详细记录  
题名:Development of a cysteine-deprived and C-terminally truncated GLP-1 receptor.
作者:UNDERWOOD CR; KNUDSEN LB; GARIBAY PW; PETERS GH; REEDTZ-RUNGE S;
来源:Peptides. 2013 Nov;49:100-8. doi: 10.1016/j.peptides.2013.09.001. Epub 2013 Sep [ IF= 2.52 ] ]
URL :10.1016/j.peptides.2013.09.001
日期:20131203
摘要:The glucagon-like peptide-1 receptor (GLP-1R) belongs to family B of the
G-protein coupled receptors (GPCRs), and has become a promising target for the
treatment of type 2 diabetes. Here we describe the development and
characterization of a fully functional cysteine-deprived and C-terminally
truncated GLP-1R. Single cysteines were initially substituted with alanine, and
functionally redundant cysteines were subsequently changed simultaneously. Our
results indicate that Cys(174), Cys(226), Cys(296) and Cys(403) are important for
the GLP-1-mediated response, whereas Cys(236), Cys(329), Cys(341), Cys(347),
Cys(438), Cys(458) and Cys(462) are not. Extensive deletions were made in the
C-terminal tail of GLP-1R in order to determine the limit for truncation. As for
other family B GPCRs, we observed a direct correlation between the length of the
C-terminal tail and specific binding of (125)I-GLP-1, indicating that the
membrane proximal part of the C-terminal is involved in receptor expression at
the cell surface. The results show that seven cysteines and more than half of the
C-terminal tail can be removed from GLP-1R without compromising GLP-1 binding or
function.

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