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Plasmodium falciparum GPI-anchored wall transfer protein 1

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Target id: 3075

Nomenclature: Plasmodium falciparum GPI-anchored wall transfer protein 1

Abbreviated Name: PfGWT1

Family: Other antimalarial targets

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Plasmodium falciparum 3D7 - 874 GWT1 GPI-anchored wall transfer protein 1, putative
Previous and Unofficial Names Click here for help
PFF0740c
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PlasmoDB
UniProtKB
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
compound VII [WO2021149692A1] Small molecule or natural product Guide to Malaria Pharmacology Ligand Pf3D7 Parasite growth inhibition assay - - 7.5 pIC50 2
pIC50 7.5 (IC50 3x10-8 M) Parasite lactate dehydrogenase (pLDH ) assay following 72 hours in culture [2]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
compound VII [WO2021149692A1] Small molecule or natural product Guide to Malaria Pharmacology Ligand PfK1 Parasite growth inhibition assay - - 7.4 pIC50 2
pIC50 7.4 (IC50 4.1x10-8 M) Parasite lactate dehydrogenase (pLDH ) assay following 72 hours in culture [2]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Malaria Pharmacology Comments
GWT1 (PfGWT1), one of the essential enzymes involved in glycosylphosphatidylinositol (GPI) biosynthesis in the malaria parasite P. falciparum, is a promising novel target for antimalarial drug development (Patent WO2004048567 [1]). In this patent representative compounds known to inhibit yeast GWT1 were assayed for antimalarial activity, with compound 3 (PubChem CID 9860834) reported to have the most potent activity.

References

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1. Hata K, Ogawa K, Tsukada I, Nakamoto K, Sagane K, Tanaka K, Tsukahara K, Horii T. (2004) Methods of screening for compounds that inhibit the biosynthesis of GPI in malaria parasites. Patent number: WO2004048567A2. Assignee: Eisai Co., Ltd. Priority date: 22/11/2002. Publication date: 10/06/2004.

2. Horii T, Suzuki S, Roupany AJA, Mui JJB, Lewis-Marshall JP, Devan FA, Cartwright MW. (2021) Novel antimalarial agent containing heterocyclic compound. Patent number: WO2021149692A1. Assignee: Eisai R&D Management Co., Ltd.. Priority date: 21/01/2020. Publication date: 29/07/2021.

How to cite this page

Other antimalarial targets: Plasmodium falciparum GPI-anchored wall transfer protein 1. Last modified on 09/03/2022. Accessed on 25/06/2022. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=3075.