NDLI: Aminoglycoside block of P2X2 receptors heterologously expressed in Xenopus laevis oocytes

Content Provider	Springer Nature Link
Author	Bongartz, Eva Verena Rettinger, Jürgen Hausmann, Ralf
Copyright Year	2010
Abstract	Aminoglycosides are polycationic antibiotics that have been shown to block a variety of cation channels. The inhibitory effect of externally applied aminoglycosides on P2X2 receptor currents was examined after heterologous expression in Xenopus laevis oocytes using the two-electrode voltage-clamp technique. All of the aminoglycosides tested inhibited the ATP-evoked responses with potencies ranging from 71 μM to 2 mM (IC$_{50}$ values). The ranked order of potency was streptomycin > gentamicin > neomycin > paromomycin > kanamycin. The inhibition of P2X receptor currents was independent of the ATP concentration used for the activation, which is compatible with a noncompetitive mechanism. The inhibition was voltage-dependent and was reduced at more positive membrane potentials. To examine whether the current block was dependent on the receptor conformation, the aminoglycoside effect on a non-desensitizing P2X2-X1 receptor chimera was analyzed. The results from these measurements suggest that inhibition is caused by an open pore block that locks the P2X receptor chimera in an open nonconducting state from which the agonist dissociation is slow. We also demonstrate that the P2X2-X1 chimera can serve as a tool to directly test whether an antagonist acts competitively or not.
Starting Page	393
Ending Page	403
Page Count	11
File Format	PDF
ISSN	15739538
Journal	Purinergic Signalling
Volume Number	6
Issue Number	4
e-ISSN	15739546
Language	English
Publisher	Springer Netherlands
Publisher Date	2010-11-16
Publisher Institution	International Purine Club
Publisher Place	Dordrecht
Access Restriction	One Nation One Subscription (ONOS)
Subject Keyword	Aminoglycoside antibiotics P2X Xenopus oocytes Open pore block Cancer Research Neurosciences Human Physiology Pharmacology/Toxicology Biomedicine general
Content Type	Text
Resource Type	Article
Subject	Cell Biology Molecular Biology Cellular and Molecular Neuroscience

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