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Drug developers are most interested in targeting PGHS-2, and Garavito's laboratory s trying to grow crystals of that form of the enzyme large enough to X-ray.
Efforts to design a new generation of anti-inflammatory pain killers focus on blocking PGHS-2, believed to be a more effective method with fewer side effects, Kulmacz says.
The directly prepared DCM-extract exhibited better activity against PGHS-2 (I[C.sub.50] = 4.0 [micro]g/ml) than against PGHS-1 (I[C.sub.50] = 17.6 [micro]g/ml).
The inducible isoenzyme PGHS-2 is stimulated by many pro-inflammatory agents and increases PGs biosynthesis rapidly at sites of inflammation (Seibert et al., 1994).
The second isoform is found in sheep placental cotyledones and its microsomal preparations have become a target for the discovery of selective PGHS-2 inhibitors (Johnson et al., 1995; Pairet and van'Ryn, 1998).
The assay was performed in a microtiter scale with purified PGHS-2 from sheep placental cotyledones (Cayman Chemical) (Johnson et al., 1995).
The determination of PGHS-1 inhibition was performed according to the PGHS-2 assay with 0.2 units purified PGHS-1 enzyme from ram seminal vesicles (Cayman Chemical), but without [Na.sub.2]EDTA and instead additional 10 [micro]l of 80 mM TRIS/HCl buffer (pH 8.0).
The presented assays are performed with purified PGHS-2 from sheep placental cotyledones (Johnson et al., 1995) and purified PGHS-1 from ram seminal vesicles, respectively, to achieve high specificity and comparability.
[Na.sub.2]EDTA protects PGHS-2 from inactivation by metalloproteases, but does not interfere with the enzyme activity.
The PGHS-1 and PGHS-2 assays are directly comparable, because both enzymes are purified and from the same species.
Known specific PGHS-2 inhibitors showed better inhibitory effects for PGHS-2 than PGHS-1 e.g.
They all exhibited inhibitory activity towards PGHS-1 and PGHS-2 in a similar range (Table 2).
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- PGI 2
- PGI 2
- PGI2-stimulating factor