The DOI matches its Crossref record; 42 of the 42 references it cites were found in a registry or an index.
New developments in tetracycline antibiotics: glycylcyclines and tetracycline efflux pump inhibitors
Abstract
The tetracyclines, discovered in the 1940s, are a well-established class of antibiotics that still have a role in treating microbial infections in man. However, the widespread emergence of bacterial resistance due to efflux and ribosomal protection mechanisms has severely limited their effectiveness. A new generation of tetracyclines, the glycylcyclines, has been developed to overcome resistance to earlier tetracyclines. One of the new glycylcyclines, 9-t-butylglyclamido-minocycline (GAR-936, tigecycline) is currently undergoing clinical trials. This review considers the current status of glycylcyclines and the possibility that resistance to these agents might arise in the future. Other approaches are also being taken to address the emergence of resistance to tetracyclines. Recently, a number of tetracycline efflux pump inhibitors have been discovered that might be used in combination with earlier tetracyclines to restore their activity against resistant organisms. However, the development of tetracycline efflux pump inhibitors is complicated by the occurrence of several efflux pump sub-families and by the presence of both efflux and ribosomal protection mechanisms in the same organism, especially in naturally occurring, Gram-positive clinical isolates.
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“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 [6]
Citations
Cites
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Cited by
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Coagulase-Negative Staphylococci
Becker, K., Heilmann, C., & Peters, G. (2014) · Clinical Microbiology Reviews · doi:10.1128/cmr.00109-13 · Cited by 1,742
Efflux-mediated antimicrobial resistance
Poole, K. (2005) · Journal of Antimicrobial Chemotherapy · doi:10.1093/jac/dki171 · Cited by 1,082
Natural products to drugs: natural product-derived compounds in clinical trials
Butler, M. S. (2008) · Natural Product Reports · doi:10.1039/b514294f · Cited by 1,086
Update on acquired tetracycline resistance genes
Roberts, M. C. (2005) · FEMS Microbiology Letters · doi:10.1016/j.femsle.2005.02.034 · Cited by 1,010
Efflux-Mediated Drug Resistance in Bacteria
Li, X.-Z., & Nikaido, H. (2004) · Drugs · doi:10.2165/00003495-200464020-00004 · Cited by 803
Metadata
- Authors
- Chopra, I.
- Affiliations
- University of Leeds (GB)
- Corresponding author
- Chopra, Ian
- Venue
- Drug Resistance Updates
- Publisher
- Elsevier BV
- Published
- 2002-06
- Volume
- 5
- Issue
- 3-4
- Pages
- 119-125
- ISSN
- 1368-7646 (ISSN-L)
- OpenAlex
- W1970691146
- Cited by
- 143
- References
- 42
- Citations by year
- 2026: 4 · 2025: 6 · 2024: 5 · 2023: 3 · 2022: 5 · 2021: 4 · 2020: 7 · 2019: 3 · 2018: 3 · 2017: 2 · 2016: 7 · 2015: 5 · 2014: 6 · 2013: 8 · 2012: 9
- FWCI
- 3.50
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Drug Resistance Updates (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Health Sciences › Medicine › Microbiology (medical) › Antibiotic Resistance in Bacteria
- Health Sciences › Medicine › Infectious Diseases › Antimicrobial Resistance in Staphylococcus
- Health Sciences › Medicine › Pharmacology (medical) › Antibiotics Pharmacokinetics and Efficacy
- Keywords
- tetracycline, glycylcyclines, tigecycline, antibiotic resistance, efflux pumps, multidrug resistance, Gram-positive bacteria, combination therapy
- MeSH terms
- Tigecycline, Humans, Microbial Sensitivity Tests, Minocycline, Structure-Activity Relationship, Tetracycline Resistance, Tetracyclines
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