TT-232

TT-232 is a synthetic cyclic heptapeptide and structural analogue of somatostatin. It acts as an agonist primarily at the somatostatin receptor subtypes SSTR1 and SSTR4. Unlike traditional somatostatin analogues, TT-232 does not inhibit growth hormone release or gastric acid secretion. Its mechanism of action involves activation of SSTR1/SSTR4 receptors leading to cell cycle arrest and induction of apoptosis in tumor cells. Additionally, it inhibits tyrosine kinases by interfering with proliferative signaling cascades and interacts with intracellular targets such as pyruvate kinase M2 (PKM2), causing its nuclear translocation and further promoting apoptosis. Preclinical studies demonstrated pronounced antiproliferative effects against a broad range of human tumor cell lines (including colon, pancreas, lymphoma, leukemia, melanoma, hepatoma) as well as efficacy in animal models for various cancers. The compound also exhibits anti-inflammatory and analgesic properties without significant endocrine side effects seen with other somatostatin analogues. Despite promising early-phase clinical results showing low toxicity and good tolerability in cancer patients (notably metastatic renal cell carcinoma), development was discontinued after phase I/II trials[1][3][4][5][6][7].

Other names

D-Phe-Cys-Tyr-D-Trp-Lys-Cys-Thr-NH2D-Phe-Cys-Tyr-D-Trp-Lys-Cys-Thr-NH-2D-Phe-Cys-Tyr-D-Trp-Lys-Cys-Thr-NH 2