Up-to-date report on the resistance of macrolide antibiotics and future macrolides.
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Accession number;00A0360408
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| Title;Up-to-date report on the resistance of macrolide antibiotics and future macrolides. |
| Author;
OHARA KOJI
(Chiba Univ., Fac. of Pharm. Sci.)
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Journal Title;Japanese Journal of Chemotherapy
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Journal Code:F0608A
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ISSN:1340-7007
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VOL.48;NO.3;PAGE.169-190(2000)
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| Figure&Table&Reference;FIG.9, TBL.2, REF.139 |
| Pub. Country;Japan |
| Language;Japanese |
| Abstract;For macrolide antibiotic resistance on the clinical isolates, it is enough to remember only that (1) macrolide antibiotics come to be unable to bind to ribosome and become resistant due to the modification of the ribosomal target site in the 23 SrRNA in the 50 S subunit of 70 S ribosome by N6, N6-dimethylase, before 30 years. Recently, however, the macrolide resistance mechanism has diversified due to the various kinds of macrolide development starting from erythromycin. Macrolide-resistant strains have evolved extremly by using large amounts of macrolides and new macrolides. The details of the dimethylational mechanism and new resistance mechanisms come to light together with the advance of recent study using biotechnology. Addition to these resistance mechanism are known as follows.: (2) basic mutation of multiple sites in the 23 SrRNA, (3) mutation of ribosomal protein in the 50 S subunit and elsewhere, (4) macrolide efflux protein, (5) changes in macrolide permeability, (6) inactivation of erythromycin esterase, (7) macrolide 2'-phosphotransferase, (8) inactivating mechanism due to the macrolide 2'-glycosylation, (9) reduction of macrolide formyl group, and (10) resistance due to macrolide deacylation. There are many subgroups, and they are specific to each strain and also to each bacterial species. Faced with the problem of the emergence of various kinds of macrolide resistance, it is expected that new macrolides (15-memberring macrolide such as azithromycin and 14-member-ring macrolide such as ketolide) will appear in the future. A new battle between the new macrolides and resistant strains showing the new mechanism is now going to start over again, and then macrolide resistance strains must be obliged to generate newly evolution of macrolide resistance mechanism (s). (author abst.) |
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