1ms6: Difference between revisions

[[Image:1ms6.gif|left|200px]]<br /><applet load="1ms6" size="350" color="white" frame="true" align="right" spinBox="true"  

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.

1MS6 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=BLN:'>BLN</scene> as [http://en.wikipedia.org/wiki/ligand ligand]. 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=1MS6 OCA].  

[[Category: Brown, M L.]]

[[Category: Cywin, C L.]]

[[Category: Emmanuel, M J.]]

[[Category: Freeman, D M.]]

[[Category: Frye, L L.]]

[[Category: Grygon, C A.]]

[[Category: Hao, M H.]]

[[Category: Hopkins, J L.]]

[[Category: Labadia, M E.]]

[[Category: Spero, D M.]]

[[Category: Thomson, D S.]]

[[Category: Ward, Y D.]]

''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 13:58:32 2008''