United States Patent Application 20210018520: COMPOSITIONS FOR AND METHODS OF DIAGNOSING, PROGNOSING, AND TREATING DIABETES
LifeTein synthesized the S961 peptides. S961 is a biosynthetic insulin receptor antagonist that inhibits cell proliferation and colony formation in breast tumor cells. S961 peptide, a biosynthetic insulin receptor antagonist, downregulates insulin receptor expression and suppresses the growth of breast cancer cells. S961-treated rats can be successfully used to screen novel therapeutic interventions having the potential to improve glucose disposal through receptor-independent mechanisms.
Insulin binds to the insulin receptor (InsR), which exists in two alternatively spliced isoforms, InsR-A and InsR-B. The insulin receptor belongs to the same family of receptor tyrosine kinases as the IGF1 receptor (IGF1R) and insulin is therefore also able to bind to the IGF1R albeit with considerably lower affinity as compared to the InsR. S961 is a single-chain peptide consisting of 43 amino acids, which have been shown to be a specific InsR antagonist. The affinity of S961 for the InsR is comparable to that of human insulin and the selectivity for the insulin receptor versus the IGF1 receptor is higher than that of human insulin. S961 is also an antagonist of the InsR of other species such as pigs and rats and it also has a considerable affinity for hybrid receptors consisting of InsR and IGF1R. S961 completely inhibits insulin action, both in cellular assays and in vivo in rats.
Thus, S961 exhibit high affinity and selectivity for the InsR and can be used to unravel the role of InsR signaling and function in both in vivo and in vitro experiments.
One Amino Acid Sequence: GSLDESFYDWFERQLGGGSGGSSLEEEWAQIQCEVWGRGCPSY, trifluoroacetate salt; Cys33-Cys40; CAS Number: 1083433-49-1;
Three Amino Acid Sequence: Gly-Ser-Leu-Asp-Glu-Ser-Phe-Tyr-Asp-Trp-Phe-Glu-Arg-Gln-Leu-Gly-Gly-Gly-Ser-Gly-Gly-Ser-Ser-Leu-Glu-Glu-Glu-Trp-Ala-Gln-Ile-Gln-Cys-Glu-Val-Trp-Gly-Arg-Gly-Cys-Pro-Ser-Tyr; Disulfide bridge: Cys33 - Cys40
Quantity: 15mg
Purity: >95%
Formula: C211H297N55O71S2
Molecular Weight: 4804.16
