Active, purified GPBAR1 (G-protein coupled bile receptor 1)

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.

Our first available pure, active membrane protein is GPBAR1 / TGR5,  a human GPCR involved in bile acid homeostasis, glucose metabolism, and weight maintenance. 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.

 

 

Active Membrane Proteins
 
 
Fig. 1: SDS-PAGE of GPBAR1, purified via Rho1D4 affinity chromatography.
L: Lysate: FT: flow through, W: Wash, E1-E3: elution fractions with purified GPCR.
GPBAR1 TGR5 SDS-PAGE showing pure protein preparation after Rho1D4 affinity chromatography
Fig. 2: Surface plasmon resonance measurement of GPBAR-1 / Taurolithocholic acid sulfate salt interaction. Using a 1:1 binding model, the Kd was determined to be 1.1x10e-8 M.
SPR data showing ligand binding to GPBAR1 TGR5 protein

Protein

GPBAR1 (G-protein coupled bile receptor 1)

Alternative names

TGR5, GPCR19, M-BAR, BG37

UniProt / UniGene

Q8TDU6 / 155918

Protein class

GPCR, class A (Rhodopsin-like receptors)

Organism

Human (Homo sapiens)

Sequence

Full-length, wildtype sequence
N-terminal HA tag (underlined), C-terminal 10x His-tag in red,
HRV 3C protease site in blue, spacer in bold grey, Rho1D4 tag in bold green
 
MKTIIALSYIFCLVFA LSLALASLIIT ANLLLALGIA WDRRLRSPPA GCFFLSLLLA GLLTGLALPT LPGLWNQSRR GYWSCLLVYL APNFSFLSLL ANLLLVHGER YMAVLRPLQP PGSIRLALLL TWAGPLLFAS LPALGWNHWT PGANCSSQAI FPAPYLYLEV YGLLLPAVGA AAFLSVRVLA TAHRQLQDIC RLERAVCRDE PSALARALTW RQARAQAGAM LLFGLCWGPY VATLLLSVLA YEQRPPLGPG TLLSLLSLGS ASAAAVPVAM GLGDQRYTAP WRAAAQRCLQ GLWGRASRDS PGPSIAYHPS SQSSVDLDLNGGHHHHHHHHHHLEVLFQGPGSSGTETSQVAPA

Affinity tags

His / Rho1D4 (both C-terminal)
Size (excluding
additional elements)
379 (330) amino acids
40,606 (35,248) Da

Expression system

Sf9 (baculovirus)

Purified via

PureCube Rho1D4 Agarose

Buffer

100 mM NaCl, 20 mM NaH2PO4 pH 7.4, 0.1% Foscholine-12, 0.01% cholesterolhemisuccinate (CHS)

Purity (SDS-PAGE)

>98%, see Fig. 1

Homogeneity

Size exclusion chromatography

Activity

Ligand binding measured by SPR using Taurolithocholic Acid Sulfate Disodium Salt (CAS 64936-83-0) at 10°C. Using a 1:1 binding model, the dissociation constant (Kd) was determined to be 1.1x10e-8 M.

Function

Receptor for bile acid. Bile acid-binding induces its internalization, activation of extracellular signal-regulated kinase and intracellular cAMP production. May be involved in the suppression of macrophage functions by bile acids, and in modulating inflammation.
Literature  references:
1. Kawamata, Y. et al. (2003) A G Protein-coupled receptor responsive to bile acids, J. Biol. Chem. 278, 11, pp9435-9440
2. Chen, X. et al. (2011) TGR5: A Novel Target for Weight Maintenance and Glucose Metabolism. Exp. Diabetes Res. Article ID 853501
3. Pols, T.W.H. et al. (2013) The bile acid membrane receptor TGR5 as an emerging target in metabolism and inflammation. J. Hepatol. 54(6):1263-1272

 

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GPBAR1/TGR5

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Current Stock Level

GPBAR1 (TGR5) protein (10 ug)

Sales price: 969,00 €

Product details