mProX™ Human GPR161 Stable Cell Line
- Product Category:
- Membrane Protein Stable Cell Lines
- Subcategory:
- GPCR Cell Lines
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Published Data
Fig.1 In human breast cancer cell lines, GPR161 plays a pivotal role in governing cellular proliferation.
To investigate the role of GPR161 in basal breast cancer cell proliferation, GPR161 was silenced using shRNA in the MCF-10A and MDA-MB-436 TNBC cell lines. This intervention significantly downregulated GPR161 expression in both cell lines compared to control shRNA. Interestingly, the knockdown of GPR161 had no notable impact on the proliferation of nontransformed MCF-10A cells. In contrast, the proliferation of MDA-MB-436 cells decreased by over twofold, suggesting that these cancer cells exhibit a reliance on GPR161-regulated pathways for their growth. In summary, this study demonstrates that GPR161 plays a crucial role in regulating proliferation within breast cancer cells, highlighting its significance in this context.
Ref: Feigin, Michael E., et al. "G-protein-coupled receptor GPR161 is overexpressed in breast cancer and is a promoter of cell proliferation and invasion." Proceedings of the National Academy of Sciences 111.11 (2014): 4191-4196.
Pubmed: 24599592
DOI: 10.1073/pnas.1320239111
Research Highlights
Nie Y, et al. "Specific binding of GPR174 by endogenous lysophosphatidylserine leads to high ." Nature communications, 2023.
Previous research has shown that several orphan G protein-coupled receptors (GPCRs), including GPR61, GPR161, and GPR174, have unknown ligands, making them difficult to study. However, a recent study has found that these receptors exhibit similar increases in cAMP levels as the fully activated D1 dopamine receptor (D1R). The study also used cryo-electron microscopy to determine the structures of the GPR61,ÄíG(s), GPR161,ÄíG(s), and GPR174,ÄíG(s) complexes without any added ligands. Interestingly, the GPR174 structure revealed that an endogenous molecule called lysophosphatidylserine (lysoPS) was present. Although GPR174 did not respond to exogenous lysoPS due to its maximum activation by the endogenous ligand, mutant versions of the receptor with lower ligand binding affinities were specifically activated by lysoPS in a dose-dependent manner. These findings not only confirm lysoPS as an endogenous ligand for GPR174, but also suggest that some orphan GPCRs may have naturally abundant ligands that contribute to their high constitutive activity. Further analysis of the structures of GPR161 and GPR61 also revealed that the second extracellular loop (ECL2) of these receptors may play a role in their constitutive activity by interacting with the orthosteric pocket. This study provides valuable insights into the activation and function of orphan GPCRs and emphasizes the importance of understanding their endogenous ligands.
Pubmed:
37737235
DOI:
10.1038/s41467-023-41654-3
Kim SE, et al. "Pax3 lineage-specific deletion of Gpr161 is associated with spinal neural tube ." bioRxiv : the preprint server for biology, 2023.
They discusses the effectiveness of mindfulness-based interventions for individuals with chronic pain. It reviews various studies that have examined the relationship between mindfulness practices and pain reduction, as well as the potential mechanisms underlying this relationship. The results suggest that mindfulness-based interventions can be beneficial in reducing pain and improving overall well-being for individuals with chronic pain. Additionally, the authors highlight the need for further research in this area, particularly regarding the long-term effects of mindfulness practices on pain management.
Pubmed:
37391407
DOI:
10.1038/s41392-023-01508-2
