TABLE 2

Binding properties of mutant receptors compared with wild type PTH-1R

Values represent mean pIC50 values ± S.E. for three independent competition binding assays using two unlabeled ligands with 125I-rPTH(1-34) as the tracer. The values are compared using d1, which represents the -fold change in the mean IC50 value of PTHrP(1-36) relative to PTH(1-34).

PTH(1-34) PTHrP(1-36) d1
PTH-1R 8.02 ± 0.17 6.81 ± 0.29 16
YL23/25RQ 8.47 ± 0.24 6.83 ± 0.08 44
VA26/28LS 8.10 ± 0.06 6.86 ± 0.08 17
DV30/31GT 8.28 ± 0.16 6.63 ± 0.17 45
MK32/34II 8.15 ± 0.12 7.02 ± 0.09 13
FL39/41VV 8.46 ± 0.20 5.71 ± 0.14 558
HR42/43LK 8.14 ± 0.17 6.85 ± 0.34 20
F39V 7.97 ± 0.09 6.54 ± 0.19 27
L41V 8.40 ± 0.18 5.43 ± 0.02 935