期刊
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
卷 34, 期 1, 页码 333-342出版社
TAYLOR & FRANCIS LTD
DOI: 10.1080/14756366.2018.1550752
关键词
Leishmania; superoxide dismutase; thiazole derivatives; thermal shift assay
资金
- Conselho Nacional de Desenvolvimento Cientifico e Tecnologico [CNPq 479160/2013-9]
Leishmaniasis is considered as one of the major neglected tropical diseases due to its magnitude and wide geographic distribution. Leishmania braziliensis, responsible for cutaneous leishmaniasis, is the most prevalent species in Brazil. Superoxide dismutase (SOD) belongs to the antioxidant pathway of the parasites and human host. Despite the differences between SOD of Leishmania braziliensis and human make this enzyme a promising target for drug development efforts. No medicinal chemistry effort has been made to identify LbSOD inhibitors. Herein, we show that thermal shift assays (TSA) and fluorescent protein-labeled assays (FPLA) can be employed as primary and secondary screens to achieve this goal. Moreover, we show that thiazole derivatives bind to LbSOD with micromolar affinity.
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