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Dipeptide nitrile inhibitors of cathepsin K.

Altmann, Eva, Aichholz, Reiner, Betschart, Claudia, Buhl, Thomas, Green, Jonathan, 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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