The Cyclooctadepsipeptide Anthelmintic Emodepside Differentially Modulates Nematode, Insect and Human Calcium-Activated Potassium (SLO) Channel Alpha Subunits

• Published in: PLoS neglected tropical diseases Vol. 9; no. 10; p. e0004062
• Main Authors: Crisford, Anna, Ebbinghaus-Kintscher, Ulrich, Schoenhense, Eva, Harder, Achim, Raming, Klaus, O’Kelly, Ita, Ndukwe, Kelechi, O’Connor, Vincent, Walker, Robert J., Holden-Dye, Lindy
• Format: Journal Article
• Language: English
• Published: United States Public Library of Science 01.10.2015; Public Library of Science (PLoS)
• Subjects: Animals; Anthelmintics - pharmacology; Calcium; Calcium - metabolism; Care and treatment; CHO Cells; Colleges & universities; Cricetulus; Depsipeptides - pharmacology; Drosophila melanogaster; Health aspects; HEK293 Cells; Humans; Insects; Investigations; Kinases; Large-Conductance Calcium-Activated Potassium Channel alpha Subunits - antagonists & inhibitors; Large-Conductance Calcium-Activated Potassium Channel alpha Subunits - drug effects; Nematoda; Nematodes; Protein Subunits; Risk factors; Roundworm infections; California

The anthelmintic emodepside paralyses adult filarial worms, via a mode of action distinct from previous anthelmintics and has recently garnered interest as a new treatment for onchocerciasis. Whole organism data suggest its anthelmintic action is underpinned by a selective activation of the nematode...