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
[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 .
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
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.
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 .