MASS-SPECTROMETRIC INVESTIGATIONS OF DRUG-RECEPTOR INTERACTIONS

Mass spectrometric (MS) detection of biologically important noncovalen t complexes is reviewed within the scope of on-going studies on this t opic from this laboratory. The merits of ion spray MS and tandem MS ar e demonstrated in this area with examples that show systematic studies of several receptor-ligand, enzyme-substrate, and enzyme-product comp lexes associated with both an established well-characterized biologica l system (lysozyme hydrolysis of N-acetylglucosamine) and an important modern receptor-ligand complex (FKBP-FK-506 and FKBP-rapamycin). Thes e examples and recent applications of negative ion MS and MS/MS with D NA adducts, heme-globin complexes, and antibiotic-binding proteins sug gest an exciting new area of applications for MS that have not been pr eviously available to investigators.