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Dipeptide nitrile inhibitors of cathepsin K.

Altmann, Eva and Aichholz, Reiner and Betschart, Claudia and Buhl, Thomas and Green, Jonathan and Lattmann, Rene and Missbach, Martin (2006) Dipeptide nitrile inhibitors of cathepsin K. Bioorganic & Medicinal Chemistry Letters, 16 (9). pp. 2549-2554. ISSN 0960-894X


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.

Item Type: Article
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Additional Information: author can archive post-print (ie final draft post-refereeing); Publisher's version/PDF cannot be used
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Date Deposited: 14 Dec 2009 14:00
Last Modified: 31 Jan 2013 01:17


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