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Chemical Compound Review

TT-232     (4S,7S,13S,16S)-7-(4- aminobutyl)-N-[(1S...

Synonyms: LS-153742, TT 232, AC1L4UU1, C53H72N12O10S2
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Disease relevance of TT-232


High impact information on TT-232

  • The SOM receptor antagonist cyclosomatostatin (c-SOM; 20 microg/kg) or, in another group, the synthetic heptapeptide agonist TT-232 (2 x 50-400 microg/kg) was administered intraperitoneally every day [4].
  • Lipoamino acid and liposaccharide conjugates of somatostatin analogue TT-232 were synthesized to modify the physicochemical properties of the parent peptide [5].
  • A novel somatostatin analogue, TT-232 (which inhibits the proliferation of various cell cultures and transplantable mouse tumours), was examined regarding its effect on human melanoma and lymphoma xenografts as a single treatment or in combination with DTIC (dacarbazine) and etoposide [1].
  • TT-232 inhibited the growth of all of the cell lines used in this study and induced apoptotic cell death [3].
  • We found a significant PTPase stimulation after TT-232 administration using an immunoblot analysis assessing the level of protein tyrosine phosphorylation, and also a direct measurement of the PTPase activity [3].

Biological context of TT-232


Anatomical context of TT-232

  • TT-232 (up to 5 mg/kg i.p.) did not induce mucosal lesions in either the stomach or the duodenum.These data suggest that TT-232, a somatostatin analogue devoid of endocrine effects, is a promising lead molecule in the search for novel, broad-spectrum anti-inflammatory and analgesic agents [10].
  • In accordance, in vitro binding experiments indicated high-affinity binding of TT-232 to (125)I labelled somatostatin sites in brain membranes [11].
  • Cutaneous neutrophil accumulation over a 3-h period after intradermal (i.d.) injection of carrageenin (1 mg/site) or interleukin 1beta (IL-1beta, 3 pmol/site) was inhibited significantly by TT-232 (3x80 microg/kg i.v.), while diclofenac (3x10 mg/kg i.v.) elicited significant inhibition only in the IL-1beta test [10].
  • TT-232 has no growth hormone release inhibitory effect and does not inhibit the secretion of gastric acid [12].
  • 3H-labeled TT-232 could be detected on the cell surface, on cytoplasmic membranes and also in the nucleus of HT-29 cells, 1-6 h after the administration of 0.5 and 50 microg/mL [3H]TT-232 [13].

Associations of TT-232 with other chemical compounds

  • 2. Cyclic synthetic octapeptide (TT-248 and TT-250) and heptapeptide (TT-232) somatostatin analogues proved to be more effective in reducing neurogenic and non-neurogenic inflammatory reactions but octreotide had no influence on either neurogenic or non-neurogenic inflammation [14].
  • The anti-inflammatory action of TT-232 is mediated through the SSTR4 receptor, and its antitumor activity is mediated through the SSTR1 receptor and by the tumor-specific isoform of pyruvate kinase [15].
  • In order to study the structure-activity relationships of TT-232, we designed and synthesized an analog of TT-232, namely Lan-7, in which the disulfide bridge is replaced by a lanthionine monosulfide bridge [16].

Gene context of TT-232

  • Taken together, we demonstrate the physical and functional association between PI 3-kinase, PKCdelta and PTPalpha in a signaling complex that mediates the antitumor activity of the somatostatin analogue TT-232 [9].
  • Blocking the signalling to ERK or p38MAPK activation had no effect on the TT-232-induced cell killing [6].
  • Our data suggest that TT-232 triggers an apoptotic type of cell death, concomitant with a strong activation of JNK and a blockade of cellular ERK2 activation pathways [6].
  • The antitumor somatostatin analogue TT-232 induces cell cycle arrest through PKCdelta and c-Src [7].
  • Pharmacological characterisation of the somatostatin analogue TT-232: effects on neurogenic and non-neurogenic inflammation and neuropathic hyperalgesia [10].

