Antimalarial targets

Overview

This family encompasses antimalarial targets identified and validated in Plasmodium, the genus of protozoan parasite known to cause malaria. The genome of P. falciparum, the species that is responsible for the majority of malaria-related deaths, has been sequenced and analysed contributing to an increased understanding of potential biological targets in the parasite. More than half of the predicted gene products exhibit little homology outside the Plasmodium genus and have not been given functional assignments, while a considerable number are unique to P. falciparum [2]. In recent years, genetic methods have facilitated the identification of new molecular targets in the parasite and it is hoped that novel cross-lifecycle targets will be elucidated to help inform antimalarial drug discovery [1].

Targets

PfATP4 (Plasmodium falciparum ATPase4) Show summary »« Hide summary More detailed page

Target Id	2971
Nomenclature	Plasmodium falciparum ATPase4
Common abbreviation	PfATP4
Previous and unofficial names	P-type ATPase4
Genes	ATP4 (Pf3D7)
UniProtKB AC	A0A143ZZK9 (Pf3D7)
PlasmoDB	PF3D7_1211900 (Pf3D7)

PfCARL (Plasmodium falciparum cyclic amine resistance locus) Show summary »« Hide summary More detailed page

Target Id	3074
Nomenclature	Plasmodium falciparum cyclic amine resistance locus
Common abbreviation	PfCARL
Genes	CARL (Pf3D7)
UniProtKB AC	C0H483 (Pf3D7)
PlasmoDB	PF3D7_0321900 (Pf3D7)

PfCLK3 (Plasmodium falciparum cyclin-dependent-like kinase CLK3) Show summary »« Hide summary More detailed page

Target Id	3105
Nomenclature	Plasmodium falciparum cyclin-dependent-like kinase CLK3
Common abbreviation	PfCLK3
Genes	CLK3 (Pf3D7)
UniProtKB AC	Q8IIL5 (Pf3D7)
PlasmoDB	PF3D7_1114700 (Pf3D7)

PfCPSF3 (Plasmodium falciparum cleavage and polyadenylation specificity factor subunit 3) Show summary »« Hide summary More detailed page

Target Id	3076
Nomenclature	Plasmodium falciparum cleavage and polyadenylation specificity factor subunit 3
Common abbreviation	PfCPSF3
Previous and unofficial names	PfCPSF73 \| PfCPSF-73
Genes	CPSF3 (Pf3D7)
UniProtKB AC	Q8IL83 (Pf3D7)
PlasmoDB	PF3D7_1438500 (Pf3D7)

PfCYTB (Plasmodium falciparum cytochrome b) Show summary »« Hide summary More detailed page

Target Id	3087
Nomenclature	Plasmodium falciparum cytochrome b
Common abbreviation	PfCYTB
Genes	CYTB (Pf3D7)
UniProtKB AC	Q02768 (Pf)
PlasmoDB	mal_mito_3 (Pf3D7)

PfDHFR-TS (Plasmodium falciparum bifunctional dihydrofolate reductase-thymidylate synthase) Show summary »« Hide summary More detailed page

Target Id	2981
Nomenclature	Plasmodium falciparum bifunctional dihydrofolate reductase-thymidylate synthase
Common abbreviation	PfDHFR-TS
Genes	DHFR-TS (Pf3D7)
UniProtKB AC	Q8I1R6 (Pf3D7)
PlasmoDB	PF3D7_0417200 (Pf3D7)

PfDHODH (Plasmodium falciparum dihydroorotate dehydrogenase) Show summary »« Hide summary More detailed page

Target Id	2949
Nomenclature	Plasmodium falciparum dihydroorotate dehydrogenase
Common abbreviation	PfDHODH
Previous and unofficial names	Pfal DHODH
Genes	DHODH (Pf3D7)
UniProtKB AC	Q08210 (Pf3D7)
PlasmoDB	PF3D7_0603300 (Pf3D7)

PfDXR (Plasmodium falciparum 1-deoxy-D-xylulose 5-phosphate reductoisomerase) Show summary »« Hide summary More detailed page

Target Id	2980
Nomenclature	Plasmodium falciparum 1-deoxy-D-xylulose 5-phosphate reductoisomerase
Common abbreviation	PfDXR
Previous and unofficial names	DOXR \| IspC
Genes	DXR (Pf3D7)
UniProtKB AC	Q8IKG4 (Pf3D7)
PlasmoDB	PF3D7_1467300 (Pf3D7)

PfeEF2 (Plasmodium falciparum elongation factor 2) Show summary »« Hide summary More detailed page

