title: The mode of action of pleuromutilin derivatives. Location and properties of the pleuromutilin binding site on Escherichia coli ribosomes.
abstract: Using equilibrium dialysis techniques it could be demonstrated that (a) the pleuromutilin derivative 14-deoxy-14[(2-diethylaminoethyl)-mercaptoacetoxy] dihydromutilin HCl binds to one site per ribosome specifically, (b) the binding constant is 1.3 times 10(7) M(-1) and (c) chloramphenicol and puromycin compete with binding of the pleuromutilin derivative. Similarly the nucleotides CpA and CpCpA also displace the unsaturated derivative of the above-mentioned pleuromutilin compound. These findings suggest that the ribosomal binding site for pleuromutilin overlaps with that for chloramphenicol and analogs of the 3'-terminus of a tRNA, like puromycin or the nucleotides CpA and CpCpA.
mesh_terms: D000900:Anti-Bacterial Agents / Q000378:metabolism*; D001665:Binding Sites; D001667:Binding, Competitive; D002701:Chloramphenicol / Q000378:metabolism / Q000494:pharmacology; D003956:Dialysis; D004224:Diterpenes / Q000378:metabolism*; D004926:Escherichia coli / Q000378:metabolism*; D007700:Kinetics; D011083:Polycyclic Compounds; D011691:Puromycin / Q000378:metabolism / Q000494:pharmacology; D011955:Receptors, Drug; D012270:Ribosomes / Q000187:drug effects / Q000378:metabolism*; D000097567:Pleuromutilins
chemical_list: D000900:Anti-Bacterial Agents; D002701:Chloramphenicol; D004224:Diterpenes; D011083:Polycyclic Compounds; D011691:Puromycin; D011955:Receptors, Drug; D000097567:Pleuromutilins