1ht8

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[[Image:1ht8.jpg|left|200px]]<br /><applet load="1ht8" size="350" color="white" frame="true" align="right" spinBox="true"
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[[Image:1ht8.jpg|left|200px]]
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caption="1ht8, resolution 2.69&Aring;" />
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'''THE 2.7 ANGSTROM RESOLUTION MODEL OF OVINE COX-1 COMPLEXED WITH ALCLOFENAC'''<br />
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{{Structure
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|PDB= 1ht8 |SIZE=350|CAPTION= <scene name='initialview01'>1ht8</scene>, resolution 2.69&Aring;
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|SITE=
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|LIGAND= <scene name='pdbligand=NAG:N-ACETYL-D-GLUCOSAMINE'>NAG</scene>, <scene name='pdbligand=BOG:B-OCTYLGLUCOSIDE'>BOG</scene>, <scene name='pdbligand=HEM:PROTOPORPHYRIN+IX+CONTAINING+FE'>HEM</scene> and <scene name='pdbligand=34C:(3-CHLORO-4-PROPOXY-PHENYL)-ACETIC ACID'>34C</scene>
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|ACTIVITY= [http://en.wikipedia.org/wiki/Prostaglandin-endoperoxide_synthase Prostaglandin-endoperoxide synthase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=1.14.99.1 1.14.99.1]
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|GENE=
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}}
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'''THE 2.7 ANGSTROM RESOLUTION MODEL OF OVINE COX-1 COMPLEXED WITH ALCLOFENAC'''
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==Overview==
==Overview==
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==About this Structure==
==About this Structure==
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1HT8 is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Ovis_aries Ovis aries] with <scene name='pdbligand=NAG:'>NAG</scene>, <scene name='pdbligand=BOG:'>BOG</scene>, <scene name='pdbligand=HEM:'>HEM</scene> and <scene name='pdbligand=34C:'>34C</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/Prostaglandin-endoperoxide_synthase Prostaglandin-endoperoxide synthase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=1.14.99.1 1.14.99.1] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1HT8 OCA].
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1HT8 is a [[Single protein]] structure of sequence from [http://en.wikipedia.org/wiki/Ovis_aries Ovis aries]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1HT8 OCA].
==Reference==
==Reference==
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Structural analysis of NSAID binding by prostaglandin H2 synthase: time-dependent and time-independent inhibitors elicit identical enzyme conformations., Selinsky BS, Gupta K, Sharkey CT, Loll PJ, Biochemistry. 2001 May 1;40(17):5172-80. PMID:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=11318639 11318639]
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Structural analysis of NSAID binding by prostaglandin H2 synthase: time-dependent and time-independent inhibitors elicit identical enzyme conformations., Selinsky BS, Gupta K, Sharkey CT, Loll PJ, Biochemistry. 2001 May 1;40(17):5172-80. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/11318639 11318639]
[[Category: Ovis aries]]
[[Category: Ovis aries]]
[[Category: Prostaglandin-endoperoxide synthase]]
[[Category: Prostaglandin-endoperoxide synthase]]
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[[Category: peroxidase]]
[[Category: peroxidase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 13:04:39 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Mar 20 11:41:19 2008''

Revision as of 09:41, 20 March 2008

Image:1ht8.jpg


PDB ID 1ht8

Drag the structure with the mouse to rotate
, resolution 2.69Å
Ligands: , , and
Activity: Prostaglandin-endoperoxide synthase, with EC number 1.14.99.1
Coordinates: save as pdb, mmCIF, xml



THE 2.7 ANGSTROM RESOLUTION MODEL OF OVINE COX-1 COMPLEXED WITH ALCLOFENAC


Overview

Nonsteroidal antiinflammatory drugs (NSAIDs) block prostanoid biosynthesis by inhibiting prostaglandin H(2) synthase (EC 1.14.99.1). NSAIDs are either rapidly reversible competitive inhibitors or slow tight-binding inhibitors of this enzyme. These different modes of inhibition correlate with clinically important differences in isoform selectivity. Hypotheses have been advanced to explain the different inhibition kinetics, but no structural data have been available to test them. We present here crystal structures of prostaglandin H(2) synthase-1 in complex with the inhibitors ibuprofen, methyl flurbiprofen, flurbiprofen, and alclofenac at resolutions ranging from 2.6 to 2.75 A. These structures allow direct comparison of enzyme complexes with reversible competitive inhibitors (ibuprofen and methyl flurbiprofen) and slow tight-binding inhibitors (alclofenac and flurbiprofen). The four inhibitors bind to the same site and adopt similar conformations. In all four complexes, the enzyme structure is essentially unchanged, exhibiting only minimal differences in the inhibitor binding site. These results argue strongly against hypotheses that explain the difference between slow tight-binding and fast reversible competitive inhibition by invoking global conformational differences or different inhibitor binding sites. Instead, they suggest that the different apparent modes of NSAID binding may result from differences in the speed and efficiency with which inhibitors can perturb the hydrogen bonding network around Arg-120 and Tyr-355.

About this Structure

1HT8 is a Single protein structure of sequence from Ovis aries. Full crystallographic information is available from OCA.

Reference

Structural analysis of NSAID binding by prostaglandin H2 synthase: time-dependent and time-independent inhibitors elicit identical enzyme conformations., Selinsky BS, Gupta K, Sharkey CT, Loll PJ, Biochemistry. 2001 May 1;40(17):5172-80. PMID:11318639

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