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2hhn

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(New page: 200px<br /> <applet load="2hhn" size="450" color="white" frame="true" align="right" spinBox="true" caption="2hhn, resolution 1.55&Aring;" /> '''Cathepsin S in comp...)
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[[Image:2hhn.gif|left|200px]]<br />
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<applet load="2hhn" size="450" color="white" frame="true" align="right" spinBox="true"
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caption="2hhn, resolution 1.55&Aring;" />
caption="2hhn, resolution 1.55&Aring;" />
'''Cathepsin S in complex with non covalent arylaminoethyl amide.'''<br />
'''Cathepsin S in complex with non covalent arylaminoethyl amide.'''<br />
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==About this Structure==
==About this Structure==
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2HHN is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with SO4 and GNQ as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/Cathepsin_S Cathepsin S], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.22.27 3.4.22.27] Full crystallographic information is available from [http://ispc.weizmann.ac.il/oca-bin/ocashort?id=2HHN OCA].
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2HHN is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with <scene name='pdbligand=SO4:'>SO4</scene> and <scene name='pdbligand=GNQ:'>GNQ</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/Cathepsin_S Cathepsin S], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.22.27 3.4.22.27] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2HHN OCA].
==Reference==
==Reference==
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[[Category: protease]]
[[Category: protease]]
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''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Mon Nov 12 22:32:50 2007''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Jan 23 15:20:38 2008''

Revision as of 13:20, 23 January 2008

Image:2hhn.jpg

2hhn, resolution 1.55Å

Drag the structure with the mouse to rotate

Cathepsin S in complex with non covalent arylaminoethyl amide.

Overview

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.

About this Structure

2HHN is a Single protein structure of sequence from Homo sapiens with and as ligands. Active as Cathepsin S, with EC number 3.4.22.27 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

Page seeded by OCA on Wed Jan 23 15:20:38 2008

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