Potencies of naturally-occurring AKH/RPCH peptides in Locusta migratoria in the acetate uptake assay in vitro and comparison with their potencies in the lipid mobilisation assay in vivo
G. Gade et al., Potencies of naturally-occurring AKH/RPCH peptides in Locusta migratoria in the acetate uptake assay in vitro and comparison with their potencies in the lipid mobilisation assay in vivo, ACT BIOL HU, 51(2-4), 2000, pp. 369-377
The biological potencies of a number of naturally-occurring octa- and decap
eptides of the large AKH/RPCH family of peptides were determined in Locusta
migratoria using the lipid-mobilising assay in vivo and the acetate uptake
assay in vitro. The most potent of the newly-tested peptides in the in vit
ro assay, Ph1-CC, differs from the endogenous major locust peptide, Lom-AKH
-I, only by an exchange of serine versus threonine at position 10. However,
the most active peptide in the ill vitro assay remains Lom-AKH-III. At the
other extreme is the peptide Mem-CC which contains a tyrosine residue at p
osition 4 rather than the more typical phenylalanine. This peptide is over
20000 times less potent than LomAKH-III in the ill vitro assay, and also re
sults in an unusual dose-response curve in the in vivo assay. Only a few pe
ptides are approximately equipotent in both assays, but mostly the bioanalo
gues have a higher potency in vitro. The majority of them are 2- to 10-fold
more potent in vitro, but Ani-AKH and LomAKH-III are 19- and 48-fold more
potent. The results are discussed in relation to either the actions of prot
eases or of possible preferential binding of different receptors involved i
n the different assays.