Top ▲

Plasmodium falciparum hexose transporter

Click here for help

Target id: 3069

Nomenclature: Plasmodium falciparum hexose transporter

Abbreviated Name: PfHT1

Family: Antimalarial targets

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Plasmodium falciparum 3D7 - 504 HT1 hexose transporter
Database Links Click here for help
PlasmoDB
UniProtKB
Selected 3D Structures Click here for help
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of Plasmodium falciparum hexose transporter PfHT1 bound with C3361
PDB Id:  6M2L
Resolution:  3.7Å
Species:  Plasmodium falciparum
References:  1
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of Plasmodium falciparum hexose transporter PfHT1 bound with glucose
PDB Id:  6M20
Resolution:  2.6Å
Species:  Plasmodium falciparum
References:  1
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
HTI-1 Small molecule or natural product Pf3D7 Parasite growth inhibition assay - - 6.4 pEC50 1
pEC50 6.4 (EC50 3.77x10-7 M) SYBR Green I assay [1]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
HTI-1 Small molecule or natural product PfDd2 Parasite growth inhibition assay - - 6.4 pEC50 1
pEC50 6.4 (EC50 3.98x10-7 M) SYBR Green I assay [1]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
TCMDC-125163 Small molecule or natural product PfK1 Parasite growth inhibition assay - - 6.0 pEC50 2
pEC50 6.0 (EC50 9.7x10-7 M) SYBR Green I assay [2]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
TCMDC-125163 Small molecule or natural product Pf3D7 Parasite growth inhibition assay - - 5.8 pEC50 2
pEC50 5.8 (EC50 1.4x10-6 M) SYBR Green I assay [2]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Malaria Pharmacology Comments
The P. falciparum hexose transporter (PfHT1) mediates glucose uptake, an essential process because the intraerythrocytic stages of the parasite's lifecycle are dependent upon host glucose for energy [3]. PfHT1 is a member of the SLC2 family of hexose and sugar alcohol transporters but is highly divergent in sequence from all human orthologs, with GLUT1 the most closely related human ortholog, sharing only 28% amino acid identity with PfHT1 [2].
PfHT1 shows promise as a target for antimalarial drug development with a focus on identifying compounds that inhibit the parasite permease without impairing function of human SLC2 transporters.

References

Show »

1. Jiang X, Yuan Y, Huang J, Zhang S, Luo S, Wang N, Pu D, Zhao N, Tang Q, Hirata K et al.. (2020) Structural Basis for Blocking Sugar Uptake into the Malaria Parasite Plasmodium falciparum. Cell, 183 (1): 258-268.e12. [PMID:32860739]

2. Ortiz D, Guiguemde WA, Johnson A, Elya C, Anderson J, Clark J, Connelly M, Yang L, Min J, Sato Y et al.. (2015) Identification of Selective Inhibitors of the Plasmodium falciparum Hexose Transporter PfHT by Screening Focused Libraries of Anti-Malarial Compounds. PLoS ONE, 10 (4): e0123598. [PMID:25894322]

3. Woodrow CJ, Penny JI, Krishna S. (1999) Intraerythrocytic Plasmodium falciparum expresses a high affinity facilitative hexose transporter. J. Biol. Chem., 274 (11): 7272-7. [PMID:10066789]

How to cite this page

Antimalarial targets: Plasmodium falciparum hexose transporter. Last modified on 23/09/2020. Accessed on 20/01/2021. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=3069.