Dipeptide nitrile inhibitors of cathepsin K |
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| Authors: | Altmann Eva Aichholz Reiner Betschart Claudia Buhl Thomas Green Jonathan Lattmann René Missbach Martin |
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| Affiliation: | Novartis Institutes for BioMedical Research, CH-4002 Basel, Switzerland. eva.altmann@novartis.com |
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| Abstract: | A series of dipeptidyl nitriles as inhibitors of cathepsin K have been explored starting from lead structure 1 (Cbz-Leu-NH-CH2-CN, IC50 = 39 nM). Attachment of non-natural amino acid side chains in P1 and modification of the P3 subunit led to inhibitors with higher potency and improved pharmacokinetic properties. |
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