1csb

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{{STRUCTURE_1csb| PDB=1csb | SCENE= }}
{{STRUCTURE_1csb| PDB=1csb | SCENE= }}
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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'''
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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===
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==Overview==
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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.
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{{ABSTRACT_PUBMED_7718586}}
==About this Structure==
==About this Structure==
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[[Category: Turk, D.]]
[[Category: Turk, D.]]
[[Category: Papain-like lysosomal dicarboxy-peptidase]]
[[Category: Papain-like lysosomal dicarboxy-peptidase]]
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Revision as of 18:16, 30 June 2008

Image:1csb.png

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

Template:ABSTRACT PUBMED 7718586

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

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