Synthesis and Pharmacological Evaluation of a Novel Peptide Based on Anemonia sulcata BDS-I Toxin as a New K_V3.4 Inhibitor Exerting a Neuroprotective Effect Against Amyloid-β Peptide.

ABSTRACT: There is increasing evidence that the fast-inactivating potassium current I_A, encoded by K_V3. 4 channels, plays an important role in Alzheimer's Disease (AD), since the neurotoxic β-amyloid peptide1-42 (Aβ_1-42) increases the I_A current triggering apoptotic processes. The specific inhibition of K_V3.4 by the marine toxin extracted from Anemonia sulcata, named blood depressing substance-I (BDS-I), reverts the Aβ peptide-induced cell death. The aim of the present study was to identify the smallest fragments of BDS-I, obtained by peptide synthesis, able to inhibit K_V3.4 currents. For this purpose, whole-cell patch clamp technique was used to evaluate the effects of BDS-I fragments on K_V3.4 currents in CHO cells

SUBMITTER: Ciccone R 

PROVIDER: S-EPMC6629785 | biostudies-literature | 2019

REPOSITORIES: biostudies-literature