Membrane proteins are the most pharmaceutically relevant protein class. At the same time, it is very difficult to obtain them in pure, active form. Cube Biotech's protein experts have worked hard to produce human GPCRs in sufficient quality that we can now offer to the community. We offer active, purified GLP1R, a human GPCR involved in insuline production and appetite regulation. The protein is available off-the shelf, ready for ligand binding studies, crystallization, and other biochemical/biophysical experiments.
Please contact us for bulk inquiries, academic projects or collaboration ideas.
Fig. 1: Size and purity of GLP1R assessed by SDS-PAGE and size exclusion chromatography. Note: GLP1R is always detected as a double band in SDS-PAGE.
Fig. 2: Surface plasmon resonance measurement of GLP1R-exendin interaction. Using a 1:1 binding model, the dissociation constant (Kd) value was determined to 6.11x10e-7 M.
Features
| Protein | GLP1R (Glucagon-like peptide 1 receptor) |
| Alternative names | GLP1-receptor |
| UniProt number | P43220 |
| Protein class | GPCR, class B |
| Organism | Human (Homo sapiens) |
| Sequence | Full-length, wildtype sequence N-terminal HA signal sequence (underlined), 10x His-tag with spacer (red), HRV 3C protease site (blue), spacer (gray), Rho1D4 tag (green)
MKTIIALSYIFCLVFARPQGATVSLW ETVQKWREYR RQCQRSLTED PPPATDLFCN RTFDEYACWP DGEPGSFVNV SCPWYLPWAS SVPQGHVYRF CTAEGLWLQK DNSSLPWRDL SECEESKRGE RSSPEEQLLF LYIIYTVGYA LSFSALVIAS AILLGFRHLH CTRNYIHLNL FASFILRALS VFIKDAALKW MYSTAAQQHQ WDGLLSYQDS LSCRLVFLLM QYCVAANYYW LLVEGVYLYT LLAFSVLSEQ WIFRLYVSIG WGVPLLFVVP WGIVKYLYED EGCWTRNSNM NYWLIIRLPI LFAIGVNFLI FVRVICIVVS KLKANLMCKT DIKCRLAKST LTLIPLLGTH EVIFAFVMDE HARGTLRFIK LFTELSFTSF QGLMVAILYC FVNNEVQLEF RKSWERWRLE HLHIQRDSSM KPLKCPTSSL SSGATAGSSM YTATCQASCS GGHHHHHHHHHH LEVLFQGPGS SGTETSQVAPA
|
| Affinity tags | His / Rho1D4 (both C-terminal) |
| Size (excluding additional elements) | 489 (463) amino acids 56,170 (53,026) Da |
| Expression system | Sf9 (baculovirus) |
| Purified via | Protein-specific affinity matrix using immobilized agonist ligand, size exclusion chromatography |
| Buffer | 20 mM HEPES pH 7.5, 150 mM NaCl, 10% Glycerol, 0.02% Foscholine-12 |
| Purity (SDS-PAGE) | >98% as determined by SDS-PAGE |
| Homogeneity | Size exclusion chromatography |
| Activity | Ligand binding measured by SPR using the agonist ligand exendin-4 at 10°C. Using a 1:1 binding model, the dissociation constant (Kd) was determined to 6.11x10e-7 M, which is in accordance with published values. |
| Function | Receptor for glucagon-like peptide 1. Expressed in pancreas, brain, heart, kidney and the GI tract. Involved in insuline secretion and appetite regulation. |
| Literature references | - Hwang JI et al. Molecular evolution of GPCRs: GLP1/GLP1 receptors. J. Mol. Endocrinol. (2014) 52 (3) 15-27.
- Sisley S. et al. Neuronal GLP1R mediates liraglutide's anorectic but not glucose-lowering effect. (2014) J. Clin. inv. 124(6)2456-2463.
|
