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Johnson, E.C. et al.

Identification and characterization of a G protein-coupled receptor for the neuropeptide proctolin in Drosophilamelanogaster.

Proctolin is a bioactive neuropeptide that modulates interneuronal and neuromuscular synaptic transmission in a wide variety of arthropods. We present several lines of evidence to propose that the orphan G protein-coupled receptor CG6986 of Drosophila is a proctolin receptor. When expressed in mammalian cells, CG6986 confers second messenger activation after proctolin application, with an EC(50) of 0.3 nM. In competition-based studies, the CG6986 receptor binds proctolin with high affinity (IC(50) = 4 nM). By microarray analysis, CG6986 transcript is consistently detected in head mRNA of different genotypes, and under different environmental conditions. By blot analysis, anti-CG6986 antibodies detect a band in tissue homogenates similar to the predicted size of the protein. Proctolin receptor immunosignals are found in the hindgut, heart, and in distinct neuronal populations of the CNS; such patterns correlate with previous demonstrations of proctolin biological activity, and in several instances, with areas of proctolin peptide immunosignals. The identification of a bona fide proctolin receptor provides the basis for a mechanistic analysis of this critical synaptic modulator.[1]

References

Identification and characterization of a G protein-coupled receptor for the neuropeptide proctolin in Drosophilamelanogaster. Johnson, E.C., Garczynski, S.F., Park, D., Crim, J.W., Nassel, D.R., Taghert, P.H. Proc. Natl. Acad. Sci. U.S.A. (2003) [Pubmed]

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