1yt7

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[[Image:1yt7.gif|left|200px]]
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{{STRUCTURE_1yt7| PDB=1yt7 | SCENE= }}
{{STRUCTURE_1yt7| PDB=1yt7 | SCENE= }}
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'''Cathepsin K complexed with a constrained ketoamide inhibitor'''
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===Cathepsin K complexed with a constrained ketoamide inhibitor===
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==Overview==
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An orally bioavailable series of ketoamide-based cathepsin K inhibitors with good pharmacokinetic properties has been identified. Starting from a potent inhibitor endowed with poor drug properties, conformational constraint of the P(2)-P(3) linker and modifications to P(1') elements led to an enhancement in potency, solubility, clearance, and bioavailability. These optimized inhibitors attenuated bone resorption in a rat TPTX hypocalcemic bone resorption model.
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(as it appears on PubMed at http://www.pubmed.gov), where 15982880 is the PubMed ID number.
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{{ABSTRACT_PUBMED_15982880}}
==About this Structure==
==About this Structure==
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[[Category: Cathepsin]]
[[Category: Cathepsin]]
[[Category: Cysteine protease]]
[[Category: Cysteine protease]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 16:45:26 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul 29 01:30:50 2008''

Revision as of 22:31, 28 July 2008

Image:1yt7.png

Template:STRUCTURE 1yt7

Cathepsin K complexed with a constrained ketoamide inhibitor

Template:ABSTRACT PUBMED 15982880

About this Structure

1YT7 is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

P2-P3 conformationally constrained ketoamide-based inhibitors of cathepsin K., Barrett DG, Boncek VM, Catalano JG, Deaton DN, Hassell AM, Jurgensen CH, Long ST, McFadyen RB, Miller AB, Miller LR, Payne JA, Ray JA, Samano V, Shewchuk LM, Tavares FX, Wells-Knecht KJ, Willard DH Jr, Wright LL, Zhou HQ, Bioorg Med Chem Lett. 2005 Aug 1;15(15):3540-6. PMID:15982880

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