2hhn: Difference between revisions

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[[Image:2hhn.jpg|left|200px]]
{{Seed}}
[[Image:2hhn.png|left|200px]]


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{{STRUCTURE_2hhn|  PDB=2hhn  |  SCENE=  }}  
{{STRUCTURE_2hhn|  PDB=2hhn  |  SCENE=  }}  


'''Cathepsin S in complex with non covalent arylaminoethyl amide.'''
===Cathepsin S in complex with non covalent arylaminoethyl amide.===




==Overview==
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The synthesis and structure-activity relationship of a series of arylaminoethyl amide cathepsin S inhibitors are reported. Optimization of P3 and P2 groups to improve overall physicochemical properties resulted in significant improvements in oral bioavailability over early lead compounds. An X-ray structure of compound 37 bound to the active site of cathepsin S is also reported.
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{{ABSTRACT_PUBMED_16876402}}


==About this Structure==
==About this Structure==
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[[Category: Noncovalent]]
[[Category: Noncovalent]]
[[Category: Protease]]
[[Category: Protease]]
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May  4 06:18:22 2008''
 
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 03:35:59 2008''

Revision as of 00:36, 28 July 2008

File:2hhn.png

Template:STRUCTURE 2hhn

Cathepsin S in complex with non covalent arylaminoethyl amide.

Template:ABSTRACT PUBMED 16876402

About this Structure

2HHN is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Synthesis and SAR of arylaminoethyl amides as noncovalent inhibitors of cathepsin S: P3 cyclic ethers., Tully DC, Liu H, Chatterjee AK, Alper PB, Epple R, Williams JA, Roberts MJ, Woodmansee DH, Masick BT, Tumanut C, Li J, Spraggon G, Hornsby M, Chang J, Tuntland T, Hollenbeck T, Gordon P, Harris JL, Karanewsky DS, Bioorg Med Chem Lett. 2006 Oct 1;16(19):5112-7. Epub 2006 Jul 28. PMID:16876402

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