Ki values obtained for enzyme inhibition and competition binding of LVV-hemorphin-7 analogs with recombinant human IRAP
| Peptide | Enzyme InhibitionKi | Competition BindingKi |
|---|---|---|
| nM | ||
| Val-Tyr-Pro-Trp-Thr-Gln-Arg-Phe | 56 | 1.0 |
| Val-Tyr-Pro-Trp-Thr | 112 | 11 |
| LVV-hemorphin-7 | 196 | 55 |
| Leu-Val-Val-Tyr-Pro-Trp-Thr | 560 | 73 |
| Val-Tyr-Pro | 620 | 3100 |
| Leu-Val-Val-Tyr | N.D. | 3400 |
Competition binding studies on [125I]-Ang IV binding to crude membranes in the presence of LVV-H7 analogs was performed as described under Materials and Methods. IRAP enzymatic activity was determined by the hydrolysis of the synthetic substrate, Leu-β-NA in the presence or absence of LVV-H7 analogs (n = 3 for each peptide).
N.D., not detected.