TABLE 2.
Ligand binding, whole cell analysis, and CTR ECD
pIC50 values, mean ± S.E. from whole cell competition binding assay using 25 pm 125I-sCT as the tracer ligand and increasing amounts of unlabeled calcitonin analogue. Experiments were conducted on intact BHK cells stably transfected with the human calcitonin receptor. Experimental details can be found under “Experimental Procedures.” Representative data are depicted in Fig. 4. Number of experiments = 3 for all measurements.
Peptide | Ligand binding, whole cell analysis |
Ligand binding, CTR ECD |
||||
---|---|---|---|---|---|---|
pIC50 | S.E. | IC50 | pIC50 | S.E. | IC50 | |
nm | nm | |||||
Pramlintide | 6.99 | ±0.08 | 100 | >10,000 | ||
sCT | 9.67 | ±0.06 | 0.21 | 7.4 | ±0.06 | 40 |
sCT(8–32) | 9.55 | ±0.14 | 0.28 | 7.3 | ±0.11 | 50 |
[Tyr32]sCT(8–32) | 7.94 | ±0.11 | 12 | >10,000 | ||
[BrPhe22]sCT(8–32) | 9.38 | ±0.13 | 0.42 | 7.1 | ±0.13 | 80 |
hCT | 8.28 | ±0.26 | 5.2 | >10,000 |