Plasmodium falciparum proline--tRNA ligase | Antimalarial targets | IUPHAR/MMV Guide to MALARIA PHARMACOLOGY

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Plasmodium falciparum proline--tRNA ligase

Target id: 3056

Nomenclature: Plasmodium falciparum proline--tRNA ligase

Abbreviated Name: PfPRS

Family: Antimalarial targets

Annotation status:  image of a grey circle Awaiting annotation/under development. Please contact us if you can help with annotation.  » Email us

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Plasmodium falciparum 3D7 - 746 PRS proline--tRNA ligase
Previous and Unofficial Names
Plasmodium falciparum prolyl-tRNA synthetase | PfPRORS
Database Links
ChEMBL Target
PlasmoDB
SynPHARM
UniProtKB
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  Crystal Structure of Prolyl-tRNA Synthetase (PRS) from Plasmodium falciparum in complex with Halofuginone and AMPPNP
PDB Id:  4YDQ
Ligand:  halofuginone
Resolution:  2.3Å
Species:  Plasmodium falciparum
References:  3
Image of receptor 3D structure from RCSB PDB
Description:  Crystal Structure of Prolyl-tRNA Synthetase (PRS) from Plasmodium falciparum
PDB Id:  4TWA
Resolution:  3.0Å
Species:  Plasmodium falciparum
References:  2
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
halofuginone PfDd2 Parasite growth inhibition assay - - 9.1 pEC50 1
pEC50 9.1 (EC50 8.1x10-10 M) SYBR Green assay [1]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
halofuginone Pf3D7 Parasite growth inhibition assay - - 9.1 pEC50 1
pEC50 9.1 (EC50 8.6x10-10 M) SYBR Green assay [1]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Malaria Pharmacology Comments
The aminoacyl-tRNA synthetases are emerging targets for antimalarial agents [4]. Although sharing a common tRNA esterification catalytic activity, these proteins are structurally diverse and physiologically distinct enzymes.

References

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1. Herman JD, Pepper LR, Cortese JF, Estiu G, Galinsky K, Zuzarte-Luis V, Derbyshire ER, Ribacke U, Lukens AK, Santos SA et al.. (2015) The cytoplasmic prolyl-tRNA synthetase of the malaria parasite is a dual-stage target of febrifugine and its analogs. Sci Transl Med, 7 (288): 288ra77. [PMID:25995223]

2. Jain V, Kikuchi H, Oshima Y, Sharma A, Yogavel M. (2014) Structural and functional analysis of the anti-malarial drug target prolyl-tRNA synthetase. J. Struct. Funct. Genomics, 15 (4): 181-90. [PMID:25047712]

3. Jain V, Yogavel M, Oshima Y, Kikuchi H, Touquet B, Hakimi MA, Sharma A. (2015) Structure of Prolyl-tRNA Synthetase-Halofuginone Complex Provides Basis for Development of Drugs against Malaria and Toxoplasmosis. Structure, 23 (5): 819-829. [PMID:25817387]

4. Manickam Y, Chaturvedi R, Babbar P, Malhotra N, Jain V, Sharma A. (2018) Drug targeting of one or more aminoacyl-tRNA synthetase in the malaria parasite Plasmodium falciparum. Drug Discov. Today, 23 (6): 1233-1240. [PMID:29408369]

How to cite this page

Antimalarial targets: Plasmodium falciparum proline--tRNA ligase. Last modified on 12/06/2019. Accessed on 19/11/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=3056.