title: Moxalactam (6059-S), a new 1-oxa-beta-lactam: binding affinity for penicillin-binding proteins of Escherichia coli K-12.
abstract: Moxalactam (6059-S) is a new beta-lactam derivative with a structure markedly different from those of penicillins or cephalosporins. The binding activity of 6059-S to penicillin-binding proteins (PBPs) in Escherichia coli K-12 was tested. [14C]benzylpenicillin- or [14C]6059-S-bound inner membrane proteins of E. coli K-12 were rapidly detected without using fluorography. 6059-S had the highest affinity for PBP-3 and -7/8, had a higher affinity than benzylpenicillin for PBP-1A, -1Bs, -4, and -5/6 and a lower affinity for PBP-2, 609134, the 1-thiacephem analog of 6059-S, showed as high an affinity for PBP-1A, -1Bs, -3, and -4 as 6059-S but a lower affinity for PBP-5/6.
mesh_terms: D001426:Bacterial Proteins / Q000378:metabolism*; D001667:Binding, Competitive; D002462:Cell Membrane / Q000378:metabolism; D002511:Cephalosporins / Q000378:metabolism*; D002513:Cephamycins / Q000378:metabolism*; D055598:Chemical Phenomena; D002621:Chemistry; D004926:Escherichia coli / Q000378:metabolism*; D008565:Membrane Proteins / Q000378:metabolism; D009070:Moxalactam; D010400:Penicillin G / Q000378:metabolism*; D011485:Protein Binding / Q000187:drug effects
chemical_list: D001426:Bacterial Proteins; D002511:Cephalosporins; D002513:Cephamycins; D008565:Membrane Proteins; D010400:Penicillin G; D009070:Moxalactam