Preliminary LC-MS Based Screening for Inhibitors of Plasmodium falciparum Thioredoxin Reductase (PfTrxR) among a Set of Antimalarials from the Malaria Box

Author： Tiwari Neil K.   Reynolds Priscilla J.   Calderón Angela I.  

Publisher： MDPI

E-ISSN： 1420-3049|21|4|424-424

ISSN： 1420-3049

Source： Molecules, Vol.21, Iss.4, 2016-03, pp. : 424-424

Access to resources Favorite

Disclaimer: Any content in publications that violate the sovereignty, the constitution or regulations of the PRC is not accepted or approved by CNPIEC.

Previous Menu Next

Abstract

Plasmodium falciparum thioredoxin reductase (PfTrxR) has been identified as a potential drug target to combat growing antimalarial drug resistance. Medicines for Malaria Venture (MMV) has pre-screened and identified a set of 400 antimalarial compounds called the Malaria Box. From those, we have evaluated their mechanisms of action through inhibition of PfTrxR and found new active chemical scaffolds. Five compounds with significant PfTrxR inhibitory activity, with IC50 values ranging from 0.9–7.5 µM against the target enzyme, were found out of the Malaria Box.

Related content

Blocking Plasmodium falciparum Malaria Transmission with Drugs: The Gametocytocidal and Sporontocidal Properties of Current and Prospective Antimalarials

By Kiszewski Anthony E.  

Pharmaceuticals, Vol. 4, Iss. 1, 2010-12 ,pp. : 44-68 (25)

MDPI

Access to resources Recommend Favorite

Design and Synthesis of Chalcone Derivatives as Inhibitors of the Ferredoxin — Ferredoxin-NADP+ Reductase Interaction of Plasmodium falciparum: Pursuing New Antimalarial Agents

By Suwito Hery   Jumina Pratiwi   Mustofa Much Zaenal   Pudjiastuti Yoko   Fanani Ritsuko   Kimata-Ariga Toru   Katahira Toshimichi   Kawakami Toshiharu   Fujiwara Hasnah   Hase Ni Nyoman Tri   Mohd Sirat Derek J.   Puspaningsih Hery  

Molecules, Vol. 19, Iss. 12, 2014-12 ,pp. : 21473-21488 (16)

MDPI

Access to resources Recommend Favorite

Isolation of α-Amylase Inhibitors from Kadsura longipedunculata Using a High-Speed Counter-Current Chromatography Target Guided by Centrifugal Ultrafiltration with LC-MS

By Cen Yin   Xiao Aiping   Chen Xiaoqing   Liu Liangliang  

Molecules, Vol. 21, Iss. 9, 2016-09 ,pp. : 1190-1190 (1)

MDPI

Access to resources Recommend Favorite

In-Depth Two-Year Study of Phenolic Profile Variability among Olive Oils from Autochthonous and Mediterranean Varieties in Morocco, as Revealed by a LC-MS Chemometric Profiling Approach

By Bajoub Aadil   Medina-Rodríguez Santiago   Olmo-García Lucía   Ajal El Amine   Monasterio Romina P.   Hanine Hafida   Fernández-Gutiérrez Alberto   Carrasco-Pancorbo Alegría  

International Journal of Molecular Sciences, Vol. 18, Iss. 1, 2016-12 ,pp. : 52-52 (1)

MDPI

Access to resources Recommend Favorite

Beta-N-methylamino-l-alanine: LC-MS/MS Optimization, Screening of Cyanobacterial Strains and Occurrence in Shellfish from Thau, a French Mediterranean Lagoon

By Réveillon Damien   Abadie Eric   Séchet Véronique   Brient Luc   Savar Véronique   Bardouil Michèle   Hess Philipp   Amzil Zouher  

Marine Drugs, Vol. 12, Iss. 11, 2014-11 ,pp. : 5441-5467 (27)

MDPI

Access to resources Recommend Favorite