1os0

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[[Image:1os0.jpg|left|200px]]
[[Image:1os0.jpg|left|200px]]
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{{Structure
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<!--
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|PDB= 1os0 |SIZE=350|CAPTION= <scene name='initialview01'>1os0</scene>, resolution 2.10&Aring;
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The line below this paragraph, containing "STRUCTURE_1os0", 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=DMS:DIMETHYL+SULFOXIDE'>DMS</scene>, <scene name='pdbligand=DPH:DEAMINO-METHYL-PHENYLALANINE'>DPH</scene>, <scene name='pdbligand=PPH:PHENYLALANINE+PHOSPHINIC+ACID'>PPH</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</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/Thermolysin Thermolysin], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.24.27 3.4.24.27] </span>
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or leave the SCENE parameter empty for the default display.
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|GENE=
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|DOMAIN=
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{{STRUCTURE_1os0| PDB=1os0 | SCENE= }}
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|RELATEDENTRY=[[1kei|1KEI]], [[2tmn|2TMN]], [[1qf0|1QF0]], [[1qf1|1QF1]], [[1qf2|1QF2]], [[1tlp|1TLP]]
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1os0 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1os0 OCA], [http://www.ebi.ac.uk/pdbsum/1os0 PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1os0 RCSB]</span>
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}}
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'''THERMOLYSIN WITH AN ALPHA-AMINO PHOSPHINIC INHIBITOR'''
'''THERMOLYSIN WITH AN ALPHA-AMINO PHOSPHINIC INHIBITOR'''
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[[Category: Selkti, M.]]
[[Category: Selkti, M.]]
[[Category: Tomas, A.]]
[[Category: Tomas, A.]]
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[[Category: alpha-amino phosphinic compound]]
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[[Category: Alpha-amino phosphinic compound]]
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[[Category: inhibition]]
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[[Category: Inhibition]]
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[[Category: neprylisin]]
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[[Category: Neprylisin]]
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[[Category: thermolysin]]
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[[Category: Thermolysin]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 04:12:42 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Mar 30 22:49:29 2008''
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Revision as of 01:12, 3 May 2008

Image:1os0.jpg

Template:STRUCTURE 1os0

THERMOLYSIN WITH AN ALPHA-AMINO PHOSPHINIC INHIBITOR


Overview

A new alpha-aminophosphinic compound able to inhibit both zinc-containing exopeptidases and endopeptidases has been crystallized with TLN as a model in order to investigate the mode of zinc recognition by the phosphinic moiety and to evaluate the potential role of the free alpha-amino group in the formation of enzyme-inhibitor complexes. In addition to the main interactions between the backbone of the inhibitor and the enzyme active site, it is observed that the phosphinic group acts as a distorted bidentate ligand for the zinc ion, while the free alpha-amino function does not directly participate in interactions within the active site. Association of the present data and the K(i) values of various analogues of the inhibitor towards TLN and neprilysin suggests differences in the hydrophobicity of the S(1)-S(2) domains of the enzymes. This could be taken into account in the design of selective inhibitors.

About this Structure

1OS0 is a Single protein structure of sequence from Bacillus thermoproteolyticus. Full crystallographic information is available from OCA.

Reference

Interactions of a new alpha-aminophosphinic derivative inside the active site of TLN (thermolysin): a model for zinc-metalloendopeptidase inhibition., Selkti M, Tomas A, Gaucher JF, Prange T, Fournie-Zaluski MC, Chen H, Roques BP, Acta Crystallogr D Biol Crystallogr. 2003 Jul;59(Pt 7):1200-5. Epub 2003, Jun 27. PMID:12832763 Page seeded by OCA on Sat May 3 04:12:42 2008

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OCA

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