicine, McMaster University, Ontario, Canada
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