Highly potent inhibitors of cathepsin K with a differently positioned cyanohydrazide warhead: structural analysis of binding mode to mature and zymogen-like enzymes

Highly potent inhibitors of cathepsin K with a differently positioned cyanohydrazide warhead: structural analysis of binding mode to mature and zymogen-like enzymes

Cathepsin K (CatK) is a target for the treatment of osteoporosis, arthritis, and bone metastasis. Peptidomimetics with a cyanohydrazide warhead represent a new class of highly potent CatK inhibitors; however, their binding mechanism is unknown. We investigated two model cyanohydrazide inhibitors wit...

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Bibliographic Details
Main Authors: Jakub Benýšek, Michal Buša, Petra Rubešová, Jindřich Fanfrlík, Martin Lepšík, Jiří Brynda, Zuzana Matoušková, Ulrike Bartz, Martin Horn, Michael Gütschow, Michael Mareš
Format: Article
Language:English
Published: Taylor & Francis Group 2022-12-01
Series:Journal of Enzyme Inhibition and Medicinal Chemistry
Subjects:
cathepsin k
protease inhibitor
cyanohydrazide warhead
azadipeptide nitrile
 structure
Online Access:http://dx.doi.org/10.1080/14756366.2021.2024527

Internet

http://dx.doi.org/10.1080/14756366.2021.2024527

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