Target Id	2975
Nomenclature	Plasmodium falciparum elongation factor 2
Common abbreviation	PfeEF2
Genes	eEF2 (Pf3D7)
UniProtKB AC	Q8IKW5 (Pf3D7)
PlasmoDB	PF3D7_1451100 (Pf3D7)

PfGWT1 (Plasmodium falciparum GPI-anchored wall transfer protein 1) Show summary »« Hide summary More detailed page

Target Id	3075
Nomenclature	Plasmodium falciparum GPI-anchored wall transfer protein 1
Common abbreviation	PfGWT1
Genes	GWT1 (Pf3D7)
UniProtKB AC	C6KSZ4 (Pf3D7)
PlasmoDB	PF3D7_0615300 (Pf3D7)

PfHDAC1 (Plasmodium falciparum histone deacetylase 1) Show summary »« Hide summary More detailed page

Target Id	3072
Nomenclature	Plasmodium falciparum histone deacetylase 1
Common abbreviation	PfHDAC1
Previous and unofficial names	PfKDAC1
Genes	HDAC1 (Pf3D7)
UniProtKB AC	Q7K6A1 (Pf3D7)
PlasmoDB	PF3D7_0925700 (Pf3D7)

PfHDP (Plasmodium falciparum heme detoxification protein) Show summary »« Hide summary More detailed page

Target Id	3079
Nomenclature	Plasmodium falciparum heme detoxification protein
Common abbreviation	PfHDP
Previous and unofficial names	Plasmodium falciparum heme ligase
Genes	HDP (Pf3D7)
UniProtKB AC	Q8IL04 (Pf3D7)
PlasmoDB	PF3D7_1446800 (Pf3D7)

PfHT (Plasmodium falciparum hexose transporter) Show summary »« Hide summary More detailed page

Target Id	3069
Nomenclature	Plasmodium falciparum hexose transporter
Common abbreviation	PfHT
Genes	HT (Pf3D7)
UniProtKB AC	Q7KWJ5 (Pf3D7)
PlasmoDB	PF3D7_0204700 (Pf3D7)

PfIspD (Plasmodium falciparum 2-C-methyl-D-erythritol 4-phosphate cytidylyltransferase) Show summary »« Hide summary More detailed page

Target Id	3064
Nomenclature	Plasmodium falciparum 2-C-methyl-D-erythritol 4-phosphate cytidylyltransferase
Common abbreviation	PfIspD
Genes	IspD (Pf3D7)
UniProtKB AC	Q8I273 (Pf3D7)
PlasmoDB	PF3D7_0106900 (Pf3D7)

PfNCR1 (Plasmodium falciparum Niemann-Pick type C1-related protein) Show summary »« Hide summary More detailed page

Target Id	3107
Nomenclature	Plasmodium falciparum Niemann-Pick type C1-related protein
Common abbreviation	PfNCR1
Genes	NCR1 (Pf3D7)
UniProtKB AC	Q8I266 (Pf3D7)
PlasmoDB	PF3D7_0107500 (Pf3D7)

PfNDH2 (Plasmodium falciparum type II NADH:ubiquinone oxidoreductase) Show summary »« Hide summary More detailed page

Target Id	3090
Nomenclature	Plasmodium falciparum type II NADH:ubiquinone oxidoreductase
Common abbreviation	PfNDH2
Genes	NDH2 (Pf3D7)
UniProtKB AC	Q8I302 (Pf3D7)
PlasmoDB	PF3D7_0915000 (Pf3D7)

PfNMT (Plasmodium falciparum N-Myristoyltransferase) Show summary »« Hide summary More detailed page

Target Id	2955
Nomenclature	Plasmodium falciparum N-Myristoyltransferase
Common abbreviation	PfNMT
Previous and unofficial names	Pfal NMT
Genes	NMT (Pf3D7)
UniProtKB AC	Q8ILW6 (Pf3D7)
PlasmoDB	PF3D7_1412800 (Pf3D7)

PfPANK1 (Plasmodium falciparum pantothenate kinase 1) Show summary »« Hide summary More detailed page

Target Id	3089
Nomenclature	Plasmodium falciparum pantothenate kinase 1
Common abbreviation	PfPANK1
Genes	PANK1 (Pf3D7)
UniProtKB AC	Q8ILP4 (Pf3D7)
PlasmoDB	PF3D7_1420600 (Pf3D7)

PfPDEalpha (Plasmodium falciparum cGMP-specific phosphodiesterase) Show summary »« Hide summary More detailed page

Target Id	3091
Nomenclature	Plasmodium falciparum cGMP-specific phosphodiesterase
Common abbreviation	PfPDEalpha
Previous and unofficial names	PfPDE1
Genes	PDEalpha (Pf3D7)
UniProtKB AC	Q8I5V4 (Pf3D7)
PlasmoDB	PF3D7_1209500 (Pf3D7)

