1q4g

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{{STRUCTURE_1q4g| PDB=1q4g | SCENE= }}
{{STRUCTURE_1q4g| PDB=1q4g | SCENE= }}
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'''2.0 Angstrom Crystal Structure of Ovine Prostaglandin H2 Synthase-1, in complex with alpha-methyl-4-biphenylacetic acid'''
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===2.0 Angstrom Crystal Structure of Ovine Prostaglandin H2 Synthase-1, in complex with alpha-methyl-4-biphenylacetic acid===
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==Overview==
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Prostaglandin H2 synthase (EC 1.14.99.1) is an integral membrane enzyme containing a cyclooxygenase site, which is the target for the non-steroidal anti-inflammatory drugs, and a spatially distinct peroxidase site. Previous crystallographic studies of this clinically important drug target have been hindered by low resolution. We present here the 2.0 A resolution X-ray crystal structure of ovine prostaglandin H2 synthase-1 in complex with alpha-methyl-4-biphenylacetic acid, a defluorinated analog of the non-steroidal anti-inflammatory drug flurbiprofen. Detergent molecules are seen to bind to the protein's membrane-binding domain, and their positions suggest the depth to which this domain is likely to penetrate into the lipid bilayer. The relation of the enzyme's proximal heme ligand His388 to the heme iron is atypical for a peroxidase; the iron-histidine bond is unusually long and a substantial tilt angle is observed between the heme and imidazole planes. A molecule of glycerol, used as a cryoprotectant during diffraction experiments, is seen to bind in the peroxidase site, offering the first view of any ligand in this active site. Insights gained from glycerol binding may prove useful in the design of a peroxidase-specific ligand.
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(as it appears on PubMed at http://www.pubmed.gov), where 14672659 is the PubMed ID number.
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{{ABSTRACT_PUBMED_14672659}}
==About this Structure==
==About this Structure==
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[[Category: Peroxidase]]
[[Category: Peroxidase]]
[[Category: Prostaglandin synthase]]
[[Category: Prostaglandin synthase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 05:51:26 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Jul 27 19:59:51 2008''

Revision as of 16:59, 27 July 2008

Image:1q4g.png

Template:STRUCTURE 1q4g

2.0 Angstrom Crystal Structure of Ovine Prostaglandin H2 Synthase-1, in complex with alpha-methyl-4-biphenylacetic acid

Template:ABSTRACT PUBMED 14672659

About this Structure

1Q4G is a Single protein structure of sequence from Ovis aries. Full crystallographic information is available from OCA.

Reference

The 2.0 A resolution crystal structure of prostaglandin H2 synthase-1: structural insights into an unusual peroxidase., Gupta K, Selinsky BS, Kaub CJ, Katz AK, Loll PJ, J Mol Biol. 2004 Jan 9;335(2):503-18. PMID:14672659

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