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Plasmodium falciparum histone acetyltransferase GCN5

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Target not currently curated in GtoImmuPdb

Malaria Pharmacology Ligand  Target has curated data in GtoMPdb

Target id: 3191

Nomenclature: Plasmodium falciparum histone acetyltransferase GCN5

Abbreviated Name: PfGCN5

Family: Chromatin modifying enzymes (Plasmodium spp.)

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Plasmodium falciparum 3D7 - 1465 GCN5 histone acetyltransferase GCN5
Previous and Unofficial Names Click here for help
GCN5 | Pf3D7_08_v3:1,028,410..1,034,211(+) | PF08_0034
Database Links Click here for help
Alphafold Q8IB67 (Pf3D7)
ChEMBL Target CHEMBL4295890 (Pf3D7)
PlasmoDB PF3D7_0823300 (Pf3D7)
UniProtKB Q8IB67 (Pf3D7)
Selected 3D Structures Click here for help
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of bromodomain from Plasmodium faciparum GCN5, PF3D7_0823300
PDB Id:  4QNS
Resolution:  1.5Å
Species:  Plasmodium falciparum 3D7
References: 
Image of receptor 3D structure from RCSB PDB
Description:  Bromodomain from Plasmodium Faciparum Gcn5, complexed with compound
PDB Id:  5TPX
Ligand:  L-45
Resolution:  2.1Å
Species:  Plasmodium falciparum 3D7
References:  3

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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
L-45 Small molecule or natural product Ligand has a PDB structure Guide to Malaria Pharmacology Ligand Pf

Plasmodium falciparum

P. falciparum (Pf) is one of five protozoan parasite species of the genus Plasmodium that cause malaria in humans. Pf is responsible for the majority of malaria related deaths and is the most prevalent species in sub-Saharan Africa.
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 Inhibition 6.6 pKd 3
⤷ pKd 6.6 (Kd 2.8x10-7 M) [3]
Description: Isothermal titration calorimetry.
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
SGC-CBP30 Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Guide to Malaria Pharmacology Ligand PfDd2

Plasmodium falciparum Dd2

P. falciparum strain Dd2 (PfDd2) is a clone derived from PfW2, following continuous culture in mefloquine. PfW2 was cloned from the Indochina III/CDC isolate, originally derived from a Laotian patient who failed chloroquine therapy.
PfDd2 can be obtained from the Malaria Research and Reference Reagent Resource Center (MR4) and is reported to be resistant to chloroquine, pyrimethamine and mefloquine.
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 Parasite growth inhibition assay - - 5.5 pIC50 1
⤷ pIC50 5.5 (IC50 3.16x10-6 M) [3H]-hypoxanthine incorporation assay (72 h with synchronous parasites) [1]
Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont)
Malaria Pharmacology Comments
P. falciparum histone acetyltransferase GCN5 (PfGCN5) is a Gcn5-related N-acetyltransferase (GNAT) belonging to the histone acetyltransferase (HAT) family [2].

References

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1. Chua MJ, Robaa D, Skinner-Adams TS, Sippl W, Andrews KT. (2018) Activity of bromodomain protein inhibitors/binders against asexual-stage Plasmodium falciparum parasites. Int J Parasitol Drugs Drug Resist, 8 (2): 189-193. [PMID:29631126]

2. Fan Q, An L, Cui L. (2004) Plasmodium falciparum histone acetyltransferase, a yeast GCN5 homologue involved in chromatin remodeling. Eukaryot Cell, 3 (2): 264-76. [PMID:15075257]

3. Moustakim M, Clark PG, Trulli L, Fuentes de Arriba AL, Ehebauer MT, Chaikuad A, Murphy EJ, Mendez-Johnson J, Daniels D, Hou CD et al.. (2017) Discovery of a PCAF Bromodomain Chemical Probe. Angew Chem Int Ed Engl, 56 (3): 827-831. [PMID:27966810]

How to cite this page

Chromatin modifying enzymes (Plasmodium spp.): Plasmodium falciparum histone acetyltransferase GCN5. Last modified on 13/12/2021. Accessed on 07/12/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=3191.