1tlo

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[[Image:1tlo.jpg|left|200px]]
[[Image:1tlo.jpg|left|200px]]
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{{Structure
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<!--
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|PDB= 1tlo |SIZE=350|CAPTION= <scene name='initialview01'>1tlo</scene>, resolution 1.9&Aring;
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The line below this paragraph, containing "STRUCTURE_1tlo", creates the "Structure Box" on the page.
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|SITE=
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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=CA:CALCIUM+ION'>CA</scene>, <scene name='pdbligand=E64:N-[N-[1-HYDROXYCARBOXYETHYL-CARBONYL]LEUCYLAMINO-BUTYL]-GUANIDINE'>E64</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/Calpain-1 Calpain-1], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.22.52 3.4.22.52] </span>
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or leave the SCENE parameter empty for the default display.
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|GENE= CAPN1, CLS1 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=10116 Rattus norvegicus])
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-->
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|DOMAIN=
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{{STRUCTURE_1tlo| PDB=1tlo | SCENE= }}
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|RELATEDENTRY=[[1kxr|1KXR]], [[1mdw|1MDW]], [[1dfo|1DFO]], [[1kfu|1KFU]], [[1kfx|1KFX]], [[1nx0|1NX0]], [[1tl9|1TL9]]
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1tlo FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1tlo OCA], [http://www.ebi.ac.uk/pdbsum/1tlo PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1tlo RCSB]</span>
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}}
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'''High resolution crystal structure of calpain I protease core in complex with E64'''
'''High resolution crystal structure of calpain I protease core in complex with E64'''
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[[Category: Davies, P L.]]
[[Category: Davies, P L.]]
[[Category: Moldoveanu, T.]]
[[Category: Moldoveanu, T.]]
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[[Category: covalently-linked inhibitor at the active site (cysteine 115) forms a thioester]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 10:06:09 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Mar 30 23:57:52 2008''
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Revision as of 07:06, 3 May 2008

Image:1tlo.jpg

Template:STRUCTURE 1tlo

High resolution crystal structure of calpain I protease core in complex with E64


Overview

The endogenous calpain inhibitor, calpastatin, modulates some patho-physiological aspects of calpain signaling. Excess calpain can escape this inhibition and as well, many calpain isoforms and autolytically generated protease core fragments are not inhibited by calpastatin. There is a need, therefore, to develop specific, cell-permeable calpain inhibitors to block uncontrolled proteolysis and prevent tissue damage during brain and heart ischemia, spinal-cord injury and Alzheimer's diseases. Here, we report the first high-resolution crystal structures of rat mu-calpain protease core complexed with two traditional, low molecular mass inhibitors, leupeptin and E64. These structures show that access to a slightly deeper, but otherwise papain-like active site is gated by two flexible loops. These loops are divergent among the calpain isoforms giving a potential structural basis for substrate/inhibitor selectivity over other papain-like cysteine proteases and between members of the calpain family.

About this Structure

1TLO is a Single protein structure of sequence from Rattus norvegicus. Full crystallographic information is available from OCA.

Reference

Crystal structures of calpain-E64 and -leupeptin inhibitor complexes reveal mobile loops gating the active site., Moldoveanu T, Campbell RL, Cuerrier D, Davies PL, J Mol Biol. 2004 Nov 5;343(5):1313-26. PMID:15491615 Page seeded by OCA on Sat May 3 10:06:09 2008

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OCA

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