Gentamicin Binds to Megalin as a Competitive Inhibitor Using the Common Ligand Binding Motif of Complement Type Repeats* Insight from the NMR structure of the 10 complement type repeat domain alone and in complex with gentamicin
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چکیده
Background: Gentamicin causes nephrotoxicity and ototoxicity using megalin as a key cellular uptake-site, but no structural data are available Results: Gentamicin binds to megalin with low affinity and exploits the common ligand binding motif Conclusion: This first structure of human megalin in complex with gentamicin suggest electrostatics to be the main binding determinant Significance: Structure-based design of gentamicin antagonists may now possible.
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تاریخ انتشار 2012