Effects of endocyclic 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 | ||||
| 13 | ETPDCAWKYCV | 1,744 ± 544 | −0.25 ± 0.01 | 5 | > 10,000 | N.D. | 3 | ||||
| 14 | ETPDCFAKYCV | >10,000 | N.D. | 3 | > 10,000 | N.D. | 3 | ||||
| 15 | ETPDCFWAYCV | 4,403 ± 2,027 | −0.58 ± 0.09 | 3 | > 10,000 | N.D. | 3 | ||||
| 16 | ETPDCFWKACV | >10,000 | N.D. | 3 | > 10,000 | N.D. | 3 | ||||
| 18 | ETPDC-WKYCV | >10,000 | N.D. | 3 | > 10,000 | N.D. | 3 | ||||
| 19 | ETPDCF-KYCV | >10,000 | N.D. | 3 | > 10,000 | N.D. | 3 | ||||
| 20 | ETPDCFW-YCV | 5,082 ± 1,991 | −1.21 ± 0.53 | 3 | > 10,000 | N.D. | 3 | ||||
| 21 | ETPDCFWK-CV | >10,000 | N.D. | 3 | > 10,000 | N.D. | 3 | ||||
| 22 | ETPDCfWKYCV | 6,680 ± 621 | −0.88 ± 0.06 | 3 | > 10,000 | −0.72 ± 0.12 | 3 | ||||
| 23 | ETPDCFwKYCV | 918 ± 8 | −0.93 ± 0.21 | 3 | 3,044 ± 445 | −1.04 ± 0.05 | 3 | ||||
| 24 | ETPDCFWkYCV | >10,000 | N.D. | 3 | > 10,000 | N.D. | 3 | ||||
| 25 | ETPDCFWKyCV | 2,247 ± 231 | −1.55 ± 0.21 | 3 | > 10,000 | N.D. | 3 | ||||
| 28 | ETPDCFHKYCV | 5,053 ± 429 | −1.32 ± 0.06 | 3 | > 10,000 | −0.86 ± 0.24 | 3 | ||||
| 32 | ETPDCFWRYCV | 684 ± 185 | −1.04 ± 0.08 | 5 | 3,068 ± 259 | −0.89 ± 0.05 | 3 | ||||
| 33 | ETPDCFWOrnYCV | 848 ± 107 | −1.25 ± 0.28 | 3 | 4,014 ± 542 | −1.96 ± 0.76 | 3 | ||||
| 35 | ETPDCFWKFCV | 4.0 ± 2.5 | −0.87 ± 0.16 | 3 | 663 ± 114 | −0.92 ± 0.04 | 3 | ||||
| 36 | ETPDCYWKYCV | 187 ± 69 | −1.14 ± 0.17 | 4 | 145 ± 11 | −0.91 ± 0.04 | 3 | ||||
| 41 | ETPDCFPKYCV | >10,000 | N.D. | 4 | > 10,000 | N.D. | 5 | ||||
| 29 | ETPDCAFWKYCV | >10,000 | −1.13 ± 0.38 | 4 | > 10,000 | −0.45 ± 0.08 | 4 | ||||
|
40
|
ETPDCFKYWCV
|
>10,000
|
N.D.
|
4
|
> 10 000
|
N.D.
|
5
| ||||