In the present report, we have analyzed the interaction pattern between the glucagon-like peptide-1 (GLP-1) receptor (GLP-1R), βarr2, and GRK2 using bioluminescence resonance energy transfer assays. We found t
将Tag-lite SNAP-GLP1R HEK293 细胞以 100,000 个细胞/孔接种到 96 孔板中,并在 37°C、5% CO2 下孵育 24 小时。用刺激缓冲液4中稀释的浓度逐渐增加的Exendin-4在室温下处理30分钟后,除去培养基。用 30 µL 稳定缓冲液 1 在室温下稳定细胞 15 分钟,然后用 100 µl 洗涤缓冲液 1 洗涤 3 次。最...
Four SNPs and resulting amino acid mutations inβarr1, namely I158V, T275I, T370M and G411S have been recently correlated with improvement in glycemic index in diabetic patients treated with GLP1R agonism. These four SNPs have not been linked with βarr1 functions thus far and when tested...
Understanding how GLP-1 interacts with its receptor (GLP-1R) can potentially lead to more effective drugs. Modeling and NMR studies of the N-terminus of GLP-1 suggest a β-turn between residues Glu9-Phe12 and a kinked alpha helix between Val16-Gly37. N-terminal turn constraints attenuated...
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