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1csb

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[[Image:1csb.gif|left|200px]]
[[Image:1csb.gif|left|200px]]
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{{Structure
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|PDB= 1csb |SIZE=350|CAPTION= <scene name='initialview01'>1csb</scene>, resolution 2.0&Aring;
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The line below this paragraph, containing "STRUCTURE_1csb", creates the "Structure Box" on the page.
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|SITE=
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|LIGAND= <scene name='pdbligand=EOH:ETHANOL'>EOH</scene>, <scene name='pdbligand=EPO:1-OXO-(2-HYDROXYBUTYL)-4-OXO+GROUP'>EPO</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_B Cathepsin B], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.22.1 3.4.22.1] </span>
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{{STRUCTURE_1csb| PDB=1csb | SCENE= }}
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|RELATEDENTRY=
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1csb FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1csb OCA], [http://www.ebi.ac.uk/pdbsum/1csb PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1csb RCSB]</span>
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}}
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'''CRYSTAL STRUCTURE OF CATHEPSIN B INHIBITED WITH CA030 AT 2.1 ANGSTROMS RESOLUTION: A BASIS FOR THE DESIGN OF SPECIFIC EPOXYSUCCINYL INHIBITORS'''
'''CRYSTAL STRUCTURE OF CATHEPSIN B INHIBITED WITH CA030 AT 2.1 ANGSTROMS RESOLUTION: A BASIS FOR THE DESIGN OF SPECIFIC EPOXYSUCCINYL INHIBITORS'''
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[[Category: Bode, W.]]
[[Category: Bode, W.]]
[[Category: Turk, D.]]
[[Category: Turk, D.]]
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[[Category: papain-like lysosomal dicarboxy-peptidase]]
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[[Category: Papain-like lysosomal dicarboxy-peptidase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri May 2 13:03:58 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Mar 30 19:27:37 2008''
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Revision as of 10:03, 2 May 2008

Image:1csb.gif

Template:STRUCTURE 1csb

CRYSTAL STRUCTURE OF CATHEPSIN B INHIBITED WITH CA030 AT 2.1 ANGSTROMS RESOLUTION: A BASIS FOR THE DESIGN OF SPECIFIC EPOXYSUCCINYL INHIBITORS


Overview

Crystals of cysteine protease human cathepsin B inhibited with CA030 (ethyl ester of epoxysuccinyl-Ile-Pro-OH) [Murata, M., et al. (1991) FEBS Lett. 280, 307-310; Towatari, T., et al. (1991) FEBS Lett. 280, 311-315] were isomorphous to a previous published structure of cathepsin B [Musil, D., et al. (1991) EMBO J. 10, 2321-2330]. The crystal structure of the complex was refined at 2.0-A resolution to an R-value of 0.194. CA030 is well-defined in the electron density. The Ile-Pro-OH part of CA030 mimics a substrate P1' and P2' residues. The structure thus reveals for the first time a substratelike interaction in the S1' and S2' sites of a papain-like cysteine protease. The CA030 ethyl ester group occupies the S2 site. The structure confirms the role of residues His 110 and His 111 as the receptors of a peptidic substrate C-terminal carboxylic group. The structure suggests that an epoxysuccinyl fragment can be used to extend binding into primed and nonprimed substrate binding sites of a papain-like cysteine protease.

About this Structure

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

Reference

Crystal structure of cathepsin B inhibited with CA030 at 2.0-A resolution: A basis for the design of specific epoxysuccinyl inhibitors., Turk D, Podobnik M, Popovic T, Katunuma N, Bode W, Huber R, Turk V, Biochemistry. 1995 Apr 11;34(14):4791-7. PMID:7718586 Page seeded by OCA on Fri May 2 13:03:58 2008

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