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New Proctolin Analogues: Synthesis and Biological Investigation in Insects.
- Source :
- Letters in Peptide Science; Oct1998, Vol. 5 Issue 5/6, p387-389, 3p
- Publication Year :
- 1998
-
Abstract
- We have extended our work on structure/activity relationship studies of the neuropeptiden proctolin (H-Arg-Tyr-Leu-Pro-Thr-OH) by evaluating the effects of the following proctolin analogues: H-X-Tyr-Leu-Pro-Thr-OH, where X = D-Arg (I), N-Me-Arg (II), Can (III), Orn(di-Me) (IV), Orn(iPr) (V), Lys(N, N-di-Me) (VI), Lys(iPr) (VII), Lys(Nic) (VIII) and D-Lys(Nic) (IX). In analogues I-IX, the N-terminal Arg residue was replaced by basic amino acid derivatives with peptides containing amino acid residues with an isosteric system on the back side chain relative to Arg (compounds III, V and VI) or homo-Arg (compound VII). Analogues I-IX were evaluated for myotropic activity on the in vitro heart preparation of Tenebrio molitor, whereas peptides II, V, and VII-IX were tested for contractile activity on the isolated foregut of locust Schistocerca gregaria. Peptide II and III showed full cardiotropic activity in T. molitor while peptides V and VII showed 40% and 15%, respectively, locust-gut contracting activity of proctolin. [ABSTRACT FROM AUTHOR]
Details
- Language :
- English
- ISSN :
- 09295666
- Volume :
- 5
- Issue :
- 5/6
- Database :
- Complementary Index
- Journal :
- Letters in Peptide Science
- Publication Type :
- Academic Journal
- Accession number :
- 71717789
- Full Text :
- https://doi.org/10.1023/A:1008831309070