Somatostatin receptors are a subfamily of GPCRs and include five members. They are widely distributed throughout the central and peripheral nervous system and can bind endogenous somatostatin with a high affinity. The activation of somatostatin receptors triggers various signaling pathways, which are related to multiple crucial physiological activities such as the suppression of GH secretion and the regulation of neural activity. Consequently, it has immense importance for comprehensive investigations of somatostatin receptors.
Fig.1 sst5TMD4 overexpression and Glioblastoma therapy.1
In an attempt to help in the discovery of pharmaceuticals for the treatment of diseases, Creative Biolabs succeeded in developing a speedy and steady Magic™ in vitro cell-based somatostatin receptor functional assay service, which is currently offered to customers throughout the world.
The activation of somatostatin receptors triggers an array of cellular reactions to transduce the signals. Accordingly, we utilize the variation of second messengers or ion fluxes caused by the treatment of samples as the indicator of our Magic™ in vitro cell-based somatostatin receptor functional assay service. Also, we can examine the fluorescent intensity to detect the receptor internalization. At Creative Biolabs, the incorporation of our professional team and top-ranking services will enable the desirable outcomes for every customer at a rapid turnover.
Fig.2 Diagram illustrates the primary intracellular signaling pathways activated by somatostatin receptor agonist binding.2
Fig.3 Advantages of our Magic™ in vitro cell-based somatostatin receptor functional assay service.
Representative data 1: All five somatostatin receptors (SSTR1-5) may be activated by the endogenous cyclic tetradecapeptide SST14, leading to increased hormone production, improved neurotransmission, halted cell development, and reduced cancer risk. Researchers have created two short cyclic SST analogs (lanreotide or octreotide) that selectively activate SSTR2 to treat acromegalia and neuroendocrine tumors. Based on a structural analysis of the human SSTR2-Gi complex in the presence of SST14 and two short cyclic SST analogs, this study uncovered the critical site for receptor binding and functional stimulation of the two SST14-derived cyclic octapeptides, providing useful information for the design of SST analog drugs that target SSTR.
Fig.4 Comparison of Ca2+ accumulation in WT SSTR2 with SST14 and two short cyclic SST analogue mutants.3
Representative data 2: SST4 is a new pain medication target, particularly for chronic neuropathy. The research investigated the activation of SST4-coupled G protein and β-arrestin, as well as the in-silico binding on the cells expressing SST4. Moreover, the research examined the different concentrations of pyrrole-pyrimidine molecules' effect on specific mice pain models. Both in vitro and in vivo studies have shown that the new orally active drugs are effectively and potently agonistic to the SST4 receptor. G protein activation showed that all four new ligands were complete agonists, however, they were unable to recruit β-arrestin. These compounds show great promise as new drugs since a single oral dose has a significant antinociceptive impact in a neuropathic pain paradigm.
Fig.5 The β-arrestin 2 recruitment assay concentration-response curves for Compounds 1-4.4
Creative Biolabs is constantly optimizing technology and services to improve our competitiveness and contribute to the industry's development. We always insist on delivering high-quality results to every customer.
If you want to know more details about our Magic™ in vitro cell-based somatostatin receptor functional assay service, feel free to contact us at your convenience.
References
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