PfPI3K (Plasmodium falciparum phosphatidylinositol 3-kinase) Show summary »« Hide summary More detailed page

Target Id	3073
Nomenclature	Plasmodium falciparum phosphatidylinositol 3-kinase
Common abbreviation	PfPI3K
Previous and unofficial names	PfVPS34
Genes	PI3K (Pf3D7)
UniProtKB AC	Q8I3V5 (Pf3D7)
PlasmoDB	PF3D7_0515300 (Pf3D7)

PfPI4K (Plasmodium falciparum phosphatidylinositol 4-kinase) Show summary »« Hide summary More detailed page

Target Id	2972
Nomenclature	Plasmodium falciparum phosphatidylinositol 4-kinase
Common abbreviation	PfPI4K
Genes	PI4K (Pf3D7)
UniProtKB AC	Q8I406 (Pf3D7)
PlasmoDB	PF3D7_0509800 (Pf3D7)

PfPKG (Plasmodium falciparum cGMP-dependent protein kinase) Show summary »« Hide summary More detailed page

Target Id	3013
Nomenclature	Plasmodium falciparum cGMP-dependent protein kinase
Common abbreviation	PfPKG
Genes	PKG (Pf3D7)
UniProtKB AC	Q8I719 (Pf3D7)
PlasmoDB	PF3D7_1436600 (Pf3D7)

PfPMV (Plasmodium falciparum plasmepsin V) Show summary »« Hide summary More detailed page

Target Id	3106
Nomenclature	Plasmodium falciparum plasmepsin V
Common abbreviation	PfPMV
Genes	PMV (Pf3D7)
UniProtKB AC	Q8I6Z5 (Pf3D7)
PlasmoDB	PF3D7_1323500 (Pf3D7)

PfPMX (Plasmodium falciparum plasmepsin X) Show summary »« Hide summary More detailed page

Target Id	3071
Systematic nomenclature	Plasmodium falciparum plasmepsin X
Common abbreviation	PfPMX
Genes	PMX (Pf3D7)
UniProtKB AC	Q8IAS0
PlasmoDB	PF3D7_0808200 (Pf3D7)

Plasmodium falciparum proteasome subunit beta type-5 Show summary »« Hide summary More detailed page

Target Id

3088

Nomenclature

Plasmodium falciparum proteasome subunit beta type-5

Genes

PF3D7_1011400 (Pf3D7)

UniProtKB AC

Q8IJT1 (Pf3D7)

PlasmoDB

PF3D7_1011400 (Pf3D7)

Inhibitors

bortezomib pIC₅₀ 7.3 (Fluorogenic peptide assay used to assess purified Pf20S proteasome activity) [4] - Plasmodium falciparum

Whole Organism Data Linked to Target

bortezomib pIC₅₀ 7.5 ([³H]-hypoxanthine incorporation) [3] - Plasmodium falciparum 3D7

bortezomib pIC₅₀ 7.5 ([³H]-hypoxanthine incorporation) [3] - Plasmodium falciparum HB3

bortezomib pIC₅₀ 7.4 ([³H]-hypoxanthine incorporation) [3] - Plasmodium falciparum Dd2

bortezomib pIC₅₀ 7.4 ([³H]-hypoxanthine incorporation) [3] - Plasmodium falciparum W2

PfPNP (Plasmodium falciparum purine nucleoside phosphorylase) Show summary »« Hide summary More detailed page

Target Id	3077
Nomenclature	Plasmodium falciparum purine nucleoside phosphorylase
Common abbreviation	PfPNP
Genes	PNP (Pf3D7)
UniProtKB AC	Q8I3X4 (Pf3D7)
PlasmoDB	PF3D7_0513300 (Pf3D7)

PfPPPK-DHPS (Plasmodium falciparum hydroxymethyldihydropterin pyrophosphokinase-dihydropteroate synthase) Show summary »« Hide summary More detailed page

Target Id	3065
Nomenclature	Plasmodium falciparum hydroxymethyldihydropterin pyrophosphokinase-dihydropteroate synthase
Common abbreviation	PfPPPK-DHPS
Genes	PPPK-DHPS (Pf3D7)
UniProtKB AC	Q8IAU3 (Pf3D7)
PlasmoDB	PF3D7_0810800 (Pf3D7)

PfSHMT (Plasmodium falciparum serine hydroxymethyltransferase) Show summary »« Hide summary More detailed page

