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Target id: 3013
Nomenclature: Plasmodium falciparum cGMP-dependent protein kinase
Abbreviated Name: PfPKG
Family: Kinases (Plasmodium spp.)
Gene and Protein Information | ||||||
Species | TM | AA | Chromosomal Location | Gene Symbol | Gene Name | Reference |
Plasmodium falciparum 3D7 | - | 853 | PKG | cGMP-dependent protein kinase |
Previous and Unofficial Names |
PKG | Pf3D7_14_v3:1,490,321..1,494,453(-) | PF14_0346 |
Database Links | |
Alphafold | Q8I719 (Pf3D7) |
PlasmoDB | PF3D7_1436600 (Pf3D7) |
UniProtKB | Q8I719 (Pf3D7) |
Selected 3D Structures | |||||||||||
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Other Binding Ligands | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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Whole Organism Assay Data Linked to This Target | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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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]. |
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]
3. El Bakkouri M, Kouidmi I, Wernimont AK, Amani M, Hutchinson A, Loppnau P, Kim JJ, Flueck C, Walker JR, Seitova A et al.. (2019) Structures of the cGMP-dependent protein kinase in malaria parasites reveal a unique structural relay mechanism for activation. Proc Natl Acad Sci U S A, 116 (28): 14164-14173. [PMID:31239348]
4. Vanaerschot M, Murithi JM, Pasaje CFA, Ghidelli-Disse S, Dwomoh L, Bird M, Spottiswoode N, Mittal N, Arendse LB, Owen ES et al.. (2020) Inhibition of Resistance-Refractory P. falciparum Kinase PKG Delivers Prophylactic, Blood Stage, and Transmission-Blocking Antiplasmodial Activity. Cell Chem Biol, 27 (7): 806-816.e8. [PMID:32359426]
Kinases (Plasmodium spp.): Plasmodium falciparum cGMP-dependent protein kinase. Last modified on 11/10/2021. Accessed on 11/11/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=3013.