Analytical, diagnostic and therapeutic context of TT-232


  1. Effect of a novel somatostatin analogue combined with cytotoxic drugs on human tumour xenografts and metastasis of B16 melanoma. Szende, B., Horváth, A., Bökönyi, G., Kéri, G. Br. J. Cancer (2003) [Pubmed]
  2. Apoptosis is induced in both drug-sensitive and multidrug-resistant hepatoma cells by somatostatin analogue TT-232. Diaconu, C.C., Szathmári, M., Kéri, G., Venetianer, A. Br. J. Cancer (1999) [Pubmed]
  3. Antiproliferative activity induced by the somatostatin analogue, TT-232, in human pancreatic cancer cells. Lee, J.U., Hosotani, R., Wada, M., Doi, R., Koshiba, T., Fujimoto, K., Miyamoto, Y., Tsuji, S., Nakajima, S., Hirohashi, M., Uehara, T., Arano, Y., Fujii, N., Imamura, M. Eur. J. Cancer (2002) [Pubmed]
  4. Antiinflammatory and analgesic effects of somatostatin released from capsaicin-sensitive sensory nerve terminals in a Freund's adjuvant-induced chronic arthritis model in the rat. Helyes, Z., Szabó, A., Németh, J., Jakab, B., Pintér, E., Bánvölgyi, A., Kereskai, L., Kéri, G., Szolcsányi, J. Arthritis Rheum. (2004) [Pubmed]
  5. Novel lipoamino acid- and liposaccharide-based system for peptide delivery: application for oral administration of tumor-selective somatostatin analogues. Tóth, I., Malkinson, J.P., Flinn, N.S., Drouillat, B., Horváth, A., Erchegyi, J., Idei, M., Venetianer, A., Artursson, P., Lazorova, L., Szende, B., Kéri, G. J. Med. Chem. (1999) [Pubmed]
  6. The somatostatin analogue TT-232 induces apoptosis in A431 cells: sustained activation of stress-activated kinases and inhibition of signalling to extracellular signal-regulated kinases. Vántus, T., Kéri, G., Krivickiene, Z., Valius, M., Steták, A., Keppens, S., Csermely, P., Bauer, P.I., Bökönyi, G., Declercq, W., Vandenabeele, P., Merlevede, W., Vandenheede, J.R. Cell. Signal. (2001) [Pubmed]
  7. The antitumor somatostatin analogue TT-232 induces cell cycle arrest through PKCdelta and c-Src. Steták, A., Lankenau, A., Vántus, T., Csermely, P., Ullrich, A., Kéri, G. Biochem. Biophys. Res. Commun. (2001) [Pubmed]
  8. The somatostatin analogue peptide TT-232 induces apoptosis and chromosome breakage in cultured human lymphocytes. Tompa, A., Jakab, M.G., Major, J., Idei, M., Bocsi, J., Mihalik, R., Szende, B., Kéri, G. Mutat. Res. (2000) [Pubmed]
  9. Physical and functional interactions between protein tyrosine phosphatase alpha, PI 3-kinase, and PKCdelta. Steták, A., Csermely, P., Ullrich, A., Kéri, G. Biochem. Biophys. Res. Commun. (2001) [Pubmed]
  10. Pharmacological characterisation of the somatostatin analogue TT-232: effects on neurogenic and non-neurogenic inflammation and neuropathic hyperalgesia. Pintér, E., Helyes, Z., Németh, J., Pórszász, R., Pethö, G., Thán, M., Kéri, G., Horváth, A., Jakab, B., Szolcsányi, J. Naunyn Schmiedebergs Arch. Pharmacol. (2002) [Pubmed]
  11. Binding crevice for TT-232 in a homology model of type 1 somatostatin receptor. Simon, A., Czajlik, A., Perczel, A., Kéri, G., Nyikos, L., Emri, Z., Kardos, J. Biochem. Biophys. Res. Commun. (2004) [Pubmed]
  12. TT-232: a somatostatin structural derivative as a potent antitumor drug candidate. Szende, B., Kéri, G. Anticancer Drugs (2003) [Pubmed]
  13. A specifically radiolabeled somatostatin analog with strong antitumor activity induces apoptosis and accumulates in the cytosol and the nucleus of HT29 human colon carcinoma cells. Szegedi, Z., Takács, J., Szende, B., Vadász, Z., Horváth, A., Gulyás, E., Tóth, G., Peták, I., Bocsi, J., Kéri, G. Endocrine (1999) [Pubmed]
  14. Anti-inflammatory effect of synthetic somatostatin analogues in the rat. Helyes, Z., Pintér, E., Németh, J., Kéri, G., Thán, M., Oroszi, G., Horváth, A., Szolcsányi, J. Br. J. Pharmacol. (2001) [Pubmed]
  15. TT232, a novel signal transduction inhibitory compound in the therapy of cancer and inflammatory diseases. Szokolóczi, O., Schwab, R., Peták, I., Orfi, L., Pap, A., Eberle, A.N., Szüts, T., Kéril, G. J. Recept. Signal Transduct. Res. (2005) [Pubmed]
  16. Synthesis, conformational analysis and bioactivity of Lan-7, a lanthionine analog of TT-232. Li, H., Jiang, X., Howell, S.B., Goodman, M. J. Pept. Sci. (2000) [Pubmed]
  17. Evaluation of the antitumor efficacy of the somatostatin structural derivative TT-232 on different tumor models. Tejeda, M., Ga??l, D., Hull??n, L., Hegymegi-Barakonyi, B., K??ri, G. Anticancer Res. (2006) [Pubmed]
  18. Growth inhibitory effect of the somatostatin structural derivative (TT-232) on leukemia models. Tejeda, M., Gaál, D., Csuka, O., Kéri, G. Anticancer Res. (2005) [Pubmed]
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