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bromodomain

NOT Open Access | Developments in drug design strategies for bromodomain protein inhibitors to target Plasmodium falciparum parasites

December 30, 2019 - 15:16 -- NOT Open Access
Author(s): 
Nguyen HHT, Yeoh LM, Chisholm SA, Duffy MF
Reference: 
Expert Opin Drug Discov. 2019 Dec 23:1-11

Bromodomains (BRDs) bind to acetylated lysine residues, often on histones. The BRD proteins can contribute to gene regulation either directly through enzymatic activity or indirectly through recruitment of chromatin-modifying complexes or transcription factors. There is no evidence of direct orthologues of the Plasmodium falciparum BRD proteins (PfBDPs) outside the apicomplexans. PfBDPs are expressed during the parasite’s life cycle in both the human host’s blood and in the mosquito. PfBDPs could also prove to be promising targets for novel antimalarials, which are urgently required to address increasing drug resistance.

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