Target Id	3066
Nomenclature	Plasmodium falciparum serine hydroxymethyltransferase
Common abbreviation	PfSHMT
Genes	SHMT (Pf3D7)
UniProtKB AC	Q8I566 (Pf3D7)
PlasmoDB	PF3D7_1235600 (Pf3D7)

PfKRS1 (Plasmodium falciparum lysine--tRNA ligase) Show summary »« Hide summary More detailed page

Target Id	3059
Nomenclature	Plasmodium falciparum lysine--tRNA ligase
Common abbreviation	PfKRS1
Previous and unofficial names	Plasmodium falciparum lysyl-tRNA synthetase
Genes	KRS1 (Pf3D7)
UniProtKB AC	Q8IDJ8 (Pf3D7)
PlasmoDB	PF3D7_1350100 (Pf3D7)

PfcPheRS (Plasmodium falciparum phenylalanine--tRNA ligase alpha subunit) Show summary »« Hide summary More detailed page

Target Id	2954
Nomenclature	Plasmodium falciparum phenylalanine--tRNA ligase alpha subunit
Common abbreviation	PfcPheRS
Previous and unofficial names	Pfal cPheRS
Genes	cPheRS (Pf3D7)
UniProtKB AC	Q8I246 (Pf3D7)
PlasmoDB	PF3D7_0109800 (Pf3D7)

PfPRS (Plasmodium falciparum proline--tRNA ligase) Show summary »« Hide summary More detailed page

Target Id	3056
Nomenclature	Plasmodium falciparum proline--tRNA ligase
Common abbreviation	PfPRS
Previous and unofficial names	Plasmodium falciparum prolyl-tRNA synthetase \| PfPRORS
Genes	PRS (Pf3D7)
UniProtKB AC	Q8I5R7 (Pf3D7)
PlasmoDB	PF3D7_1213800 (Pf3D7)

PfThrRS (Plasmodium falciparum threonine--tRNA ligase) Show summary »« Hide summary More detailed page

Target Id	3058
Nomenclature	Plasmodium falciparum threonine--tRNA ligase
Common abbreviation	PfThrRS
Previous and unofficial names	Plasmodium falciparum threoninyl-tRNA synthetase
Genes	ThrRS (Pf3D7)
UniProtKB AC	Q8IIA4 (Pf3D7)
PlasmoDB	PF3D7_1126000 (Pf3D7)

Plasmodium falciparum V-type proton ATPase Show summary »« Hide summary More detailed page

Target Id	3078
Nomenclature	Plasmodium falciparum V-type proton ATPase
Previous and unofficial names	Plasmodium falciparum V-type H+ ATPase
Genes	PF3D7_1341900 (Pf3D7)
UniProtKB AC	Q8IDS0 (Pf3D7)
PlasmoDB	PF3D7_1341900 (Pf3D7)

References

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1. Flannery EL, Fidock DA, Winzeler EA. (2013) Using genetic methods to define the targets of compounds with antimalarial activity. J. Med. Chem., 56 (20): 7761-71. [PMID:23927658]

2. Gardner MJ, Hall N, Fung E, White O, Berriman M, Hyman RW, Carlton JM, Pain A, Nelson KE, Bowman S et al.. (2002) Genome sequence of the human malaria parasite Plasmodium falciparum. Nature, 419 (6906): 498-511. [PMID:12368864]

3. Reynolds JM, El Bissati K, Brandenburg J, Günzl A, Mamoun CB. (2007) Antimalarial activity of the anticancer and proteasome inhibitor bortezomib and its analog ZL3B. BMC Clin Pharmacol, 7: 13. [PMID:17956613]

4. Xie SC, Gillett DL, Spillman NJ, Tsu C, Luth MR, Ottilie S, Duffy S, Gould AE, Hales P, Seager BA et al.. (2018) Target Validation and Identification of Novel Boronate Inhibitors of the Plasmodium falciparum Proteasome. J. Med. Chem., 61 (22): 10053-10066. [PMID:30373366]

How to cite this family page

Database page citation:

Antimalarial targets. Accessed on 04/04/2020. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=970.

Concise Guide to PHARMACOLOGY citation:

Alexander SPH, Kelly E, Mathie A, Peters JA, Veale EL, Armstrong JF, Faccenda E, Harding SD, Pawson AJ, Sharman JL, Southan C, Buneman OP, Cidlowski JA, Christopoulos A, Davenport AP, Fabbro D, Spedding M, Striessnig J, Davies JA; CGTP Collaborators. (2019) The Concise Guide to PHARMACOLOGY 2019/20: Introduction and Other Protein Targets. Br J Pharmacol. 176 Issue S1: S1-S20.