Cited by 157RNA and protein synthesis mechanismsAntibiotic Resistance in BacteriaBacterial Genetics and Biotechnology

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Glycylcyclines bind to the high-affinity tetracycline ribosomal binding site and evade Tet(M)- and Tet(O)-mediated ribosomal protection

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Bergeron, J, Ammirati, M, Danley, D, James, L, Norcia, M, Retsema, J, Strick, C A, Su, W G, Sutcliffe, J, Wondrack, L·1996·Antimicrobial Agents and Chemotherapy

DOI 10.1128/aac.40.9.2226PMC PMC163507

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Abstract

N,N-dimethylglycylamido (DMG) derivatives of 6-demethyl-6-deoxytetracycline and doxycycline bind 5-fold more effectively than tetracycline to the tetracycline high-affinity binding site on the Escherichia coli 70S ribosome, which correlates with a 10-fold increase in potency for inhibition of E. coli cell-free translation. The potencies of DMG-doxycycline and DMG-6-demethyl-6-deoxytetracycline were unaffected by the ribosomal tetracycline resistance factors Tet(M) and Tet(O) in cell-free translation assays and whole-cell bioassays with a conditional Tet(M)-producing E. coli strain.

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Authors: Bergeron, J., Ammirati, M., Danley, D., James, L., Norcia, M., Retsema, J., Strick, C. A., Su, W. G., Sutcliffe, J., & Wondrack, L.
Affiliations: Pfizer (United States) (US)
ORCID: Ammirati, M
Venue: Antimicrobial Agents and Chemotherapy
Publisher: American Society for Microbiology
Published: 1996-09
Volume: 40
Issue: 9
Pages: 2226-2228
ISSN: 0066-4804 (ISSN-L)
1098-6596
DOI: 10.1128/aac.40.9.2226
PMC: PMC163507
OpenAlex: W2101570801
Cited by: 157
References: 24
Citations by year: 2026: 1 · 2025: 3 · 2024: 1 · 2023: 2 · 2022: 2 · 2021: 5 · 2020: 1 · 2019: 3 · 2018: 4 · 2017: 4 · 2016: 3 · 2015: 9 · 2014: 8 · 2013: 8 · 2012: 7
FWCI: 0.51
Type: journal article
Language: en
Open access: green
europepmc.org
Licence: journals.asm.org/non-commercial-tdm-license (tdm)
Locations: Antimicrobial Agents and Chemotherapy (publishedVersion)
Europe PMC (PubMed Central) (publishedVersion)
PubMed Central (publishedVersion)
PubMed (publishedVersion)
Topics: Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › RNA and protein synthesis mechanisms
Health Sciences › Medicine › Microbiology (medical) › Antibiotic Resistance in Bacteria
Life Sciences › Biochemistry, Genetics and Molecular Biology › Genetics › Bacterial Genetics and Biotechnology
Keywords: glycylcyclines, tetM, tetO, tetracycline resistance, Escherichia coli ribosome, antibiotic resistance
MeSH terms: Anti-Bacterial Agents, Biological Assay, Cell-Free System, Doxycycline, Escherichia coli, Glycylglycine, Peptide Biosynthesis, Ribosomes, Tetracycline Resistance

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Glycylcyclines bind to the high-affinity tetracycline ribosomal binding site and evade Tet(M)- and Tet(O)-mediated ribosomal protection

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