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Please use this identifier to cite or link to this item: http://repository.li.mahidol.ac.th/dspace/handle/123456789/41890
Title: Hundreds of dual-stage antimalarial molecules discovered by a functional gametocyte screen
Authors: Celia Miguel-Blanco
Irene Molina
Ana I. Bardera
Beatriz Díaz
Laura De Las Heras
Sonia Lozano
Carolina González
Janneth Rodrigues
Michael J. Delves
Andrea Ruecker
Gonzalo Colmenarejo
Sara Viera
María S. Martínez-Martínez
Esther Fernández
Jake Baum
Robert E. Sinden
Esperanza Herreros
GlaxoSmithKline plc, Spain
Imperial College London
Mahidol University
Nuffield Department of Clinical Medicine
Keywords: Biochemistry, Genetics and Molecular Biology;Chemistry
Issue Date: 17-May-2017
Citation: Nature Communications. Vol.8, (2017)
Abstract: © The Author(s) 2017. Plasmodium falciparum stage V gametocytes are responsible for parasite transmission, and drugs targeting this stage are needed to support malaria elimination. We here screen the Tres Cantos Antimalarial Set (TCAMS) using the previously developed P. falciparum female gametocyte activation assay (Pf FGAA), which assesses stage V female gametocyte viability and functionality using Pfs25 expression. We identify over 400 compounds with activities <2 μM, chemically classified into 57 clusters and 33 singletons. Up to 68% of the hits are chemotypes described for the first time as late-stage gametocyte-targeting molecules. In addition, the biological profile of 90 compounds representing the chemical diversity is assessed. We confirm in vitro transmission-blocking activity of four of the six selected molecules belonging to three distinct scaffold clusters. Overall, this TCAMS gametocyte screen provides 276 promising antimalarial molecules with dual asexual/sexual activity, representing starting points for target identification and candidate selection.
URI: https://www.scopus.com/inward/record.uri?partnerID=HzOxMe3b&scp=85019859594&origin=inward
http://repository.li.mahidol.ac.th/dspace/handle/123456789/41890
ISSN: 20411723
Appears in Collections:Scopus 2016-2017

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