MM-45289, A POTENT GLYCOPEPTIDE ANTIBIOTIC WHICH INTERACTS WEAKLY WITH DIACETYL-L-LYSYL-D-ALANYL-D-ALANINE

MM 45289 (A82846A, eremomycin), a glycopeptide antibiotic of the vancomycin type, was confirmed to have improved antibacterial activity over vancomycin. However its affinity (Ka) for the target site peptide mimetic diacetyl-L-lysyl-D-alanyl-D-alanine (DALAA) was 23-fold lower. Concentrations of DALAA required to reverse the antibacterial activity of MM 45289 were in the order of 10 to 50-fold higher than for vancomycin. These results have implications for both mode of action studies and mechanism-based screening strategies for this class of antibiotic. © 1990, JAPAN ANTIBIOTICS RESEARCH ASSOCIATION. All rights reserved.