Analogs of Manduca adipokinetic hormone tested in a bioassay and in a receptor-binding assay.
Single amino acid replacement analogs of Manduca adipokinetic hormone (M-AKH) pGlu-Leu-Thr-Phe-Thr-Ser-Ser-Trp-GlyNH2 were tested for activity in bioassays as well as receptor binding assays. Amino acids were replaced by Ala and by D-analogs. In addition an extended M-AKH and analogs containing photo affinity labels were tested. All analogs had reduced activity. All the peptides which had enough activity to allow a full dose response curve reached the same maximal activity as native M-AKH. The use of analogs, in which L-Phe4 was replaced by Ala or by D-Phe and of L-Thr3 replaced by D-Thr, as competitors led to improved binding of M-AKH in our competitive receptor binding assay. In the bioassay an inactive concentration of Ala4 M-AKH increased the activity of a half optimal concentration of native M-AKH.
Ziegler
R
R
Department of Biochemistry and Center for Insect Science, University of Arizona, Tucson 85721, USA. ziegler@zoologie.uni-halle.de
Cushing
A S
AS
Walpole
P
P
Jasensky
R D
RD
Morimoto
H
H
D000273:Adipose Tissue / Q000378:metabolism; D000818:Animals; D001681:Biological Assay; D002462:Cell Membrane / Q000378:metabolism; D007301:Insect Hormones / Q000737:chemistry / Q000494:pharmacology*; D007814:Larva; D018402:Manduca; D009842:Oligopeptides / Q000737:chemistry / Q000494:pharmacology*; D006005:Phosphorylases / Q000378:metabolism; D011485:Protein Binding; D011761:Pyrrolidonecarboxylic Acid / Q000031:analogs & derivatives; D011956:Receptors, Cell Surface / Q000378:metabolism; D013329:Structure-Activity Relationship
D007301:Insect Hormones; D009842:Oligopeptides; D011956:Receptors, Cell Surface; C044833:adipokinetic hormone; D006005:Phosphorylases; D011761:Pyrrolidonecarboxylic Acid