Active, purified membrane protein / nanodisc preparation containing MSP1E3-His scaffold protein and POPC phospholipids. 20 microgram in solution. Shipped on dry ice
Active, purified OPRM1 (Mu-type-opioid receptor) in nanodisc
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.
S-PAGE of OPRM1 in nanodisc, purified via Rho1D4 affinity chromatography.
Orange arrow: GPCR; Green arrow: membrane scaffold protein
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Protein
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OPRM1 (Mu-type opioid receptor 1)
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Alternative names
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MOR1, MOP, Mu opiate receptor |
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UniProt
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P35372
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Protein class
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GPCR, class A (Rhodopsin-like receptors) |
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Organism
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Human (Homo sapiens) |
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Sequence
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Full-length, wildtype sequence
Initial methionine in bold, spacer in bold grey, Rho1D4 tag in bold green
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M D S S A A P T N A S N C T D A L A Y S S C S P A P S P G S W V N L S H L D G N L S D P C G P N R T D L G G R D S L C P P T G S P S M I T A I T I M A L Y S I V C V V G L F G N F L V M Y V I V R Y T K M K T A T N I Y I F N L A L A D A L A T S T L P F Q S V N Y L M G T W P F G T I L C K I V I S I D Y Y N M F T S I F T L C T M S V D R Y I A V C H P V K A L D F R T P R N A K I I N V C N W I L S S A I G L P V M F M A T T K Y R Q G S I D C T L T F S H P T W Y W E N L L K I C V F I F A F I M P V L I I T V C Y G L M I L R L K S V R M L S G S K E K D R N L R R I T R M V L V V V A V F I V C W T P I H I Y V I I K A L V T I P E T T F Q T V S W H F C I A L G Y T N S C L N P V L Y A F L D E N F K R C F R E F C I P T S S N I E Q Q N S T R I R Q N T R D H P S T A N T V D R T N H Q L E N L E A E T A P L PG S S GT E T S Q V A P A
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Affinity tags
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Rho1D4 (C-terminal) |
Size (excluding
additional elements)
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413 (400) amino acids
45,953 (44,779) Da
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Expression system
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Sf9 (baculovirus) |
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Purified via
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PureCube Rho1D4 Agarose |
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Buffer
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100 mM NaCl, 20 mM NaH2PO4, pH 7.4 |
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Nanodisc
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MSP1E3D1 protein, His-tagged, with POPC lipids |
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Purity (SDS-PAGE)
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>98% (see Fig. 1) |
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Homogeneity
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Size exclusion chromatography |
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Activity
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Ligand binding measured by SPR using Endomorphin (synthetic peptide YPWF) at 10°C. Using a 1:1 binding model, the kD was determined to be 14.5 nM.
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Function
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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.
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Literature references
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1. 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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