MEET THE GUEST EDITOR [Hot Topic: Modern Omics-Based Platform for High Throughput Screening for Novel Drug Targets (Part 2) (Guest Editor: Canhua Huang)]

2012 ◽  
Vol 15 (4) ◽  
pp. 338-338
Author(s):  
Canhua Huang
2018 ◽  
Author(s):  
Priscilla Wander ◽  
Sandra S. Pinhanços ◽  
Bianca Koopmans ◽  
M. Emmy M. Dolman ◽  
Pauline Schneider ◽  
...  

2010 ◽  
Vol 185 (2) ◽  
pp. 204-212 ◽  
Author(s):  
Nikhil G. Thaker ◽  
Peter R. McDonald ◽  
Fang Zhang ◽  
Carolyn A. Kitchens ◽  
Tong Ying Shun ◽  
...  

2016 ◽  
pp. AAC.00218-16 ◽  
Author(s):  
Thomas E. Kraft ◽  
Monique R. Heitmeier ◽  
Marina Putanko ◽  
Rachel L. Edwards ◽  
Ma. Xenia G. Ilagan ◽  
...  

The glucose transporter PfHT is essential to the survival of the malaria parasitePlasmodium falciparumand has been shown to be a druggable target with high potential for pharmacological intervention. Identification of compounds against novel drug targets is crucial to combating resistance against current therapeutics. Here, we describe the development of a cell-based assay system readily adaptable to high-throughput screening that directly measures compound effects on PfHT-mediated glucose transport. Intracellular glucose concentrations are detected using a genetically encoded fluorescence resonance energy transfer (FRET)-based glucose-sensor. This allows assessment of the ability of small molecules to inhibit glucose uptake with high accuracy (Z'-factor of >0.8), thereby eliminating the need for radiolabeled substrates. Furthermore, we have adapted this assay to counter screen PfHT hits against the human orthologues GLUT1, 2, 3 and 4. We report the identification of several hits after screening the Medicines for Malaria Venture (MMV) Malaria Box, a library of 400 compounds known to inhibit erythrocytic development ofP. falciparum. Hit compounds were characterized by determining the half-maximal inhibitory concentration (IC50) for the uptake of radiolabeled glucose into isolatedP. falciparumparasites. One of our hits, compound MMV009085, shows high potency and ortholog selectivity, thereby successfully validating our assay for anti-malarial screening.


2004 ◽  
Vol 10 (4) ◽  
pp. 1241-1249 ◽  
Author(s):  
Carsten Müller-Tidow ◽  
Joachim Schwäble ◽  
Björn Steffen ◽  
Nicola Tidow ◽  
Burkhardt Brandt ◽  
...  

2020 ◽  
Vol 19 (5) ◽  
pp. 300-300 ◽  
Author(s):  
Sorin Avram ◽  
Liliana Halip ◽  
Ramona Curpan ◽  
Tudor I. Oprea

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