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Plasmodium falciparum cytochrome b

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Target id: 3087

Nomenclature: Plasmodium falciparum cytochrome b

Abbreviated Name: PfCYTB

Family: Mitochondrial function/Mitochondrial electron flow

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Plasmodium falciparum 3D7 - 376 CYTB
Database Links Click here for help
ChEMBL Target
PlasmoDB
UniProtKB

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Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
compound 11c [PMID: 30613327] Small molecule or natural product Ligand has a PDB structure Pf Inhibition 9.1 pIC50 3
pIC50 9.1 (IC50 7.5x10-10 M) [3]
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
ELQ-300 Small molecule or natural product Pb Parasite liver stage assay - - 9.0 pEC50 4
pEC50 9.0 (EC50 1.02x10-9 M) Luciferase bioluminescence assay to measure viability of exoerythrocytic forms [4]
Lifecycle stages: Plasmodium liver stage (sporozoite, hepatic schizont, hepatic merozoite)
compound 27 [PMID: 32945666] Small molecule or natural product Pf3D7 Parasite growth inhibition assay - - 7.2 pEC50 2
pEC50 7.2 (EC50 7x10-8 M) SYBR Green I assay [2]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
atovaquone Small molecule or natural product Approved drug Ligand has a PDB structure PfD6 Parasite growth inhibition assay - - 10.0 pIC50 1
pIC50 10.0 (IC50 1x10-10 M) [3H]-hypoxanthine incorporation [1]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
atovaquone Small molecule or natural product Approved drug Ligand has a PDB structure PfW2 Parasite growth inhibition assay - - 9.7 pIC50 1
pIC50 9.7 (IC50 2x10-10 M) [3H]-hypoxanthine incorporation [1]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
atovaquone Small molecule or natural product Approved drug Ligand has a PDB structure Pf7G8 Parasite growth inhibition assay - - 9.5 pIC50 1
pIC50 9.5 (IC50 3x10-10 M) [3H]-hypoxanthine incorporation [1]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
atovaquone Small molecule or natural product Approved drug Ligand has a PDB structure PfTM90C2A Parasite growth inhibition assay - - 9.3 pIC50 1
pIC50 9.3 (IC50 5x10-10 M) [3H]-hypoxanthine incorporation [1]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
atovaquone Small molecule or natural product Approved drug Ligand has a PDB structure PfNF54 Parasite growth inhibition assay - - 9.2 pIC50 1
pIC50 9.2 (IC50 6x10-10 M) [3H]-hypoxanthine incorporation [1]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
atovaquone Small molecule or natural product Approved drug Ligand has a PDB structure PfK1 Parasite growth inhibition assay - - 9.0 pIC50 1
pIC50 9.0 (IC50 1.1x10-9 M) [3H]-hypoxanthine incorporation [1]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
atovaquone Small molecule or natural product Approved drug Ligand has a PDB structure PfV1/S Parasite growth inhibition assay - - 8.9 pIC50 1
pIC50 8.9 (IC50 1.4x10-9 M) [3H]-hypoxanthine incorporation [1]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
ELQ-300 Small molecule or natural product PfW2 Parasite growth inhibition assay - - 8.6 – 8.7 pIC50 4
pIC50 8.7 (IC50 1.8x10-9 M) SYBR green method, measured at 72h [4]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
pIC50 8.6 (IC50 2.27x10-9 M) [3H]-hypoxanthine incorporation [4]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
ELQ-300 Small molecule or natural product PfTM90C2B Parasite growth inhibition assay - - 8.6 – 8.8 pIC50 4
pIC50 8.8 (IC50 1.7x10-9 M) SYBR green method, measured at 72h [4]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
pIC50 8.6 (IC50 2.84x10-9 M) [3H]-hypoxanthine incorporation [4]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
ELQ-300 Small molecule or natural product PfDd2 Parasite growth inhibition assay - - 8.6 pIC50 4
pIC50 8.6 (IC50 2.5x10-9 M) SYBR green method, measured at 72h [4]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
ELQ-300 Small molecule or natural product PfD6 Parasite growth inhibition assay - - 8.5 – 8.7 pIC50 4
pIC50 8.7 (IC50 2.2x10-9 M) SYBR green method, measured at 72h [4]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
pIC50 8.5 (IC50 3.06x10-9 M) [3H]-hypoxanthine incorporation [4]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
ELQ-300 Small molecule or natural product PfTM91C235 Parasite growth inhibition assay - - 8.4 pIC50 4
pIC50 8.4 (IC50 4.34x10-9 M) [3H]-hypoxanthine incorporation [4]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
compound 11c [PMID: 30613327] Small molecule or natural product Ligand has a PDB structure PfW2 Parasite growth inhibition assay - - 7.8 pIC50 3
pIC50 7.8 (IC50 1.5x10-8 M) SYBR Green I method, measured at 48h [3]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
compound 11c [PMID: 30613327] Small molecule or natural product Ligand has a PDB structure Pf3D7 Parasite growth inhibition assay - - 7.5 pIC50 3
pIC50 7.5 (IC50 3.3x10-8 M) SYBR Green I method, measured at 48h [3]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
ELQ-300 Small molecule or natural product PfNF54 Parasite late stage (IV–V) gametocyte assay - - 7.1 pIC50 4
pIC50 7.1 (IC50 7.19x10-8 M) High-content fluorescence-based image analysis of gametocyte viability throughout a period of 72 hours [4]
Lifecycle stages: Plasmodium sexual blood stage (gametocyte)
ELQ-300 Small molecule or natural product Pc Parasite liver stage assay - - ~7.0 pIC50 4
pIC50 ~7.0 (IC50 ~1x10-7 M) High-content fluorescence imaging to quantify the number of developing hepatic schizonts in primary rhesus hepatocytes infected with sporozoites from the M strain of P. cynomolgi [4]
Lifecycle stages: Plasmodium liver stage (sporozoite, hepatic schizont, hepatic merozoite)
compound 27 [PMID: 32945666] Small molecule or natural product Pb Parasite liver stage assay - - 6.5 pIC50 2
pIC50 6.5 (IC50 3x10-7 M) Luciferase bioluminescence assay to measure viability of exoerythrocytic forms (EEF) [2]
Lifecycle stages: Plasmodium liver stage (sporozoite, hepatic schizont, hepatic merozoite)
compound 11c [PMID: 30613327] Small molecule or natural product Ligand has a PDB structure PfTM90C2B Parasite growth inhibition assay - - 6.3 pIC50 3
pIC50 6.3 (IC50 5x10-7 M) SYBR Green I method, measured at 48h [3]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
ELQ-300 Small molecule or natural product PfNF54 Parasite early stage (I–III) gametocyte assay - - - - 4
Giemsa-stained blood film counts: treated gametocytes did not develop past stage III, even at 0.1 μM, the lowest dose tested [4]
Lifecycle stages: Plasmodium sexual blood stage (gametocyte)
Malaria Pharmacology Comments
The cytochrome bc1 complex is the third component of the mitochondrial electron transport chain and is the target of several potent antimalarial compounds, including the naphthoquinone atovaquone and the 4(1H)-quinolone ELQ-300.

