TABLE 1

Binding properties of the chimeric receptor PTH1R-NT2 compared with wild type PTH-1R

Values represent mean pIC50 values ± S.E. for three independent competition binding assays using membrane preparations and four different unlabeled ligands with 125I-rPTH(1-34) as the tracer. The values are compared using d1, d2, or d3 which represent the -fold change in mean IC50 values, where d1 compares PTHrP(1-36) relative to PTH(1-34), d2 compares Phe23-PTH(1-34) relative to PTH(1-34), and d3 compares PTHrP(1-36) relative to Trp23-PTHrP(1-36). d1, d2, and d3 values for PTH-2R from whole cell binding were 213, 72 and 25, respectively (from Figure 2), or 134, 28 and 71, respectively (from Gardella et al., 1996).

PTH(1-34) PTHrP(1-36) d1 Phe23-PTH(1-34) d2 Trp23-PTHrP(1-36) d3
PTH-1R 8.02 ± 0.17 6.81 ± 0.29 16 6.99 ± 0.21 11 7.65 ± 0.15 7
PTH1R-NT2 8.45 ± 0.13 6.01 ± 0.05 277 6.42 ± 0.19 108 8.10 ± 0.25 124