Neuropeptide B/W Family Related Drug Discovery Products
Creative Biolabs has the assays you can rely on for high throughput screening, lead optimization, characterizing and discovering targets, and uncovering the complexity of disease pathways. We can offer membrane protein in vitro assay kits that save valuable laboratory time and is ideal for high throughput screening.
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Recently, the endogenous ligands for the hitherto orphan G-protein coupled receptors GPR7 (NPBWR1) and GPR8 were shown to be neuropeptides B (NPB) and W (NPW) (NPBWR2). This neuropeptide system is believed to have a part in controlling neuroendocrine function, eating behavior, energy homeostasis, and inflammation-related discomfort. These receptors are strongly and specifically expressed in the extended amygdala, which suggests that they may have a role in controlling fear, anxiety, and stress-related reactions.
Fig.1 The NPB/NPW neuropeptide system. (Hondo, 2008)
Creative Biolabs offers high-quality neuropeptide B/W family drug discovery in vitro assays and related products to contribute to the success of your project:
Overview of Neuropeptide B/W Family
The amino acid counts for human NPBWR1 and NPBWR2 are 328 and 333, respectively, and they have a 64% similarity in their sequences. NPBW1 and NPBW2 are the GPCR family members that are primarily connected to somatostatin and opioid receptors. The NPBW1 orthologues in other mammalian species have shown significant levels of conservation throughout evolution using amino-acid analysis. Yet, although being found in a number of mammalian species, including the monkey, lemur, bat, shrew, and rabbit, the gene encoding NPBWR2 has not been found in rodents. NPBWR1 and NPBWR2 both couple to G-proteins of the Gi-class. This shows that the GIRK (Kir3) channels are how these neuropeptides exert their inhibitory effects on neurons. Moreover, it was discovered that NPB and NPW increase Erk p42/p44 activity in NCI-H295 cells originating from human adrenocortical cancer. These activations are most likely caused by beta/gamma subunits that Gi-prot releases.
The highest quantities of NPBWR1 mRNA and binding signals are expressed by the CeA and BNST. The ventral tuberomamillary nuclei of the hypothalamus and suprachiasmatic (SCN) nuclei are other nuclei with significant amounts of NPBWR1 expression and binding. These findings imply that NPBWR1 may play a role in the control of stress and emotional reactions, particularly those related to the physiological and behavioral manifestations of fear and anxiety. Human hippocampal and amygdala NPBWR2 mRNA is highly expressed. The corpus callosum, cerebellum, substantia nigra, and caudate nucleus all showed lower levels of expression.
Fig.2 Schematic representation of the NPB/W-GPR7 system in mouse brain. (Hondo, 2008)
Neuropeptide B/W Family Drug Discovery
It has been shown that NPBW1 regulates eating, metabolism, and obesity, which intriguingly seems to be exclusive to male mice. We still don't know if this holds true for people. In humans, abdominal obesity is more common in men and is a risk factor on its own for coronary heart disease. When starting a drug discovery program based on this emerging transmitter system, whether as a potential target for treating inflammation-mediated pain or for modulating feeding behavior, it is important to take into account that activating or disrupting the NPBW1 transmitter system has not yet had significant effects on growth and mortality.
Reference
- Hondo, M.; et al. The NPB/NPW neuropeptide system and its role in regulating energy homeostasis, pain, and emotion. Orphan G Protein-Coupled Receptors and Novel Neuropeptides. 2008, 239-256.
