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Review
. 2007 Aug;11(4):440-5.
doi: 10.1016/j.cbpa.2007.05.038.

Drug discovery for malaria: a very challenging and timely endeavor

Michael H Gelb  1
Affiliations
Review

Drug discovery for malaria: a very challenging and timely endeavor

Michael H Gelb. Curr Opin Chem Biol. 2007 Aug.

Abstract

The prevalence of resistance to known antimalarial drugs has resulted in the expansion of antimalarial drug discovery efforts. Academic and nonprofit institutions are partnering with the pharmaceutical industry to develop new antimalarial drugs. Several new antimalarial agents are undergoing clinical trials, mainly those resurrected from previous antimalarial drug discovery programs. Novel antimalarials are being advanced through the drug development process, of course, with the anticipated high failure rate typical of drug discovery. Many of these are summarized in this review. Mechanisms for funding antimalarial drug discovery and genomic information to aid drug target selection have never been better. It remains to be seen whether ongoing efforts will be sufficient for reducing malaria burden in the developing world.

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Figures

Figure 1
Figure 1
Structure of anti-malarial agents. See text for further discussion.
Figure 2
Figure 2
Proposed mechanism for heme iron-catalyzed generation of a carbon-centered radical from the anti-malarial agent OZ277. The carbon-centered radical is proposed to alkylate a number of parasite proteins. See text for further discussion.
Figure 3
Figure 3
Generation of the active anti-malarial agent T3 from the pro-drug TE3. See text for further discussion.
See this image and copyright information in PMC

References

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