High-Throughput Sampling of Chemical Space to Explore Inhibition of a Cancer-Associated Protease

Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F61388963%3A_____%2F23%3A00618332" target="_blank" >RIV/61388963:_____/23:00618332 - isvavai.cz</a>
Result on the web
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DOI - Digital Object Identifier
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Result language
angličtina
Original language name
High-Throughput Sampling of Chemical Space to Explore Inhibition of a Cancer-Associated Protease
Original language description
This study investigates the inhibition of Fibroblast Activation Protein (FAP), a serine protease overexpressed in more than 90% of epithelial tumors but minimally present in healthy tissues. Using high-throughput sampling and direct testing of reaction mixtures, we identified potent peptidomimetic inhibitors with an α-ketoamide warhead, opening new P' positions for exploration. The DIANA assay enabled the determination of inhibition constants (Ki) directly from reaction mixtures, demonstrating that the inhibition potency remains consistent with pure compounds. This approach facilitates rapid and efficient screening, making FAP a promising target for cancer diagnostics and therapy.
Czech name
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Czech description
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Project
Result was created during the realization of more than one project. More information in the Projects tab.
Continuities
I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace

Publication year
2023
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

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