biostudies-literaturePhan TNKorean government (MSIT)National Research Foundation of Korea1835https://www.ebi.ac.uk/biostudies/studies/S-EPMC11054337biostudies-literatureUnknown29(8)Leishmaniasis, an infectious disease caused by pathogenic <i>Leishmania</i> parasites, affects millions of people in developing countries, and its re-emergence in developed countries, particularly in Europe, poses a growing public health concern. The limitations of current treatments and the absence of effective vaccines necessitate the development of novel therapeutics. In this study, we focused on identifying small molecule inhibitors which prevents the interaction between peroxin 5 (PEX5) and peroxisomal targeting signal 1 (PTS1), pivotal for kinetoplastid parasite survival. The <i>Leishmania donovani</i> PEX5, containing a C-terminal tetratricopeptide repeat (TPR) domain, was expressed and purified, followed by the quantification of kinetic parameters of PEX5-PTS1 interactions. A fluorMolecules (Basel, Switzerland)Identification of <i>Leishmania donovani</i> PEX5-PTS1 Interaction Inhibitors through Fluorescence Polarization-Based High-Throughput Screening.PMC11054337NRF-2023M3A9G6057281Shum DNo JHPhan TNPark KPfalseIdentification of <i>Leishmania donovani</i> PEX5-PTS1 Interaction Inhibitors through Fluorescence Polarization-Based High-Throughput Screening.Leishmaniasis, an infectious disease caused by pathogenic <i>Leishmania</i> parasites, affects millions of people in developing countries, and its re-emergence in developed countries, particularly in Europe, poses a growing public health concern. The limitations of current treatments and the absence of effective vaccines necessitate the development of novel therapeutics. In this study, we focused on identifying small molecule inhibitors which prevents the interaction between peroxin 5 (PEX5) and peroxisomal targeting signal 1 (PTS1), pivotal for kinetoplastid parasite survival. The <i>Leishmania donovani</i> PEX5, containing a C-terminal tetratricopeptide repeat (TPR) domain, was expressed and purified, followed by the quantification of kinetic parameters of PEX5-PTS1 interactions. A fluor2024-01-01T00:00:00Z2024 Apr2026-04-24T03:14:45.984Z2026-04-24T03:09:36.41ZS-EPMC110543373867565310.3390/molecules29081835