Plasmodium falciparum cGMP-dependent protein kinase | Antimalarial targets | IUPHAR/MMV Guide to MALARIA PHARMACOLOGY

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Plasmodium falciparum cGMP-dependent protein kinase

Target id: 3013

Nomenclature: Plasmodium falciparum cGMP-dependent protein kinase

Abbreviated Name: PfPKG

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 - 853 PKG cGMP-dependent protein kinase
Database Links
UniProtKB
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  Crystal Structure of PF3D7_1436600
PDB Id:  5DYK
Resolution:  2.45Å
Species:  Plasmodium falciparum
References: 
Other Binding Ligands
Key to terms and symbols Click column headers to sort
Ligand Sp. Action Value Parameter Reference
ML10 Pf3D7 Inhibition 9.8 pIC50 2
pIC50 9.8 (IC50 1.6x10-10 M) [2]
Description: microfluidic mobility shift assay
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
ML10 Pf3D7 Parasite growth inhibition assay - - 8.7 pEC50 2
pEC50 8.7 (EC50 2.1x10-9 M) [3H]-hypoxanthine incorporation [2]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Malaria Pharmacology Comments
The Plasmodium cGMP-dependent protein kinase (PfPKG) is an attractive target for next generation antimalarials as it has been implicated in multiple cellular activities at various stages of the parasite lifecycle [1]. A medicinal chemistry programme has identified an imidazopyridine series that demonstrates promising activity and may warrant further development [2].

References

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1. Alam MM, Solyakov L, Bottrill AR, Flueck C, Siddiqui FA, Singh S, Mistry S, Viskaduraki M, Lee K, Hopp CS et al.. (2015) Phosphoproteomics reveals malaria parasite Protein Kinase G as a signalling hub regulating egress and invasion. Nat Commun, 6: 7285. [PMID:26149123]

2. Baker DA, Stewart LB, Large JM, Bowyer PW, Ansell KH, Jiménez-Díaz MB, El Bakkouri M, Birchall K, Dechering KJ, Bouloc NS et al.. (2017) A potent series targeting the malarial cGMP-dependent protein kinase clears infection and blocks transmission. Nat Commun, 8 (1): 430. [PMID:28874661]

How to cite this page

Antimalarial targets: Plasmodium falciparum cGMP-dependent protein kinase. Last modified on 04/06/2019. Accessed on 18/08/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=3013.