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New proctolin analogues: Synthesis and biological investigation in insects

Research output: Contribution to journalArticle

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Author(s)

Mariola Kuczer, Grzegorz Rosiński, Jonathan Issberner, Richard Osborne, Danuta Konopińska

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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-X1-Tyr-Leu-Pro-Thr-OH, where X1 = 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.

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Details

Original languageEnglish
Pages (from-to)387-389
Number of pages3
JournalLetters in Peptide Science
Volume5
Issue number5-6
DOIs
Publication statusPublished - 1 Jan 1998

    Research areas

  • Insect neuropeptide proctolin, Myotropic effects in insects, Proctolin and its analogues, Synthesis of proctolin analogues

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ID: 255577961