An ability of polypeptide PP-14 to modulate the excitability of nociceptive neuron membrane was investigated by patch-
clamp method. The agent was demonstrated to decrease the voltage sensitivity of slow sodium channels NaV1.8, responsible
for nociceptive signal coding. Extracellular application of PP-14 induced a significant decrease in the effective charge
transfer (Zeff) of the activation gating machinery of NaV1.8 channels, which indicates that the polypeptide may produce
analgesia. Nevertheless, the effect of PP-14 is less pronounced as compared to a sharp decrease in nociceptive neuron
excitability induced by a more complex molecule of defensin NP-1 applied at subnanomolar concentrations. Quantum-
chemical analysis of PP-14 and NP-1 steric structures made it possible to account for the relative efficacy of ligand-
receptor binding of these polypeptides.
Key words:
nociception, patch-clamp method, slow sodium channels, polypeptides, quantum-chemical calculations
Cite:
Plakhova V. B., Rogachevsky I. V., Shelykh Т. N., Podzorova S. A., Krylov B. V.
Tsiklicheskii polipeptid pp-14 moduliruet potentsialochuvstvitelnost medlennykh natrievykh kanalov
[Cyclic polypeptide pp-14 modulates the voltage sensitivity of slow sodium channels].
Sensornye sistemy [Sensory systems].
2016.
V. 30(3).
P. 234-240 (in Russian).
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