mProX™ Human SSTR3 Stable Cell Line
- Product Category:
- Membrane Protein Stable Cell Lines
- Subcategory:
- GPCR Cell Lines
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Published Data
Fig.1 SSTR phosphorylation of SSTRs in HEK293 cells.
SSTR3 is phosphorylated in HEK293 cells with ITF2984 specificity. HEK293 cells that were transiently transfected with HA-SSTR3 were treated for 5 minutes at 37 °C with 10 M SST-14, Octreotide, Pasireotide, or ITF2984. After being lysed, cells were immunoblotted using the phosphosite-specific antibodies that were listed.
Ref: Modena, Daniela, et al. "Identification of a Novel SSTR3 Full Agonist for the Treatment of Nonfunctioning Pituitary Adenomas." Cancers 15.13 (2023): 3453.
Pubmed: 37444563
DOI: 10.3390/cancers15133453
Research Highlights
In a mouse model of glucose excursion, the imidazolyl-tetrahydro-β-carboline class of sstr3 antagonists showed effectiveness and may have therapeutic potential for type 2 diabetes. The oral, telemetrized cardiovascular (CV) pups that were tested with the initial candidate in this class experienced unacceptable QTc interval prolongation.
Shah, Shrenik K., et al. "Discovery of MK-1421, a potent, selective sstr3 antagonist, as a development candidate for type 2 diabetes." ACS Medicinal Chemistry Letters 6.5 (2015): 513-517.
Pubmed:
26005524
DOI:
10.1021/ml500514w
These results imply that the function of somatostatin analogue therapy, whether radiolabeled or not, should be reevaluated in light of the underlying SDHB immunohistochemical pattern.
Elston, Marianne S., et al. "Increased SSTR2A and SSTR3 expression in succinate dehydrogenase-deficient pheochromocytomas and paragangliomas." Human pathology 46.3 (2015): 390-396.
Pubmed:
25554089
DOI:
10.1016/j.humpath.2014.11.012