| Glucagon-like peptide-I (GLP-1), part of the secretin peptide family, is a class B (class 2)
receptor and is involved in glucose-dependent insulin secretion. Insulin secretion is
predominantly controlled by glucose levels in the blood, however glucagon stimulates the
secretion of insulin (Drucker et al. 1987). The GLP-1 receptor couples to Gs to increase
cAMP levels (Mayo et al. 2003). GLP-1 has been shown to delay gastric emptying and
regulate appetite. Due to the involvement in insulin secretion GLP-1 has been identified as
a therapeutic target in type II diabetes (Mayo et al. 2003, D’Alessio et al. 2004). Millipore's
GLP-1 membrane preparations are crude membrane preparations made from our
proprietary stable recombinant cell lines to ensure high-level of GPCR surface expression;
thus, they are ideal HTS tools for screening of antagonists of GLP-1 interactions with GLP-1.
The membrane preparations exhibit a Kd of 0.27 nM for [125I]-GLP-1. With 10 μg/well GLP-1
Membrane Prep and 0.5 nM [125I]-GLP-1, a greater than 9-fold signal-to-background ratio
was obtained. |
日本
