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Imaging of Plasmodium Liver Stages to Drive Next-Generation Antimalarial Drug Discovery

by Zhou, Bin , Gordon, Perry , Groessl, Todd , Plouffe, David M. , Roland, Jason , Gettayacamin, Montip , Mazier, Dominique , Fidock, David A. , Kuhen, Kelli L. , Winzeler, Elizabeth A. , Sattabongkot, Jetsumon , Schultz, Peter G. , Dharia, Neekesh V. , Bopp, Selina E. , Chatterjee, Arnab , Che, Jianwei , Diagana, Thierry T. , Kato, Nobutaka , McNamara, Case W. , Bright, A. Taylor , Richmond, Wendy , Zhou, Yingyao , Meister, Stephan , Nagle, Advait , Borboa, Rachel , Tuntland, Tove , Cohen, Steve , Bonamy, Ghislain M. C. , Nam, Tae-gyu , Gagaring, Kerstin , Lee, Marcus C. S. , Wu, Tao , Rottmann, Matthias , Froissard, Patrick , Glynne, Richard J. , Barnes, S. Whitney , Walker, John R.

in animal models / Animals / Antibiotics. Antiinfectious agents. Antiparasitic agents / Antimalarials / Antimalarials - chemistry / Antimalarials - pharmacokinetics / Antimalarials - pharmacology / Antimalarials - therapeutic use / Biological and medical sciences / Blood / Cell Line, Tumor / Chemicals / Dominant species / Drug Discovery / Drug Evaluation, Preclinical / Drug Resistance / Drug therapy / drugs / erythrocytes / Erythrocytes - parasitology / General pharmacology / Humans / image analysis / Imidazoles - chemistry / Imidazoles - pharmacokinetics / Imidazoles - pharmacology / Imidazoles - therapeutic use / Infections / Inhibitory concentration 50 / Liver / Liver - parasitology / Malaria / Malaria - drug therapy / Malaria - parasitology / Malaria - prevention & control / Medical sciences / Mice / Mice, Inbred BALB C / Molecular Structure / Narcotics / Parasites / Pharmaceutical technology. Pharmaceutical industry / Pharmacology. Drug treatments / Piperazines - chemistry / Piperazines - pharmacokinetics / Piperazines - pharmacology / Piperazines - therapeutic use / Plasmodium / Plasmodium - cytology / Plasmodium - drug effects / Plasmodium - growth & development / Plasmodium - physiology / Plasmodium berghei - cytology / Plasmodium berghei - drug effects / Plasmodium berghei - growth & development / Plasmodium berghei - physiology / Plasmodium falciparum - cytology / Plasmodium falciparum - drug effects / Plasmodium falciparum - growth & development / Plasmodium falciparum - physiology / Plasmodium yoelii - cytology / Plasmodium yoelii - drug effects / Plasmodium yoelii - growth & development / Plasmodium yoelii - physiology / Polymorphism, Single Nucleotide / Protozoan Proteins - chemistry / Protozoan Proteins - genetics / Protozoan Proteins - metabolism / Random Allocation / researchers / Scaffolds / Schizonts / Small Molecule Libraries / Sporozoites - drug effects / Sporozoites - growth & development / Vector-borne diseases

2011

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Imaging of Plasmodium Liver Stages to Drive Next-Generation Antimalarial Drug Discovery

2011

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Imaging of Plasmodium Liver Stages to Drive Next-Generation Antimalarial Drug Discovery

2011

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Journal Article

Imaging of Plasmodium Liver Stages to Drive Next-Generation Antimalarial Drug Discovery

Zhou, Bin,

Gordon, Perry,

Groessl, Todd,

Plouffe, David M.,

Roland, Jason,

Gettayacamin, Montip,

Mazier, Dominique,

Fidock, David A.,

Kuhen, Kelli L.,

Winzeler, Elizabeth A.,

Sattabongkot, Jetsumon,

Schultz, Peter G.,

Dharia, Neekesh V.,

Bopp, Selina E.,

Chatterjee, Arnab,

Che, Jianwei,

Diagana, Thierry T.,

Kato, Nobutaka,

McNamara, Case W.,

Bright, A. Taylor,

Richmond, Wendy,

Zhou, Yingyao,

Meister, Stephan,

Nagle, Advait,

Borboa, Rachel,

Tuntland, Tove,

Cohen, Steve,

Bonamy, Ghislain M. C.,

Nam, Tae-gyu,

Gagaring, Kerstin,

Lee, Marcus C. S.,

Wu, Tao,

Rottmann, Matthias,

Froissard, Patrick,

Glynne, Richard J.,

Barnes, S. Whitney,

Walker, John R.

2011

Overview

Most malaria drug development focuses on parasite stages detected in red blood cells, even though, to achieve eradication, next-generation drugs active against both erythrocytic and exo-erythrocytic forms would be preferable. We applied a multifactorial approach to a set of > 4000 commercially available compounds with previously demonstrated blood-stage activity (median inhibitory concentration < 1 micromolar) and identified chemical scaffolds with potent activity against both forms. From this screen, we identified an imidazolopiperazine scaffold series that was highly enriched among compounds active against Plasmodium liver stages. The orally bioavailable lead imidazolopiperazine confers complete causal prophylactic protection (15 milligrams/kilogram) in rodent models of malaria and shows potent in vivo blood-stage therapeutic activity. The open-source chemical tools resulting from our effort provide starting points for future drug discovery programs, as well as opportunities for researchers to investigate the biology of exo-erythrocytic forms.

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Publisher

American Association for the Advancement of Science,The American Association for the Advancement of Science

Subject

animal models

/ Animals

/ Antibiotics. Antiinfectious agents. Antiparasitic agents

/ Antimalarials

/ Antimalarials - chemistry

/ Antimalarials - pharmacokinetics

/ Antimalarials - pharmacology