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Plasmodium vivax

Help on GtoMPdb Target Species Data

The GtoMPdb includes species information for antimalarial ligands and their target interactions.

Each individual Malaria Target Species page provides a detailed description of the species and a table displaying all interactions (contained in the database) associated with it.

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Species ID:104
Name:Plasmodium vivax
Associated with:3 targets
6 ligands
Description
P. vivax (Pv) is one of five protozoan parasite species of the genus Plasmodium that cause malaria in humans. Pv is the second most common cause of malaria in humans, after P. falciparum, and is prevalent in Southeast Asia and Latin America. Pv has a dormant liver stage that can reactivate and lead to clinical symptoms.

Interactions

Interactions
Key to terms and symbols Click column headers to sort
Target Ligand Sp. Action Value Parameter Reference
Plasmodium falciparum dihydroorotate dehydrogenase DSM265 Pv

Plasmodium vivax

P. vivax (Pv) is one of five protozoan parasite species of the genus Plasmodium that cause malaria in humans. Pv is the second most common cause of malaria in humans, after P. falciparum, and is prevalent in Southeast Asia and Latin America. Pv has a dormant liver stage that can reactivate and lead to clinical symptoms.
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 Inhibition 7.1 pIC50 2
pIC50 7.1 (IC50 7.2x10-8 M) [2]
Description: Steady-state kinetic analysis.
Plasmodium falciparum dihydroorotate dehydrogenase DSM421 Pv

Plasmodium vivax

P. vivax (Pv) is one of five protozoan parasite species of the genus Plasmodium that cause malaria in humans. Pv is the second most common cause of malaria in humans, after P. falciparum, and is prevalent in Southeast Asia and Latin America. Pv has a dormant liver stage that can reactivate and lead to clinical symptoms.
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 - 6.7 pEC50 4
pEC50 6.7 (EC50 1.8x10-7 M) [4]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Description: Blood-stage: schizont maturation assay using P. vivax field isolates.
Plasmodium falciparum dihydroorotate dehydrogenase DSM421 Pv

Plasmodium vivax

P. vivax (Pv) is one of five protozoan parasite species of the genus Plasmodium that cause malaria in humans. Pv is the second most common cause of malaria in humans, after P. falciparum, and is prevalent in Southeast Asia and Latin America. Pv has a dormant liver stage that can reactivate and lead to clinical symptoms.
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 Inhibition 7.0 pIC50 4
pIC50 7.0 (IC50 9.4x10-8 M) [4]
Description: Steady-state kinetic analysis of recombinant enzyme inhibition.
Plasmodium falciparum dihydroorotate dehydrogenase DSM502 Pv

Plasmodium vivax

P. vivax (Pv) is one of five protozoan parasite species of the genus Plasmodium that cause malaria in humans. Pv is the second most common cause of malaria in humans, after P. falciparum, and is prevalent in Southeast Asia and Latin America. Pv has a dormant liver stage that can reactivate and lead to clinical symptoms.
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 Inhibition 7.8 pIC50 2
pIC50 7.8 (IC50 1.4x10-8 M) [2]
Description: Steady-state kinetic analysis.
Plasmodium falciparum dihydroorotate dehydrogenase DSM705 Pv

Plasmodium vivax

P. vivax (Pv) is one of five protozoan parasite species of the genus Plasmodium that cause malaria in humans. Pv is the second most common cause of malaria in humans, after P. falciparum, and is prevalent in Southeast Asia and Latin America. Pv has a dormant liver stage that can reactivate and lead to clinical symptoms.
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 Inhibition 7.3 pIC50 3
pIC50 7.3 (IC50 5.2x10-8 M) [3]
Description: Steady-state kinetic analysis.
Plasmodium falciparum bifunctional dihydrofolate reductase-thymidylate synthase P218 Pv

Plasmodium vivax

P. vivax (Pv) is one of five protozoan parasite species of the genus Plasmodium that cause malaria in humans. Pv is the second most common cause of malaria in humans, after P. falciparum, and is prevalent in Southeast Asia and Latin America. Pv has a dormant liver stage that can reactivate and lead to clinical symptoms.
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 - 7.3 pEC50 5
pEC50 7.3 (EC50 4.5x10-8 M) Primary human hepatocyte assay to assess inhibition of hepatic schizonts (prophylactic activity) [5]
Lifecycle stages: Plasmodium liver stage (sporozoite, hepatic schizont, hepatic merozoite)
Description: Parasite liver stage assay
Plasmodium falciparum lysyl-tRNA synthetase compound 5 [PMID: 30894487] Pv

Plasmodium vivax

P. vivax (Pv) is one of five protozoan parasite species of the genus Plasmodium that cause malaria in humans. Pv is the second most common cause of malaria in humans, after P. falciparum, and is prevalent in Southeast Asia and Latin America. Pv has a dormant liver stage that can reactivate and lead to clinical symptoms.
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 - 6.0 pEC50 1
pEC50 6.0 (EC50 9.5x10-7 M) [1]
Lifecycle stages: Plasmodium liver stage (sporozoite, hepatic schizont, hepatic merozoite)
Description: Parasite liver stage assay

References

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1. Baragaña B, Forte B, Choi R, Nakazawa Hewitt S, Bueren-Calabuig JA, Pisco JP, Peet C, Dranow DM, Robinson DA, Jansen C et al.. (2019) Lysyl-tRNA synthetase as a drug target in malaria and cryptosporidiosis. Proc Natl Acad Sci USA, 116 (14): 7015-7020. [PMID:30894487]

2. Kokkonda S, Deng X, White KL, El Mazouni F, White J, Shackleford DM, Katneni K, Chiu FCK, Barker H, McLaren J et al.. (2020) Lead Optimization of a Pyrrole-Based Dihydroorotate Dehydrogenase Inhibitor Series for the Treatment of Malaria. J Med Chem, 63 (9): 4929-4956. [PMID:32248693]

3. Palmer MJ, Deng X, Watts S, Krilov G, Gerasyuto A, Kokkonda S, El Mazouni F, White J, White KL, Striepen J et al.. (2021) Potent Antimalarials with Development Potential Identified by Structure-Guided Computational Optimization of a Pyrrole-Based Dihydroorotate Dehydrogenase Inhibitor Series. J Med Chem, 64 (9): 6085-6136. [PMID:33876936]

4. Phillips MA, White KL, Kokkonda S, Deng X, White J, El Mazouni F, Marsh K, Tomchick DR, Manjalanagara K, Rudra KR et al.. (2016) A Triazolopyrimidine-Based Dihydroorotate Dehydrogenase Inhibitor with Improved Drug-like Properties for Treatment and Prevention of Malaria. ACS Infect Dis, 2 (12): 945-957. [PMID:27641613]

5. Roth A, Maher SP, Conway AJ, Ubalee R, Chaumeau V, Andolina C, Kaba SA, Vantaux A, Bakowski MA, Thomson-Luque R et al.. (2018) A comprehensive model for assessment of liver stage therapies targeting Plasmodium vivax and Plasmodium falciparum. Nat Commun, 9 (1): 1837. [PMID:29743474]