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 (K A in the range of 1.00–2.51 µM. The only amine with submicromolar activating properties was 1-(2-aminoethyl-piperazine) with a K A of 0.71 µM, whereas histamine, dopamine and serotonin showed K A 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.

The first activation studies of the η-carbonic anhydrase from the malaria parasite Plasmodium falciparum with amines and amino acids / Angeli A.; Del Prete S.; Alasmary F.A.S.; Alqahtani L.S.; AlOthman Z.; Donald W.A.; Capasso C.; Supuran C.T.. - In: BIOORGANIC CHEMISTRY. - ISSN 0045-2068. - ELETTRONICO. - 80:(2018), pp. 94-98. [10.1016/j.bioorg.2018.06.002]

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

Angeli A.;Supuran C. T.
2018

Abstract

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 (K A in the range of 1.00–2.51 µM. The only amine with submicromolar activating properties was 1-(2-aminoethyl-piperazine) with a K A of 0.71 µM, whereas histamine, dopamine and serotonin showed K A 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.
2018
80
94
98
Angeli A.; Del Prete S.; Alasmary F.A.S.; Alqahtani L.S.; AlOthman Z.; Donald W.A.; Capasso C.; Supuran C.T.
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Utilizza questo identificatore per citare o creare un link a questa risorsa: https://hdl.handle.net/2158/1189324
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