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Plasmodium falciparum histone acetyltransferase GCN5

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Target id: 3191

Nomenclature: Plasmodium falciparum histone acetyltransferase GCN5

Abbreviated Name: PfGCN5

Family: Other antimalarial targets

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Plasmodium falciparum 3D7 - - GCN5 histone acetyltransferase GCN5
Previous and Unofficial Names Click here for help
GCN5 | histone acetyltransferase GCN5 | PF08_0034
Database Links Click here for help
ChEMBL Target
PlasmoDB
UniProtKB
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 Pf 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 PfDd2 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

Other antimalarial targets: Plasmodium falciparum histone acetyltransferase GCN5. Last modified on 30/08/2021. Accessed on 19/09/2021. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=3191.