Pub. Date : 2005 Mar
PMID : 15494548
8 Functional Relationships(s)Download |
Sentence | Compound Name | Protein Name | Organism |
| 1 | We report here the pharmacological properties of a third selective COX-2 inhibitor, valdecoxib, which is the most potent and in vitro selective of the marketed COX-2 inhibitors that we have studied. | valdecoxib | mitochondrially encoded cytochrome c oxidase II | Homo sapiens |
| 2 | We report here the pharmacological properties of a third selective COX-2 inhibitor, valdecoxib, which is the most potent and in vitro selective of the marketed COX-2 inhibitors that we have studied. | valdecoxib | mitochondrially encoded cytochrome c oxidase II | Homo sapiens |
| 3 | Valdecoxib potently inhibits recombinant COX-2, with an IC(50) of 0.005 microM; this compares with IC values of 0.05 microM for celecoxib, 0.5 microM for rofecoxib, and 5 microM for etoricoxib. | valdecoxib | mitochondrially encoded cytochrome c oxidase II | Homo sapiens |
| 4 | Unique binding interactions of valdecoxib with COX-2 translate into a fast rate of inactivation of COX-2 (110,000 M/s compared with 7000 M/s for rofecoxib and 80 M/s for etoricoxib). | valdecoxib | mitochondrially encoded cytochrome c oxidase II | Homo sapiens |
| 5 | Unique binding interactions of valdecoxib with COX-2 translate into a fast rate of inactivation of COX-2 (110,000 M/s compared with 7000 M/s for rofecoxib and 80 M/s for etoricoxib). | valdecoxib | mitochondrially encoded cytochrome c oxidase II | Homo sapiens |
| 6 | The overall saturation binding affinity for COX-2 of valdecoxib is 2.6 nM (compared with 1.6 nM for celecoxib, 51 nM for rofecoxib, and 260 nM for etoricoxib), with a slow off-rate (t(1/2) approximately 98 min). | valdecoxib | mitochondrially encoded cytochrome c oxidase II | Homo sapiens |
| 7 | Collectively, these data provide a mechanistic basis for the potency and in vitro selectivity of valdecoxib for COX-2. | valdecoxib | mitochondrially encoded cytochrome c oxidase II | Homo sapiens |
| 8 | Valdecoxib showed similar activity in the human whole-blood COX assay (COX-2 IC(50) = 0.24 microM; COX-1 IC(50) = 21.9 microM). | valdecoxib | mitochondrially encoded cytochrome c oxidase II | Homo sapiens |