Identification and characterization of the novel reversible and selective cathepsin X inhibitors

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ID: 58845
2017
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Abstract
Abstract Cathepsin X is a cysteine peptidase involved in the progression of cancer and neurodegenerative diseases. Targeting this enzyme with selective inhibitors opens a new possibility for intervention in several therapeutic areas. In this study triazole-based reversible and selective inhibitors of cathepsin X have been identified. Their selectivity and binding is enhanced when the 2,3-dihydrobenzo[b][1,4]dioxine moiety is present as the R1 substituent. Of a series of selected triazole-benzodioxine derivatives, compound 22 is the most potent inhibitor of cathepsin X carboxypeptidase activity (Ki = 2.45 ± 0.05 μM) with at least 100-fold greater selectivity in comparison to cathepsin B or other related cysteine peptidases. Compound 22 is not cytotoxic to prostate cancer cells PC-3 or pheochromocytoma PC-12 cells at concentrations up to 10 μM. It significantly inhibits the migration of tumor cells and increases the outgrowth of neurites, both processes being under the control of cathepsin X carboxypeptidase activity. Compound 22 and other characterized triazole-based inhibitors thus possess a great potential for further development resulting in several in vivo applications.
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fonovic2017identificationscientific Use this key to autocite in the manuscript while using SciMatic Manuscript Manager or Thesis Manager
Authors Fonović, Urša Pečar;Mitrović, Ana;Knez, Damijan;Jakoš, Tanja;Pišlar, Anja;Brus, Boris;Doljak, Bojan;Stojan, Jure;Žakelj, Simon;Trontelj, Jurij;Gobec, Stanislav;Kos, Janko;
Journal Scientific reports
Year 2017
DOI
DOI not found
URL
http://link.springer.com/article/10.1038/s41598-017-11935-1
Keywords
chemistry Biology (General) Medicine Science

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