Production Of Radiolabeled Monoclonal Antibody Conjugates By Photoaffinity Labeling PDF Download

This report discusses activities and progress that has occurred since initiation of this project on September 1, 1989. We have synthesized ethyl N, N(prime)-bis(benzoylmercaptoacetyl)-2,3-diaminopropanoate, a ligand to be used as a bifunctional chelating agent (BFCA), to form 186Re or 188Re (186Re/188Re) complexes. 186Re/188Re, in reducing media, reacts with this ligand to form 186Re/188Re-CO2DADS chelates that will be used to formulate new radiolabeled photoaffinity labels (RPALs). Initial steps have been taken to synthesize R-As-dithiol compounds. This approach will be used to produce 77As-RPALs or covalently link 77As directly to monoclonal antibodies (MAbs). The R group will contain a group that can be used for conjugation reactions. Spectral and photochemical properties of various types of photoaffinity labels (PALs) have been studied. Acrylo-azido compounds and 9-azido acridine have been studied as well as several other photoprobes. The binding characteristics of the azido-based PALs to HSA have been studied and progress has been made on developing techniques for efficiently separating of non-covalently sound PALs. The Nd-YAG laser was purchased and arrived in 1990. It has been assembled and tested and is now operational.