3bc3

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[[Image:3bc3.jpg|left|200px]]
[[Image:3bc3.jpg|left|200px]]
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{{Structure
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<!--
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|PDB= 3bc3 |SIZE=350|CAPTION= <scene name='initialview01'>3bc3</scene>, resolution 2.200&Aring;
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The line below this paragraph, containing "STRUCTURE_3bc3", creates the "Structure Box" on the page.
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|SITE= <scene name='pdbsite=AC1:Opt+Binding+Site+For+Residue+A+300'>AC1</scene> and <scene name='pdbsite=AC2:Opt+Binding+Site+For+Residue+B+400'>AC2</scene>
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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|LIGAND= <scene name='pdbligand=CSW:CYSTEINE-S-DIOXIDE'>CSW</scene>, <scene name='pdbligand=OPT:S-BENZYL-N-(BIPHENYL-4-YLACETYL)-L-CYSTEINYL-N~5~-(DIAMINOMETHYL)-D-ORNITHYL-N-(2-PHENYLETHYL)-L-TYROSINAMIDE'>OPT</scene>
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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|ACTIVITY= <span class='plainlinks'>[http://en.wikipedia.org/wiki/Cathepsin_L Cathepsin L], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.22.15 3.4.22.15] </span>
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or leave the SCENE parameter empty for the default display.
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|GENE= CTSL ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])
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-->
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|DOMAIN=
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{{STRUCTURE_3bc3| PDB=3bc3 | SCENE= }}
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|RELATEDENTRY=[[1mhw|1MHW]]
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3bc3 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3bc3 OCA], [http://www.ebi.ac.uk/pdbsum/3bc3 PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=3bc3 RCSB]</span>
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}}
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'''Exploring inhibitor binding at the S subsites of cathepsin L'''
'''Exploring inhibitor binding at the S subsites of cathepsin L'''
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[[Category: Tulsidas, S R.]]
[[Category: Tulsidas, S R.]]
[[Category: Ziomek, E.]]
[[Category: Ziomek, E.]]
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[[Category: cathepsin l inhibitor binding at the s subsite]]
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[[Category: Cathepsin l inhibitor binding at the s subsite]]
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[[Category: glycoprotein]]
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[[Category: Glycoprotein]]
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[[Category: hydrolase]]
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[[Category: Hydrolase]]
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[[Category: lysosome]]
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[[Category: Lysosome]]
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[[Category: protease]]
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[[Category: Protease]]
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[[Category: thiol protease]]
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[[Category: Thiol protease]]
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[[Category: zymogen]]
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[[Category: Zymogen]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 20:37:20 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 05:24:58 2008''
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Revision as of 17:37, 4 May 2008

Image:3bc3.jpg

Template:STRUCTURE 3bc3

Exploring inhibitor binding at the S subsites of cathepsin L


Overview

We report a series of noncovalent, reversible inhibitors of cathepsin L that have been designed to explore additional binding interactions with the S' subsites. The design was based on our previously reported crystal structure that suggested the possibility of engineering increased interactions with the S' subsites ( Chowdhury et al. J. Med. Chem. 2002, 45, 5321-5329 ). A representative of these new inhibitors has been co-crystallized with mature cathepsin L, and the structure has been solved and refined at 2.2 A. The inhibitors described in this work extend farther into the S' subsites of cathepsins than any inhibitors reported in the literature thus far. These interactions appear to make use of a S3' subsite that can potentially be exploited for enhanced specificity and/or affinity.

About this Structure

3BC3 is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Exploring inhibitor binding at the s' subsites of cathepsin L., Chowdhury SF, Joseph L, Kumar S, Tulsidas SR, Bhat S, Ziomek E, Menard R, Sivaraman J, Purisima EO, J Med Chem. 2008 Mar 13;51(5):1361-8. Epub 2008 Feb 16. PMID:18278855 Page seeded by OCA on Sun May 4 20:37:20 2008

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OCA

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