References

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1. Delves M, Plouffe D, Scheurer C, Meister S, Wittlin S, Winzeler EA, Sinden RE, Leroy D. (2012) The activities of current antimalarial drugs on the life cycle stages of Plasmodium: a comparative study with human and rodent parasites. PLoS Med, 9 (2): e1001169. [PMID:22363211]

2. Eagon S, Hammill JT, Sigal M, Ahn KJ, Tryhorn JE, Koch G, Belanger B, Chaplan CA, Loop L, Kashtanova AS et al.. (2020) Synthesis and Structure-Activity Relationship of Dual-Stage Antimalarial Pyrazolo[3,4-b]pyridines. J Med Chem, 63 (20): 11902-11919. [PMID:32945666]

3. Hong WD, Leung SC, Amporndanai K, Davies J, Priestley RS, Nixon GL, Berry NG, Hasnain SS, Antonyuk S, Ward SA et al.. (2018) Potent Antimalarial 2-Pyrazolyl Quinolone bc1 (Qi) Inhibitors with Improved Drug-like Properties. ACS Med Chem Lett, 9 (12): 1205-1210. [PMID:30613327]

4. Nilsen A, LaCrue AN, White KL, Forquer IP, Cross RM, Marfurt J, Mather MW, Delves MJ, Shackleford DM, Saenz FE et al.. (2013) Quinolone-3-diarylethers: a new class of antimalarial drug. Sci Transl Med, 5 (177): 177ra37. [PMID:23515079]

How to cite this page

Mitochondrial function/Mitochondrial electron flow: Plasmodium falciparum cytochrome b. Last modified on 22/01/2021. Accessed on 18/10/2021. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=3087.