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 have reconstituted the proteins into nanodiscs for stabilization. Our first available pure, active, nanodisc inserted membrane protein is OPRM1, a human GPCR involved in opiate response, pain modulation and analgesia, but also breast cancer. The protein is ready for ligand binding studies, crystallization, and other biochemical/biophysical experiments.
Features
| Protein |
OPRM1 (Mu-type opioid receptor 1) |
| Alternative names |
MOR1, MOP, Mu opiate receptor |
| UniProt number |
P35372 |
| Protein class |
GPCR, class A (Rhodopsin-like receptors) |
| Organism |
Human (Homo sapiens) |
| Sequence |
Full-length, wildtype sequence Initial methionine (bold), spacer (gray), Rho1D4 tag (green)
MDSSAAPTNAS NCTDALAYSS CSPAPSPGSW VNLSHLDGNL SDPCGPNRTD LGGRDSLCPP TGSPSMITAI TIMALYSIVC VVGLFGNFLV MYVIVRYTKM KTATNIYIFN LALADALATS TLPFQSVNYL MGTWPFGTIL CKIVISIDYY NMFTSIFTLC TMSVDRYIAV CHPVKALDFR TPRNAKIINV CNWILSSAIG LPVMFMATTK YRQGSIDCTL TFSHPTWYWE NLLKICVFIF AFIMPVLIIT VCYGLMILRL KSVRMLSGSK EKDRNLRRIT RMVLVVVAVF IVCWTPIHIY VIIKALVTIP ETTFQTVSWH FCIALGYTNS CLNPVLYAFL DENFKRCFRE FCIPTSSNIE QQNSTRIRQN TRDHPSTANT VDRTNHQLEN LEAETAPLP GSSG TETSQVAPA
|
| Affinity tags |
Rho1D4 (C-terminal) |
| Size (excluding additional elements) |
413 (400) amino acids 45,953 (44,779) Da |
| Expression system |
Sf9 (baculovirus) |
| Purified via |
PureCube Rho1D4 Agarose |
| Buffer |
100 mM NaCl, 20 mM NaH2PO4, pH 7.4 |
| Nanodisc |
MSP1E3D1 protein, His-tagged, with POPC lipids |
| Purity (SDS-PAGE) |
>98% (see Fig. 1) |
| Homogeneity |
Size exclusion chromatography |
| Function |
OPRM1 is the most relevant physiological target for most clinically relevant analgesics. Receptor for endogenous opioids such as beta-endorphin and endomorphin, and for natural and synthetic opioids including morphine, heroin, DAMGO, fentanyl, etorphine, buprenorphin and methadone. |
| Literature references |
- Burford, NT et al. Discovery of positive allosteric modulators and silent allosteric modulators of the µ-opioid receptor. (2013) PNAS 110 (26) 10830-10835
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