Radiolabelled GLP-1 receptor antagonist binds to GLP-1 receptor-expressing human tissues
نویسندگان
چکیده
منابع مشابه
Peptide binding at the GLP-1 receptor.
The receptor for GLP-1 [glucagon-like peptide-1-(7-36)-amide] is a member of the 'Family B' of GPCRs (G-protein-coupled receptors) comprising an extracellular N-terminal domain containing six conserved cysteine residues (the N-domain) and a core domain (or J-domain) comprising the seven transmembrane helices and interconnecting loop regions. According to the two-domain model for peptide binding...
متن کاملGLP-1 receptor expression in human tumors and human normal tissues: potential for in vivo targeting.
UNLABELLED Peptide hormone receptors overexpressed in human tumors, such as somatostatin receptors, can be used for in vivo targeting for diagnostic and therapeutic purposes. A novel promising candidate in this field is the GLP-1 receptor, which was recently shown to be massively overexpressed in gut and lung neuroendocrine tumors--in particular, in insulinomas. Anticipating a major development...
متن کاملPurslane Effect on GLP-1 and GLP-1 receptor in type 2 diabetes
BACKGROUND The aim of this study was to examine the effect of purslane seeds in glucagon-like peptide-1 concentration and glucagon-like peptide-1 receptor in women with diabetes. METHODS This was a quasi-experimental study. The population was consisted of the city of Sari where diabetic women with diabetes II who had no history of using purslane seeds. All individuals used the same dose of me...
متن کاملGlucagon receptor antagonist-mediated improvements in glycemic control are dependent on functional pancreatic GLP-1 receptor.
Antagonism of the glucagon receptor (GCGR) is associated with increased circulating levels of glucagon-like peptide-1 (GLP-1). To investigate the contribution of GLP-1 to the antidiabetic actions of GCGR antagonism, we administered an anti-GCGR monoclonal antibody (mAb B) to wild-type mice and GLP-1 receptor knockout (GLP-1R KO) mice. Treatment of wild-type mice with mAb B lowered fasting blood...
متن کاملExpression and Characterization of a Potent Long-Acting GLP-1 Receptor Agonist, GLP-1-IgG2σ-Fc
Human GLP-1 (glucagon-like peptide-1) can produce a remarkable improvement in glycemic control in patients with type 2 diabetes. However, its clinical benefits are limited by its short half-life, which is less than 2 min because of its small size and rapid enzymatic inactivation by dipeptidyl peptidase IV. We engineered GLP-1-IgG2σ-Fc, a 68-kDa fusion protein linking a variant human GLP-1 (A8G/...
متن کاملذخیره در منابع من
با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید
ژورنال
عنوان ژورنال: European Journal of Nuclear Medicine and Molecular Imaging
سال: 2014
ISSN: 1619-7070,1619-7089
DOI: 10.1007/s00259-013-2684-4