{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,10,5]],"date-time":"2026-10-05T00:07:43Z","timestamp":1791158863038,"version":"4.1.0"},"reference-count":34,"publisher":"American Society for Microbiology","issue":"6","license":[{"start":{"date-parts":[[2004,6,1]],"date-time":"2004-06-01T00:00:00Z","timestamp":1086048000000},"content-version":"tdm","delay-in-days":0,"URL":"https:\/\/journals.asm.org\/non-commercial-tdm-license"}],"content-domain":{"domain":["journals.asm.org"],"crossmark-restriction":true},"short-container-title":["Antimicrob Agents Chemother"],"published-print":{"date-parts":[[2004,6]]},"abstract":"<jats:title>ABSTRACT<\/jats:title>\n          <jats:p>\n            The activity of tigecycline, 9-(\n            <jats:italic>t<\/jats:italic>\n            -butylglycylamido)-minocycline, against\n            <jats:italic>Escherichia coli<\/jats:italic>\n            KAM3 (\n            <jats:italic>acrB<\/jats:italic>\n            ) strains harboring plasmids encoding various tetracycline-specific efflux transporter genes,\n            <jats:italic>tet<\/jats:italic>\n            (B),\n            <jats:italic>tet<\/jats:italic>\n            (C), and\n            <jats:italic>tet<\/jats:italic>\n            (K), and multidrug transporter genes,\n            <jats:italic>acrAB<\/jats:italic>\n            ,\n            <jats:italic>acrEF<\/jats:italic>\n            , and\n            <jats:italic>bcr<\/jats:italic>\n            , was examined. Tigecycline showed potent activity against all three Tet-expressing, tetracycline-resistant strains, with the MICs for the strains being equal to that for the host strain. In the Tet(B)-containing vesicle study, tigecycline did not significantly inhibit tetracycline efflux-coupled proton translocation and at 10 \u03bcM did not cause proton translocation. This suggests that tigecycline is not recognized by the Tet efflux transporter at a low concentration; therefore, it exhibits significant antibacterial activity. These properties can explain its potent activity against bacteria with a Tet efflux resistance determinant. Tigecycline induced the Tet(B) protein approximately four times more efficiently than tetracycline, as determined by Western blotting, indicating that it is at least recognized by a TetR repressor. The MICs for multidrug efflux proteins AcrAB and AcrEF were increased fourfold. Tigecycline inhibited active ethidium bromide efflux from intact\n            <jats:italic>E. coli<\/jats:italic>\n            cells overproducing AcrAB. Therefore, tigecycline is a possible substrate of AcrAB and its close homolog, AcrEF, which are resistance-modulation-division-type multicomponent efflux transporters.\n          <\/jats:p>","DOI":"10.1128\/aac.48.6.2179-2184.2004","type":"journal-article","created":{"date-parts":[[2004,5,21]],"date-time":"2004-05-21T18:38:42Z","timestamp":1085164722000},"page":"2179-2184","update-policy":"https:\/\/doi.org\/10.1128\/asmj-crossmark-policy-page","source":"Crossref","is-referenced-by-count":103,"title":["Effects of Efflux Transporter Genes on Susceptibility of\n            <i>Escherichia coli<\/i>\n            to Tigecycline (GAR-936)"],"prefix":"10.1128","volume":"48","author":[{"given":"Takahiro","family":"Hirata","sequence":"first","affiliation":[{"name":"Department of Cell Membrane Biology, Institute of Scientific and Industrial Research, Osaka University, Ibaraki"},{"name":"CREST, Japan Science and Technology Corporation, Osaka 567-0047"},{"name":"Faculty of Pharmaceutical Science, Osaka University, Suita, Osaka 565-0871, Japan"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Asami","family":"Saito","sequence":"additional","affiliation":[{"name":"Department of Cell Membrane Biology, Institute of Scientific and Industrial Research, Osaka University, Ibaraki"},{"name":"Faculty of Pharmaceutical Science, Osaka University, Suita, Osaka 565-0871, Japan"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Kunihiko","family":"Nishino","sequence":"additional","affiliation":[{"name":"Department of Cell Membrane Biology, Institute of Scientific and Industrial Research, Osaka University, Ibaraki"},{"name":"CREST, Japan Science and Technology Corporation, Osaka 567-0047"},{"name":"Faculty of Pharmaceutical Science, Osaka University, Suita, Osaka 565-0871, Japan"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Norihisa","family":"Tamura","sequence":"additional","affiliation":[{"name":"Department of Cell Membrane Biology, Institute of Scientific and Industrial Research, Osaka University, Ibaraki"},{"name":"CREST, Japan Science and Technology Corporation, Osaka 567-0047"},{"name":"Faculty of Pharmaceutical Science, Osaka University, Suita, Osaka 565-0871, Japan"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Akihito","family":"Yamaguchi","sequence":"additional","affiliation":[{"name":"Department of Cell Membrane Biology, Institute of Scientific and Industrial Research, Osaka University, Ibaraki"},{"name":"CREST, Japan Science and Technology Corporation, Osaka 567-0047"},{"name":"Faculty of Pharmaceutical Science, Osaka University, Suita, Osaka 565-0871, Japan"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"235","reference":[{"key":"e_1_3_2_2_2","doi-asserted-by":"crossref","first-page":"379","DOI":"10.1517\/13543784.12.3.379","volume":"12","year":"2003","unstructured":"Abbanat, D., M. 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