Cloning and functional expression of the first Drosophila melanogaster sulfakinin receptor DSK-R1
| Autor: | Roger A. Martin, Carol A Bannow, Marjorie R. Zantello, Katherine J. Burton, Martha J. Larsen, David E. Lowery, Teresa Kubiak |
|---|---|
| Rok vydání: | 2002 |
| Předmět: |
G protein
Molecular Sequence Data Biophysics Receptors Cell Surface Biology Pertussis toxin Biochemistry Cell Line Receptors G-Protein-Coupled Animals Drosophila Proteins Humans Amino Acid Sequence Cloning Molecular Receptor Molecular Biology Chromatography High Pressure Liquid Phylogeny G protein-coupled receptor Cloning Dose-Response Relationship Drug Neuropeptides Biological activity Cell Biology biology.organism_classification Drosophila melanogaster Calcium Receptors Cholecystokinin Signal transduction Oligopeptides |
| Zdroj: | Biochemical and biophysical research communications. 291(2) |
| ISSN: | 0006-291X |
| Popis: | Described in this report is a successful cloning and characterization of a functionally active Drosophila sulfakinin receptor designated DSK-R1. When expressed in mammalian cells, DSK-R1 was activated by a sulfated, Met(7--Leu(7)-substituted analog of drosulfakinin-1, FDDY(SO(3)H)GHLRF-NH(2) ([Leu(7)]-DSK-1S). The interaction of [Leu(7)]-DSK-1S with DSK-R1 led to a dose-dependent intracellular calcium increase with an EC(50) in the low nanomolar range. The observed Ca(2+) signal predominantly resulted from activation of pertussis toxin (PTX)-insensitive signaling pathways pointing most likely to G(q/11) involvement in coupling to the activated receptor. The unsulfated [Leu(7)]-DSK-1 was ca. 3000-fold less potent than its sulfated counterpart which stresses the importance of the sulfate moiety for the biological activity of drosulfakinin. The DSK-R1 was specific for the insect sulfakinin since two related vertebrate sulfated peptides, human CCK-8 and gastrin-II, were found inactive when tested at concentrations up to 10(-5) M. To our knowledge, the cloned DSK-R1 receptor is the first functionally active Drosophila sulfakinin receptor reported to date. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|
Full Text from ScienceDirect