1ms6

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{{STRUCTURE_1ms6| PDB=1ms6 | SCENE= }}
{{STRUCTURE_1ms6| PDB=1ms6 | SCENE= }}
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'''Dipeptide Nitrile Inhibitor Bound to Cathepsin S.'''
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===Dipeptide Nitrile Inhibitor Bound to Cathepsin S.===
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==Overview==
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The specificity of the immune response relies on processing of foreign proteins and presentation of antigenic peptides at the cell surface. Inhibition of antigen presentation, and the subsequent activation of T-cells, should, in theory, modulate the immune response. The cysteine protease Cathepsin S performs a fundamental step in antigen presentation and therefore represents an attractive target for inhibition. Herein, we report a series of potent and reversible Cathepsin S inhibitors based on dipeptide nitriles. These inhibitors show nanomolar inhibition of the target enzyme as well as cellular potency in a human B cell line. The first X-ray crystal structure of a reversible inhibitor cocrystallized with Cathepsin S is also reported.
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(as it appears on PubMed at http://www.pubmed.gov), where 12459015 is the PubMed ID number.
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{{ABSTRACT_PUBMED_12459015}}
==About this Structure==
==About this Structure==
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[[Category: Hydrolase]]
[[Category: Hydrolase]]
[[Category: Protease]]
[[Category: Protease]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 01:39:32 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 15:41:35 2008''

Revision as of 12:41, 28 July 2008

Image:1ms6.png

Template:STRUCTURE 1ms6

Dipeptide Nitrile Inhibitor Bound to Cathepsin S.

Template:ABSTRACT PUBMED 12459015

About this Structure

1MS6 is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Design and synthesis of dipeptide nitriles as reversible and potent Cathepsin S inhibitors., Ward YD, Thomson DS, Frye LL, Cywin CL, Morwick T, Emmanuel MJ, Zindell R, McNeil D, Bekkali Y, Girardot M, Hrapchak M, DeTuri M, Crane K, White D, Pav S, Wang Y, Hao MH, Grygon CA, Labadia ME, Freeman DM, Davidson W, Hopkins JL, Brown ML, Spero DM, J Med Chem. 2002 Dec 5;45(25):5471-82. PMID:12459015

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