Cover image for Vol. 11 Issue 20

Editorial Board Chairs: Antonello Mai, Rainer Metternich. Assoc. Editors: David Peralta, Scott Williams (Sr)

Impact Factor: 2.98

ISI Journal Citation Reports © Ranking: 2015: 18/59 (Chemistry Medicinal); 76/253 (Pharmacology & Pharmacy)

Online ISSN: 1860-7187

Associated Title(s): Angewandte Chemie International Edition, Chemistry - A European Journal, Chemistry – An Asian Journal, ChemBioChem, Medicinal Research Reviews, Molecular Informatics

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October 19, 2016

ACT-451840: An Antimalarial Drug with a Novel Mechanism of Action

ACT-451840: An Antimalarial Drug with a Novel Mechanism of Action

Malaria remains one of the most significant health burdens in poorer parts of the world. With the recent emergence of initial signs of parasites resistant to artemisinine combination therapy, and in the absence of effective malaria vaccines, the quest for antimalarials with different mechanisms of action has gained increased importance.

Industry–university collaborative efforts led by Christoph Boss (Actelion Pharamceuticals Ltd.) and Sergio Wittlin (Swiss Tropical and Public Health Institute) toward the identification of an antimalarial drug with a novel mechanism of action resulted in the identification of ACT-451840, which was investigated in clinical trials.

Read the recent Actelion press release as well as our news article; the full paper can be found here: 10.1002/cmdc.201600298.

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    Version of Record online: 25 OCT 2016 | DOI: 10.1002/cmdc.201600463

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    Clarity in Retro-spect: Both oligonucleotides (red ribbons) and toxins (orange squares) enter cells by endocytosis and traffic to early endosomes (EE). Oligos traffic to late endosomes (LE) and thence to lysosomes (LY), where they are degraded. Toxins traffic via the Retromer complex (R) to the trans Golgi (TG) to become active. Retro-1 blocks toxin trafficking and also releases oligos from late endosomes.

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