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The first activation studies of the η-carbonic anhydrase from the malaria parasite Plasmodium falciparum with amines and amino acids

Publication date:

October 2018


Source:Bioorganic Chemistry, Volume 80

Author(s): Andrea Angeli, Sonia Del Prete, Fatmah A.S. Alasmary, Linah S. Alqahtani, Zeid AlOthman, William A. Donald, Clemente Capasso, Claudiu T. Supuran

The first activation study of a η-class carbonic anhydrase (CAs, EC 4.2.1.1) is reported. A panel of 24 natural and non-natural amino acids and amines was used to explore the activation profile of Plasmodium falciparum CA (PfACA). The most effective activators belonged to the amino acid chemotype, with d-Glu, l-Asp, l-/d-Phe and l-/d-DOPA possessing activation constant in the range of 82 nM–0.75 µM, whereas l-/d-His, l-Tyr, 4-amino-l-Phe and l-Gln were slightly less effective (KA in the range of 1.00–2.51 µM. The only amine with submicromolar activating properties was 1-(2-aminoethyl-piperazine) with a KA of 0.71 µM, whereas histamine, dopamine and serotonin showed KA ranging between 7.18 and 9.97 µM. As CA activators have scarcely been investigated for their interaction with protozoan CAs, this study may be relevant for an improved understanding of the role of this enzyme in the life cycle of the malaria producing organisms belonging to the genus Plasmodium.
Graphical abstract




Authors:   Author(s): Andrea Angeli, Sonia Del Prete, Fatmah A.S. Alasmary, Linah S. Alqahtani, Zeid AlOthman, William A. Donald, Clemente Capasso, Claudiu T. Supuran
Journal:   Bioorganic Chemistry
Volume:   80
Year:   2018
Pages:   94
DOI:   10.1016/j.bioorg.2018.06.002
Publication date:   18-Jun-2018
Facts, background information, dossiers
  • Plasmodium falciparum
  • CAS
  • amino acids
  • serotonin
  • piperazine
  • malaria
  • histamine
  • Genus
  • dopamine
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