1pge
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PROSTAGLANDIN H2 SYNTHASE-1 COMPLEXED WITH P-(2'-IODO-5'-THENOYL)HYDROTROPIC ACID (IODOSUPROFEN)
OverviewOverview
The cyclooxygenase activity of the membrane protein prostaglandin H2, synthase isoform 1 (PGHS-1) is the target of the nonsteroidal, antiinflammatory drugs (NSAIDs). The X-ray crystal structures of PGHS-1 in, complex with the NSAIDs flurbiprofen and bromoaspirin have been determined, previously [Picot, D., et al. (1994) Nature 367, 243-249; Loll, P. J., et, al. (1995) Nat. Struct. Biol. 2, 637-643]. We report here the preparation, and characterization of novel potent iodinated analogs of the NSAIDs, indomethacin and suprofen, as well as the refined X-ray crystal structures, of their complexes with PGHS-1. The PGHS-iodosuprofen complex structure, has been refined at 3.5 A to an R-value of 0.189 and shows the suprofen, analog to share a common mode of binding with flurbiprofen. The, ... [(full description)]
About this StructureAbout this Structure
1PGE is a [Single protein] structure of sequence from [Ovis aries] with NAG, BOG, HEM and ISF as [ligands]. Active as [[1]], with EC number [1.14.99.1]. Full crystallographic information is available from [OCA].
ReferenceReference
Synthesis and use of iodinated nonsteroidal antiinflammatory drug analogs as crystallographic probes of the prostaglandin H2 synthase cyclooxygenase active site., Loll PJ, Picot D, Ekabo O, Garavito RM, Biochemistry. 1996 Jun 11;35(23):7330-40. PMID:8652509
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