TY - JOUR
T1 - Global phenotypic screening for antimalarials
AU - Guiguemde, W. Armand
AU - Shelat, Anang A.
AU - Garcia-Bustos, Jose F.
AU - Diagana, Thierry T.
AU - Gamo, Francisco Javier
AU - Guy, R. Kiplin
PY - 2012/1/27
Y1 - 2012/1/27
N2 - Malaria, a devastating infectious disease caused by Plasmodium spp., leads to roughly 655,000 deaths per year, mostly of African children. To compound the problem, drug resistance has emerged to all classical antimalarials and may be emerging for artemisinin-based combination therapies. To address the need for new antimalarials with novel mechanisms, several groups carried out phenotypic screening campaigns to identify compounds inhibiting growth of the blood stages of Plasmodium falciparum. In this review, we describe the characterization of these compounds, explore currently ongoing strategies to develop lead molecules, and endorse the concept of a "malaria box" of publicly accessible active compounds.
AB - Malaria, a devastating infectious disease caused by Plasmodium spp., leads to roughly 655,000 deaths per year, mostly of African children. To compound the problem, drug resistance has emerged to all classical antimalarials and may be emerging for artemisinin-based combination therapies. To address the need for new antimalarials with novel mechanisms, several groups carried out phenotypic screening campaigns to identify compounds inhibiting growth of the blood stages of Plasmodium falciparum. In this review, we describe the characterization of these compounds, explore currently ongoing strategies to develop lead molecules, and endorse the concept of a "malaria box" of publicly accessible active compounds.
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U2 - 10.1016/j.chembiol.2012.01.004
DO - 10.1016/j.chembiol.2012.01.004
M3 - Review article
C2 - 22284359
AN - SCOPUS:84856367163
SN - 1074-5521
VL - 19
SP - 116
EP - 129
JO - Chemistry and Biology
JF - Chemistry and Biology
IS - 1
ER -