Pub. Date : 1999 Feb 8
PMID : 10091674
5 Functional Relationships(s)Download |
Sentence | Compound Name | Protein Name | Organism |
| 1 | Structure-based design of COX-2 selectivity into flurbiprofen. | Flurbiprofen | mitochondrially encoded cytochrome c oxidase II | Homo sapiens |
| 2 | Comparative computer modeling of the X-ray crystal structures of cyclooxygenase isoforms COX-1 and COX-2 has led to the design of COX-2 selectivity into the nonselective inhibitor flurbiprofen. | Flurbiprofen | mitochondrially encoded cytochrome c oxidase II | Homo sapiens |
| 3 | Comparative computer modeling of the X-ray crystal structures of cyclooxygenase isoforms COX-1 and COX-2 has led to the design of COX-2 selectivity into the nonselective inhibitor flurbiprofen. | Flurbiprofen | mitochondrially encoded cytochrome c oxidase II | Homo sapiens |
| 4 | The COX-2 modeling was based on a postulated binding mode for flurbiprofen and took advantage of a small alcove in the COX-2 active site created by different positions of the Leu384 sidechain between COX-1 and COX-2. | Flurbiprofen | mitochondrially encoded cytochrome c oxidase II | Homo sapiens |
| 5 | The design hypothesis was tested by synthesis and biological assay of a series of flurbiprofen analogs, culminating in the discovery of several inhibitors having up to 78-fold selectivity for COX-2 over COX-1. | Flurbiprofen | mitochondrially encoded cytochrome c oxidase II | Homo sapiens |