Coast, Geoffrey and Zabrocki, J. and Nachman, R.J. (2002) Diuretic and myotropic activities of N-terminal truncated analogs of Musca domestica kinin neuropeptide. Peptides 23 (4), pp. 701-708. ISSN 0196-9781.
Abstract
Musca kinin (Musdo-K; NTVVLGKKQRFHSWG-NH2) and N-terminal truncated analogs of 4–14 residues in length were assayed for diuretic and myotropic activity on housefly Malpighian tubules and hindgut, respectively. The pentapeptide was the minimum sequence required for biological activity, but it was > 5 orders of magnitude less potent than the intact peptide. The pharmacological profiles of the different analogs in the two assays were very similar, suggesting the same receptor is present on both tissues. Potency was little affected by the deletion of Asn1, but was reduced > 10-fold after the removal of Thr2. Deletion of the next 5 residues had relatively little effect, but after the second lysyl residue (Lys8) was removed potency fell by one to two orders of magnitude. There was a similar drop in potency after the removal of Arg10, and at 100 μM the pentapeptide had only 20% of the diuretic activity of the intact peptide. The importance of Arg10 was confirmed by comparing dose-response curves for Musdo-K [6–15] and Acheta kinin-V (AFSHWG-NH2) in the diuretic assay; the substitution of arginine by alanine produced a significant reduction in potency and some loss of activity.
Metadata
| Item Type: | Article |
|---|---|
| School: | Birkbeck Faculties and Schools > Faculty of Science > School of Natural Sciences |
| Depositing User: | Sarah Hall |
| Date Deposited: | 20 May 2019 11:50 |
| Last Modified: | 02 Aug 2023 17:51 |
| URI: | https://eprints.bbk.ac.uk/id/eprint/27575 |
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