{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,10,15]],"date-time":"2026-10-15T00:46:44Z","timestamp":1792025204789,"version":"4.4.0"},"reference-count":40,"publisher":"MDPI AG","issue":"3","license":[{"start":{"date-parts":[[2023,1,30]],"date-time":"2023-01-30T00:00:00Z","timestamp":1675036800000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/creativecommons.org\/licenses\/by\/4.0\/"}],"funder":[{"name":"National Natural Science Foundation of China","award":["21878022"],"award-info":[{"award-number":["21878022"]}]},{"name":"National Natural Science Foundation of China","award":["81673335"],"award-info":[{"award-number":["81673335"]}]},{"name":"National Natural Science Foundation of China","award":["32201053"],"award-info":[{"award-number":["32201053"]}]},{"name":"National Natural Science Foundation of China","award":["2021YFC2103100"],"award-info":[{"award-number":["2021YFC2103100"]}]},{"name":"National Natural Science Foundation of China","award":["2021YFF0600700"],"award-info":[{"award-number":["2021YFF0600700"]}]},{"name":"National Natural Science Foundation of China","award":["3100012222222"],"award-info":[{"award-number":["3100012222222"]}]},{"name":"National Key R&amp;D Program of China","award":["21878022"],"award-info":[{"award-number":["21878022"]}]},{"name":"National Key R&amp;D Program of China","award":["81673335"],"award-info":[{"award-number":["81673335"]}]},{"name":"National Key R&amp;D Program of China","award":["32201053"],"award-info":[{"award-number":["32201053"]}]},{"name":"National Key R&amp;D Program of China","award":["2021YFC2103100"],"award-info":[{"award-number":["2021YFC2103100"]}]},{"name":"National Key R&amp;D Program of China","award":["2021YFF0600700"],"award-info":[{"award-number":["2021YFF0600700"]}]},{"name":"National Key R&amp;D Program of China","award":["3100012222222"],"award-info":[{"award-number":["3100012222222"]}]},{"name":"Beijing Institute of Technology Research Fund Program for Young Scholars","award":["21878022"],"award-info":[{"award-number":["21878022"]}]},{"name":"Beijing Institute of Technology Research Fund Program for Young Scholars","award":["81673335"],"award-info":[{"award-number":["81673335"]}]},{"name":"Beijing Institute of Technology Research Fund Program for Young Scholars","award":["32201053"],"award-info":[{"award-number":["32201053"]}]},{"name":"Beijing Institute of Technology Research Fund Program for Young Scholars","award":["2021YFC2103100"],"award-info":[{"award-number":["2021YFC2103100"]}]},{"name":"Beijing Institute of Technology Research Fund Program for Young Scholars","award":["2021YFF0600700"],"award-info":[{"award-number":["2021YFF0600700"]}]},{"name":"Beijing Institute of Technology Research Fund Program for Young Scholars","award":["3100012222222"],"award-info":[{"award-number":["3100012222222"]}]}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Molecules"],"abstract":"<jats:p>Structurally unrelated antibiotics MLSB (macrolide-lincosamide-streptogramin B) compromised with clinically resistant pathogens because of the cross-resistance resulting from the structural modification of rRNA A2058. The structure\u2013activity relationships of a novel 3-O-descladinose azithromycin chemotype conjugating with nucleobases were fully explored with the aid of engineered E. coli SQ110DTC and SQ110LPTD. The conjugates of macrolides with nucleobases, especially adenine, displayed antibacterial superiority over telithromycin, azithromycin and clindamycin against rRNA A2058\/2059-mutated engineered E. coli strains at the cost of lowering permeability and increasing vulnerability to efflux proteins against clinical isolates.<\/jats:p>","DOI":"10.3390\/molecules28031327","type":"journal-article","created":{"date-parts":[[2023,1,30]],"date-time":"2023-01-30T07:56:48Z","timestamp":1675065408000},"page":"1327","update-policy":"https:\/\/doi.org\/10.3390\/mdpi_crossmark_policy","source":"Crossref","is-referenced-by-count":1,"title":["Design, Synthesis and Biological Evaluation of Conjugates of 3-O-Descladinose-azithromycin and Nucleobases against rRNA A2058G- or A2059G-Mutated Strains"],"prefix":"10.3390","volume":"28","author":[{"given":"Xiaotian","family":"Lian","sequence":"first","affiliation":[{"name":"Key Laboratory of Medical Molecule Science and Pharmaceutical Engineering, School of Chemistry and Chemical Engineering, Beijing Institute of Technology, Beijing 102488, China"},{"name":"Yangtze Delta Region Academy, Beijing Institute of Technology, Jiaxing 314019, China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Wentian","family":"Liu","sequence":"additional","affiliation":[{"name":"Key Laboratory of Medical Molecule Science and Pharmaceutical Engineering, School of Chemistry and Chemical Engineering, Beijing Institute of Technology, Beijing 102488, China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Bingzhi","family":"Fan","sequence":"additional","affiliation":[{"name":"Key Laboratory of Medical Molecule Science and Pharmaceutical Engineering, School of Chemistry and Chemical Engineering, Beijing Institute of Technology, Beijing 102488, China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Mingjia","family":"Yu","sequence":"additional","affiliation":[{"name":"Key Laboratory of Medical Molecule Science and Pharmaceutical Engineering, School of Chemistry and Chemical Engineering, Beijing Institute of Technology, Beijing 102488, China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-1309-8521","authenticated-orcid":false,"given":"Jianhua","family":"Liang","sequence":"additional","affiliation":[{"name":"Key Laboratory of Medical Molecule Science and Pharmaceutical Engineering, School of Chemistry and Chemical Engineering, Beijing Institute of Technology, Beijing 102488, China"},{"name":"Yangtze Delta Region Academy, Beijing Institute of Technology, Jiaxing 314019, China"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"1968","published-online":{"date-parts":[[2023,1,30]]},"reference":[{"key":"ref_1","doi-asserted-by":"crossref","first-page":"35","DOI":"10.1038\/nrmicro3155","article-title":"Ribosome-targeting antibiotics and mechanisms of bacterial resistance","volume":"12","author":"Wilson","year":"2014","journal-title":"Nat. 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