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

• Main Authors: Jakub Benýšek (Author), Michal Buša (Author), Petra Rubešová (Author), Jindřich Fanfrlík (Author), Martin Lepšík (Author), Jiří Brynda (Author), Zuzana Matoušková (Author), Ulrike Bartz (Author), Martin Horn (Author), Michael Gütschow (Author), Michael Mareš (Author)
• Format: Book
• Published: Taylor & Francis Group, 2022-12-01T00:00:00Z.
• Subjects: article
• Online Access: Connect to this object online.

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...