Human NPBWR2

Figure. Concentration-dependent activation of NPBWR2 by NPW‐30

Reporter cells were transfected with either the expression plasmid for human neuropeptides B and W receptor 2 (NPBWR2) or the mock plasmid and treated with various concentrations of NPW‐30. Data points shown are the mean ± SEM of an experiment (n = 3), and the curve is a fit to Hill equation with an EC50 of 14 nM.

Nomenclature
neuropeptides B and W receptor 2
Available assay modes
Agonist, Inverse agonist, Antagonist, PAM, NAM
Panels
à la carte, Human non-orphan GPCRs

Neuropeptide W/neuropeptide B receptors

The neuropeptide BW receptor 1 (NPBW1, provisional nomenclature [1]) is activated by two 23-amino-acid peptides, neuropeptide W (neuropeptide W-23) and neuropeptide B (neuropeptide B-23) [2,3]. C-terminally extended forms of the peptides (neuropeptide W-30 and neuropeptide B-29) also activate NPBW1 [4]. Unique to both forms of neuropeptide B is the N-terminal bromination of the first tryptophan residue, and it is from this post-translational modification that the nomenclature NPB is derived. These peptides were first identified from bovine hypothalamus and therefore are classed as neuropeptides. Endogenous variants of the peptides without the N-terminal bromination, des-Br-neuropeptide B-23 and des-Br-neuropeptide B-29, were not found to be major components of bovine hypothalamic tissue extracts. The NPBW2 receptor is activated by the short and C-terminal extended forms of neuropeptide W and neuropeptide B [4].

References

  1. Foord SM, Bonner TI, Neubig RR, et al. International Union of Pharmacology. XLVI. G protein-coupled receptor list. Pharmacol Rev 2005;57:279-88.
  2. Shimomura Y, Harada M, Goto M, et al. Identification of neuropeptide W as the endogenous ligand for orphan G-protein-coupled receptors GPR7 and GPR8. J Biol Chem 2002;277:35826-32.
  3. Fujii R, Yoshida H, Fukusumi S, et al. Identification of a neuropeptide modified with bromine as an endogenous ligand for GPR7. J Biol Chem 2002;277:34010-6.
  4. Brezillon S, Lannoy V, Franssen JD, et al. Identification of natural ligands for the orphan G protein-coupled receptors GPR7 and GPR8. J Biol Chem 2003;278:776-83.
Excerpt from IUPHAR/BPS Guide to Pharmacology

Related Receptors

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