Pub. Date : 1995
PMID : 8587470
4 Functional Relationships(s)Download |
Sentence | Compound Name | Protein Name | Organism |
1 | The structure-activity relationships of phosphoramidon analogues for inhibition of endothelin-converting enzyme (ECE), neutral endopeptidase 24.11 (NEP), and angiotensin-converting enzyme (ACE) were compared. | phosphoramidon | endothelin converting enzyme 1 | Homo sapiens |
2 | Phosphoramidon inhibited ECE, NEP, and ACE activities with IC50 values of 3.5, 0.034, and 78 microM, respectively. | phosphoramidon | endothelin converting enzyme 1 | Homo sapiens |
3 | Removal of the rhamnose moiety of phosphoramidon (dipeptide 3) reduced the potency for ECE (IC50 = 70 microM), whereas the potencies for NEP (0.003 microM) and ACE (0.20 microM) were increased. | phosphoramidon | endothelin converting enzyme 1 | Homo sapiens |
4 | These results suggest that a hydrophobic group in the P1 position of phosphoramidon analogues increases the potency for ECE significantly, whereas compounds containing a free phosphonic acid are optimal for inhibition of NEP and ACE. | phosphoramidon | endothelin converting enzyme 1 | Homo sapiens |