Structure-activity studies of Drosophila adipokinetic hormone (AKH) by a cellular expression system of dipteran AKH receptors

General and Comparative Endocrinology
Jelle CaersLiliane Schoofs

Abstract

Structure-activity studies for the adipokinetic hormone receptor of insects were for the first time performed in a cellular expression system. A series of single amino acid replacement analogues for the endogenous adipokinetic hormone of Drosophila melanogaster (pGlu-Leu-Thr-Phe-Ser-Pro-Asp-Trp-NH(2)) were screened for activity with a bioluminescence cellular assay, expressing the G-protein coupled receptor. For this series of peptide analogues, one amino acid of the N-terminal tetrapeptide was successively replaced by alanine, while those of the C-terminal tetrapeptide were successively substituted by glycine; other modifications included the blocked N- and C-termini that were replaced by an acetylated alanine and a hydroxyl group, respectively. The analogue series was tested on the AKH receptors of two dipteran species, D. melanogaster and Anopheles gambiae. The blocked termini of the AKH peptide probably play a minor role in receptor interaction and activation, but are considered functionally important elements to protect the peptide against exopeptidases. In contrast, the amino acids at positions 2, 3, 4 and 5 from the N-terminus all seem to be crucial for receptor activation. This can be explained by the potential presence...Continue Reading

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Citations

Sep 24, 2015·Annual Review of Cell and Developmental Biology·Edward Owusu-Ansah, Norbert Perrimon
Feb 3, 2015·Insect Biochemistry and Molecular Biology·Suresh SajwanMichal Zurovec
Nov 9, 2016·General and Comparative Endocrinology·Marie-Pierre DubosPascal Favrel
Feb 15, 2018·International Journal of Molecular Sciences·Elisabeth MarchalHeleen Verlinden
Sep 1, 2019·Archives of Insect Biochemistry and Physiology·Gerd GädeHeather G Marco
Aug 16, 2015·Genetics·Martina GálikováRonald P Kühnlein
Jul 25, 2021·International Journal of Molecular Sciences·Jonathan M NelsonErik C Johnson
Feb 11, 2020·Journal of Proteome Research·Laura A FleitesMichelle L Heck

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