CKI-7-Bound Structures of Two APH Enzymes
2011
Crystal Structures of Two Aminoglycoside Kinases with a Protein Kinase Inhibitor
publication
10 minutes
Evidence: moderate
Author Information
Author(s): Fong Desiree H., Xiong Bing, Hwang Jiyoung, Berghuis Albert M.
Primary Institution: McGill University
Hypothesis
Can CKI-7 inhibit aminoglycoside-modifying enzymes to combat antibiotic resistance?
Conclusion
The study shows that CKI-7 can inhibit two aminoglycoside kinases, providing a basis for developing inhibitors to combat antibiotic resistance.
Supporting Evidence
- CKI-7 was found to inhibit APH(9)-Ia in a competitive manner.
- The study provides the first structures of a eukaryotic protein kinase inhibitor in complex with bacterial kinases.
- CKI-7 binds to the nucleotide-binding pocket of the enzymes.
Takeaway
Scientists found a way to use a special drug to help antibiotics work better against bacteria that are usually resistant.
Methodology
The researchers determined the crystal structures of two aminoglycoside kinases in complex with the inhibitor CKI-7.
Limitations
The inhibitors were only effective in vitro and may not work in all bacterial strains.
Digital Object Identifier (DOI)
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