The DOI matches its Crossref record; 24 of the 24 references it cites were found in a registry or an index.
Glycylcyclines bind to the high-affinity tetracycline ribosomal binding site and evade Tet(M)- and Tet(O)-mediated ribosomal protection
Open accessAbstract
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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“In contrast, the attached C9-glycyl side chain of Tgc would prevent access of the residues of loop III of TetM (Fig. 3 E and F), leading us to suggest that this steric hindrance contributes, together with the increased affinity of Tgc (7,8,27), to explaining how Tgc overcomes TetM-mediated resistance whereas tetracycline cannot (8).”
From Structural basis for TetM-mediated tetracycline resistance (2012) · cites this paper as [7]
In the citing paper
“The third generation of tetracycline derivatives, such as tigecycline (Tgc), display enhanced antimicrobial activity, overcoming efflux and ribosome protection mechanisms (6)(7)(8).”
From Structural basis for TetM-mediated tetracycline resistance (2012) · cites this paper as [7]
Citations
Cites
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[6] Use of T7 RNA polymerase to direct expression of cloned genes
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Cited by
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Chopra, I., & Roberts, M. (2001) · Microbiology and Molecular Biology Reviews · doi:10.1128/mmbr.65.2.232-260.2001 · Cited by 4,517
Tetracycline Antibiotics and ResistancePreprint
Grossman, T. H. (2016) · Cold Spring Harbor Perspectives in Medicine · doi:10.1101/cshperspect.a025387 · Cited by 737
Brown‐Elliott, B. A., Nash, K. A., & Wallace, R. J. (2012) · Clinical Microbiology Reviews · doi:10.1128/cmr.05030-11 · Cited by 551
Tetracycline antibiotics and resistance mechanisms
Nguyen, F., Starosta, A. L., Arenz, S., Sohmen, D., Dönhöfer, A., & Wilson, D. N. (2014) · Biological Chemistry · doi:10.1515/hsz-2013-0292 · Cited by 529
The Evolving Role of Chemical Synthesis in Antibacterial Drug Discovery
Wright, P. M., Seiple, I. B., & Myers, A. G. (2014) · Angewandte Chemie International Edition · doi:10.1002/anie.201310843 · Cited by 428
Metadata
- 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
- 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
- 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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