Table 4. Binding characteristics of the radiolabeled GHRH antagonist JV-1-42 and GHRH analog [His1, Nle27]hGH-RH(1-32)NH2 for human cancer lines grown in nude mice.
| JV-1-42
|
[His1, Nle27]hGH-RH(1-32)NH2
|
|||
|---|---|---|---|---|
| Tumors | Kd | Bmax | Kd | Bmax |
| HT | 6.95 ± 0.21 | 384.7 ± 1.45 | 8.75 ± 0.16 | 290.8 ± 13.5 |
| RL | 4.11 ± 0.04 | 301.2 ± 19.5 | 4.60 ± 0.21 | 203.0 ± 5.6 |
| MiaPaCa-2 | 8.24 ± 0.40 | 523.3 ± 24.4 | ND | ND |
| H82 | 5.25 ± 0.21 | 364.2 ± 10.6 | 12.1 ± 0.95 | 320.9 ± 19.2 |
| H345 | 9.15 | 499.3 | 4.92 | 1,158.2 |
| DBTRG-05 | 1.07 ± 0.09 | 156.6 ± 8.80 | 14.3 ± 0.15 | 79.7 ± 10.3 |
Shown are values for the dissociation constant, Kd, expressed in nM (mean ± SD) and maximal binding capacity, Bmax, expressed as fmol per mg of protein (mean ± SD). ND, not detected.