Work

Triosephosphate isomerase from Fasciola hepatica : high-resolution crystal structure as a drug target

Year: 2025

Type: article

Abstract: The trematode liver fluke Fasciola hepatica causes the neglected tropical disease fascioliasis in humans and is associated with significant losses in agricultural industry due to reduced animal productivity. Triosephosphate isomerase (TPI) is a glycolytic enzyme that has been researched as a drug target for various parasites, including F. hepatica. The high-resolution crystal structure of F. hepatica TPI (FhTPI) has been solved at 1.51 Å resolution in its monoclinic form. The structure has been used to perform molecular-docking studies with the most successful fasciolocide triclabendazole (TCBZ), which has recently been suggested to target FhTPI. Two FhTPI residues, Lys50 and Asp51, are located at the dimer interface and are found in close proximity to the docked TCBZ. These residues are not conserved in mammalian hosts.

Source: Acta Crystallographica Section F Structural Biology Communications

DOI: 10.1107/s2053230x25006454

Authors: Georgios Kontellas, David J. Studholme, Mark van der Giezen, David J. Timson, Jennifer A. Littlechild, Michail N. Isupov

Institutions: University of Exeter, University of Stavanger, University of Brighton

Language: English

Topic: Helminth infection and control

Subfield: Small Animals

Field: Veterinary

Domain: Health Sciences

SDG: Good health and well-being

Open Access status: hybrid

Estimated APC paid: $3,520