Effects of exocyclic modifications in U-II on the binding of [125I-Tyr9]hU-II on the human and rat U-II receptor
Binding assay using membranes isolated from a stable HEK293 cell line expressing the U-II receptor.
Peptide | Structure | Human U-II Receptor | Rat U-II Receptor | ||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|
| Ki ±
S.E.M.a | nH ± S.E.M.
| n
b
| Ki ±
S.E.M.a | nH ± S.E.M.
| n
b
| ||||||
| nM | nM | ||||||||||
| 1 | ETPDCFWKYCV (hUT-II) | 12 ± 5 | −1.11 ± 0.26 | 4 | 63 ± 17 | −1.04 ± 0.06 | 4 | ||||
| 30 | QHGTAPECFWKYCI (rUT-II) | 14 ± 4 | −0.76 ± 0.06 | 3 | 28 ± 8 | −1.09 ± 0.05 | 3 | ||||
| 2 | CFWKYC | 530 ± 164 | −0.90 ± 0.06 | 3 | 4,550 ± 421 | −1.1 ± 0.03 | 3 | ||||
| 3 | TPDCFWKYCV | 27 ± 17 | −0.97 ± 0.11 | 3 | 63 ± 17 | −1.04 ± 0.06 | 4 | ||||
| 4 | PDCFWKYCV | 4.6 ± 1.2 | −0.95 ± 0.11 | 3 | 28 ± 8 | −1.09 ± 0.05 | 3 | ||||
| 5 | DCFWKYCV | 5.5 ± 0.4 | −0.68 ± 0.13 | 4 | 13 ± 3 | −1.26 ± 0.21 | 4 | ||||
| 6 | CFWKYCV | 13 ± 7 | −0.51 ± 0.04 | 3 | >10,000 | N.D. | 3 | ||||
| 7 | ETPDCFWKYC | >10,000 | N.D. | 3 | 2,672 ± 407 | −0.87 ± 0.03 | 4 | ||||
| 38 | ECFWKYCV | 2.6 ± 0.8 | −0.78 ± 0.14 | 3 | 51 ± 29 | −0.77 ± 0.24 | 3 | ||||
| 8 | ATPDCFWKYCV | 17 ± 5 | −0.91 ± 0.47 | 4 | 30 ± 8 | −0.97 ± 0.03 | 4 | ||||
| 9 | EAPDCFWKYCV | 5.4 ± 2.5 | −1.15 ± 0.30 | 3 | 52 ± 30 | −0.75 ± 0.08 | 3 | ||||
| 10 | ETADCFWKYCV | 12 ± 5.3 | −0.54 ± 0.05 | 4 | 66 ± 28 | −0.70 ± 0.08 | 3 | ||||
| 11 | ETPACFWKYCV | 11 ± 3.5 | −0.80 ± 0.18 | 5 | 19 ± 5 | −1.11 ± 0.05 | 3 | ||||
| 17 | ETPDCFWKYCA | 171 ± 29 | −1.19 ± 0.28 | 4 | 1,718 ± 542 | −1.22 ± 0.17 | 4 | ||||
| 31 | AAAACFWKYCV | 7.3 ± 1.8 | −1.39 ± 0.39 | 3 | 31 ± 4 | −1.29 ± 0.11 | 3 | ||||
|
27
|
ETPDCFWKYCV-NH2
|
10 ± 4
|
−0.81 ± 0.13
|
4
|
31 ± 3
|
−0.98 ± 0.09
|
3
| ||||