The product is a potent and selective agonist of the
SSTR5 (somatostatin 5) receptor and the sixth molecule designed by the company using its GPCR Structure-Based Drug Design (SBDD) platform to enter clinical development.
DOTATOC shows the highest affinity for the SSTR2 receptor with a weaker affinity for SSTR3 and
SSTR5. (1)
[SUV.sub.max] of PanNEN was higher than that of GINENs, which was consistent with prior studies [21,22], where the investigators found higher levels of messenger RNA expression of SSTR2 and
SSTR5 in pancreatic than in gastrointestinal NENs.
[sup.68]Ga-DOTA peptides bind to SSTRs, in particular SSTR3 and
SSTR5, both of which are usually overexpressed in neuroendocrine cells [24].
CC1 pretreatment was performed using the OptiView method for 8-72 min (except for SSTR3 with protease pretreatment for 4 min), followed by incubation with primary antibodies (SSTR1: 1:3000 (Gramsch, Schwabhausen, Germany), SSTR2A: 1: 500 (Dianova, Hamburg, Germany), SSTR3: 1: 250 (Abcam, Cambridge, United Kingdom), SSTR4: 1: 1000 (Gentex, Zeeland, United States),
SSTR5: 1:100 (Abcam, Cambridge, United Kingdom), alpha-subunit: 1: 400 (Immunotech, Prague, Czech Republic), PIT-1: 1:200 (8 min) (Cell Signaling Technology, Danvers, United States)) at 37[degrees]C for 32 min if not stated otherwise.
Octreotide: Octreotide, is an eight amino acid, synthetic, long-acting somatostatin analogue that inhibits insulin secretion by binding to somatostatin receptors 2 and 5 (SSTR2 and
SSTR5) (110).
This study aimed to evaluate short-term preoperative octreotide (OCT) use in TSHoma patients and to investigate SSTR2 and
SSTR5 expression and observe structural changes in tumor tissue.
The
SSTR5 has been found to preferentially bind SS-28 rather than SS-14 (Patel et al., 1994).
Duan et al., "Somatostatin receptors SSTR2 and
SSTR5 are expressed in the human thoracic duct," Lymphology, vol.
His result was SSTR2 (2+),
SSTR5 (2+), and mTOR (-).
In particular, [sup.68]Ga-DOTANOC also shows a good affinity for SSTR subtypes 3 and 5, [sup.68]Ga-DOTATOC also binds to
SSTR5 (although with lower affinity than DOTANOC), while [sup.68]Ga-DOTATATE has a predominant affinity for SSTR2 [19].