同样，Promega的Beta-Glo检测系统可测量β-arrestin的激活，β-arrestin是 GPCR 脱敏和内化的关键介质[8]...
This has led to the concept of ligand bias, the ability of compounds to selectively engage or inhibit different signaling pathways. The studies discussed in this review provide evidence for bias between G protein and β-arrestin pathway signaling. However, bias between other signaling pathways such...
et al. MicroRNA-100 suppresses the migration and invasion of breast cancer cells by targeting FZD-8 and inhibiting Wnt/beta-catenin signaling pathway. Tumour Biol. 37, 5001–5011 (2015). 64 McCabe, J. M. & Leahy, D. J. Smoothened goes molecular: new pieces in the hedgehog signaling ...
同样,Promega的Beta-Glo检测系统可测量 β-arrestin 的激活,β-arrestin是 GPCR 脱敏和内化的关键介质[8]。总之,验证 GPCR 的潜在激动剂或拮抗剂是药物开发的重要一步。通过使用这些检测方法,研究人员可以鉴定出对 GPCR 具有高亲和力和特异性的化合物,从而开发出有效且安全的疗法。Functional assays are used to ...
We deploy multiplexed detection for cAMP, calcium flux, IP1/IP3, and β-arrestin recruitment, covering Gi/Gs/Gq-coupled receptors. Customized reporter gene assays validate pathway-specific activation, critical for characterizing biased signaling in cancer immunotherapy and metabolic disorder targets like ...
MULTISCREEN™ Beta Arrestin Technology for Untagged GPCRs View Our Extensive Catalog of HTS-Ready Assays and Stable Cell Lines Explore Our Research Articles A legacy of excellence, a future of innovation Unrivaled Expertise • 100% service client return business and success rate ...
In this study, we showed that a ligand of PTHR1 (PTH1-11) that signals through all receptor-engaged pathways, albeit with moderately diminished potency for β-arrestin recruitment, can be converted to a ligand that is highly biased for signaling through the Gαs pathway through linkage with ...
Therefore, through the pan-GPCR cell library, drug safety can be evaluated based on mechanisms such as whether the drug inhibits the side effects caused by the β-arrestin signaling pathway. Evaluating the safety of known drugs using the pan-GPCR cell lines library offers numerous benefits. The...
2. Gurevich, V. V. & Gurevich, E. V. GPCR signaling regulation: the role of GRKs and arrestins. Front. Pharmacol. 10, 125 (2019). 3. Hauser, A. S., Attwood, M. M., Rask-Andersen, M., Schioth, H. B. & Gloriam, D. E. Trends in GPCR drug discovery: new agents, targets...
Spiegel A. CELL SIGNALING: beta-Arrestin--Not Just for G Protein-Coupled Receptors. Science. 2003 Sep 5;301(5638):1338-9. PubMed ID: * Review: GPCRs (Guanine Nucleotide Binding–Protein Coupled Receptors) comprise large and diverse gene families in fungi, plants, and the animal kingdom. ...