Publications by authors named "B V Krylov"
Article Synopsis
- - The study explores how the compound Ac-Lys-Lys-Lys-NH (Ac-KKK-NH) binds to the Na1.8 channel, which plays a key role in encoding pain signals in the peripheral nervous system, using both experimental and theoretical techniques.
- - Experimental results show that when Ac-KKK-NH is applied at a concentration of 100 nM, it significantly reduces the effective charge of the Na1.8 channel's activation gating, and it exhibits strong analgesic effects in pain tests conducted in live animals.
- - Conformational analysis reveals that the distances between positively charged groups in Ac-KKK-NH are 11-12 Å, and docking studies identify its binding site on the voltage-sensing
The present work continues our recent series of articles that aim to elucidate the ligand-receptor binding mechanism of short cationic peptides to the Na1.8 channel in the nociceptive neuron. The applied methodological approach has involved several methods: the patch-clamp experimental evaluation of the effective charge of the Na1.
View Article and Find Full Text PDFThe signaling or non-pumping Na,K-ATPase function was first observed by us in the nociceptive neuron; Na,K-ATPase transduced the signals from the opioid-like receptors to Na1.8 channels. This study elucidates the role of the rhamnosyl residue of ouabain in the activation of the Na,K-ATPase signaling function.
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- This study aimed to assess how magnesium-L-threonate (L-TAMS) affects the pain relief from opioids in advanced cancer patients who are already using opioids for pain management.
- A clinical trial was conducted with 83 cancer patients randomly assigned to receive either L-TAMS or a placebo, measuring the changes in their daily morphine doses over time.
- Results showed that patients taking L-TAMS needed less morphine over 90 days compared to those on the placebo, indicating better pain relief and less opioid-related side effects, like constipation.
Role of the Guanidinium Groups in Ligand-Receptor Binding of Arginine-Containing Short Peptides to the Slow Sodium Channel: Quantitative Approach to Drug Design of Peptide Analgesics.
Int J Mol Sci
September 2022
Several arginine-containing short peptides have been shown by the patch-clamp method to effectively modulate the Na1.8 channel activation gating system, which makes them promising candidates for the role of a novel analgesic medicinal substance. As demonstrated by the organotypic tissue culture method, all active and inactive peptides studied do not trigger the downstream signaling cascades controlling neurite outgrowth and should not be expected to evoke adverse side effects on the tissue level upon their medicinal administration.
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