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2bdl

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Image:2bdl.gif

2bdl, resolution 2.0Å

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Cathepsin K complexed with a pyrrolidine ketoamide-based inhibitor

Contents

Overview

Starting from a potent pantolactone ketoamide cathepsin K inhibitor, discovered from structural screening, conversion of the lactone scaffold, to a pyrrolidine scaffold allowed exploration of the S(3) subsite of, cathepsin K. Manipulation of P3 and P1' groups afforded potent inhibitors, with drug-like properties.

Disease

Known disease associated with this structure: Pycnodysostosis OMIM:[601105]

About this Structure

2BDL is a Single protein structure of sequence from Homo sapiens with 4PR as ligand. Active as Cathepsin K, with EC number 3.4.22.38 Full crystallographic information is available from OCA.

Reference

Novel, potent P2-P3 pyrrolidine derivatives of ketoamide-based cathepsin K inhibitors., Barrett DG, Catalano JG, Deaton DN, Hassell AM, Long ST, Miller AB, Miller LR, Ray JA, Samano V, Shewchuk LM, Wells-Knecht KJ, Willard DH Jr, Wright LL, Bioorg Med Chem Lett. 2006 Mar 15;16(6):1735-9. Epub 2006 Jan 11. PMID:16376075

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