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Plasmodium falciparum acetyl-CoA synthetase

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Target id: 3174

Nomenclature: Plasmodium falciparum acetyl-CoA synthetase

Abbreviated Name: PfACS

Family: Other antimalarial targets

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Plasmodium falciparum 3D7 - 997 ACAS acetyl-CoA synthetase
Previous and Unofficial Names Click here for help
ACAS | Pf3D7_06_v3:1,113,448..1,117,623(-) | PFF1350c | AcAS
Database Links Click here for help
Alphafold C6KTB4 (Pf3D7)
PlasmoDB PF3D7_0627800 (Pf3D7)
UniProtKB C6KTB4 (Pf3D7)
Whole Organism Assay Data Linked to This Target
Key to terms and symbols Click column headers to sort
Ligand Sp. Assay description Type Action Value Parameter Reference
MMV693183 Small molecule or natural product Guide to Malaria Pharmacology Ligand PfNF54

Plasmodium falciparum NF54

P. falciparum strain NF54 (PfNF54) was derived from a patient who had never left the Netherlands.
PfNF54 can be obtained from the European Malaria Reagent Repository or the Malaria Research and Reference Reagent Resource Center (MR4) and is sensitive to a panel of antimalarial compounds including chloroquine and pyrimethamine.
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 Parasite growth inhibition assay - - 8.6 pIC50 4
⤷ pIC50 8.6 (IC50 2.4x10-9 M) SYBR Green incorporation (72h assay) [4]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
MMV693183 Small molecule or natural product Guide to Malaria Pharmacology Ligand Pf

Plasmodium falciparum

P. falciparum (Pf) is one of five protozoan parasite species of the genus Plasmodium that cause malaria in humans. Pf is responsible for the majority of malaria related deaths and is the most prevalent species in sub-Saharan Africa.
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 Parasite growth inhibition assay - - 8.6 pIC50 1
⤷ pIC50 8.6 (IC50 2.5x10-9 M) SYBR Green assay [1]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
MMV689258 Small molecule or natural product Guide to Malaria Pharmacology Ligand Pf

Plasmodium falciparum

P. falciparum (Pf) is one of five protozoan parasite species of the genus Plasmodium that cause malaria in humans. Pf is responsible for the majority of malaria related deaths and is the most prevalent species in sub-Saharan Africa.
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 - - 8.3 pIC50 3
⤷ pIC50 8.3 (IC50 5x10-9 M) [3]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
MMV693183 Small molecule or natural product Guide to Malaria Pharmacology Ligand PfNF54

Plasmodium falciparum NF54

P. falciparum strain NF54 (PfNF54) was derived from a patient who had never left the Netherlands.
PfNF54 can be obtained from the European Malaria Reagent Repository or the Malaria Research and Reference Reagent Resource Center (MR4) and is sensitive to a panel of antimalarial compounds including chloroquine and pyrimethamine.
✖
 Parasite gametocyte viability assay - - 8.1 pIC50 4
⤷ pIC50 8.1 (IC50 8x10-9 M) [4]
Lifecycle stages: Plasmodium sexual blood stage (gametocyte)
Malaria Pharmacology Comments
P. falciparum acetyl-coenzyme A (CoA) synthetase (PfACS) has been selected by the Malaria Drug Accelerator (MalDA) consortium as a high priority target for antimalarial drug discovery [2]. The enzyme acetylates CoA to form acetyl CoA, an essential cellular metabolite. PfACS has been genetically and chemically validated [3,5].

References

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1. de Vries LE, Jansen PAM, Barcelo C, Munro J, Verhoef JMJ, Pasaje CFA, Rubiano K, Striepen J, Bolscher JM, Henderson R et al.. (2021) Preclinical characterization and target validation of the antimalarial pantothenamide MMV693183. bioRxiv, Preprint. DOI: 10.1101/2021.05.12.443866

2. Forte B, Ottilie S, Plater A, Campo B, Dechering KJ, Gamo FJ, Goldberg DE, Istvan ES, Lee M, Lukens AK et al.. (2021) Prioritization of Molecular Targets for Antimalarial Drug Discovery. ACS Infect Dis, 7 (10): 2764-2776. [PMID:34523908]

3. Schalkwijk J, Allman EL, Jansen PAM, de Vries LE, Verhoef JMJ, Jackowski S, Botman PNM, Beuckens-Schortinghuis CA, Koolen KMJ, Bolscher JM et al.. (2019) Antimalarial pantothenamide metabolites target acetyl-coenzyme A biosynthesis in Plasmodium falciparum. Sci Transl Med, 11 (510). [PMID:31534021]

4. Schalkwijk J, Hermkens PHH, Dechering KJ, Bonnert RV. (2020) Pantothenamide analogues. Patent number: WO2020141155A1. Assignee: Medicines for Malaria Venture (MMV). Priority date: 31/12/2018. Publication date: 09/07/2020.

5. Summers RL, Pasaje CFA, Pisco JP, Striepen J, Luth MR, Kumpornsin K, Carpenter EF, Munro JT, Lin D, Plater A et al.. (2022) Chemogenomics identifies acetyl-coenzyme A synthetase as a target for malaria treatment and prevention. Cell Chem Biol, 29 (2): 191-201.e8. [PMID:34348113]

How to cite this page

Other antimalarial targets: Plasmodium falciparum acetyl-CoA synthetase. Last modified on 08/04/2022. Accessed on 13/12/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=3174.