Skip to main content
padlock icon - secure page this page is secure

Synthesis and In Vitro Study of the Anticancer Activity of New Analogs of Octreotide

Buy Article:

$68.00 + tax (Refund Policy)

Based on the structure of Octreotide (SMS 201-995) some modified at positions 5 with Dap (diaminopropanoic acid), Dab (diaminobutanoic acid) and Orn new C-amide analogs were synthesized. The Thr6 was replaced by unnatural amino acids Tle (t-leucine). The cytotoxic effects of the novel compounds were tested in vitro against a panel of human tumor cell lines. All investigated compounds exhibited different concentration-dependent antiproliferative effects against the HT-29, MDA-MB-231, HepG2 and HeLa cell lines after 24 h treatment. The compound 2 (D-Phe-c(Cys-Phe-D-Trp- Dap-Tle-Cys)-Thr-NH2) had antiproliferative effects on MDA-MB-231 cells with the IC50 0.03 mM. The HeLa and HepG-2 cells were most sensitive towards tested compounds at various concentrations. Results demonstrated that the peptide analogs 3 (D-Phe-c(Cys-Phe-D-Trp-Lys-Tle-Cys)-Thr-NH2), 4 (D-Phe-c(Cys-Phe-D-Trp-Orn-Tle-Cys)-Thr-NH2) and 5 (RC-102) exert the most pronounced inhibition of the cell vitality up to 77% at higher concentrations and were not toxic to the normal Lep-3 cells.
No References
No Citations
No Supplementary Data
No Article Media
No Metrics

Keywords: Cytotoxic; G-protein-coupled receptors; SPPS; carcinoid syndrome; growth hormone; neuroendocrine tumors; octreotide; peptide receptor; somatostatin analogs; unnatural amino acids

Document Type: Research Article

Publication date: December 1, 2012

More about this publication?
  • Protein & Peptide Letters publishes short papers in all important aspects of protein and peptide research, including structural studies, recombinant expression, function, synthesis, enzymology, immunology, molecular modeling, drug design etc. Manuscripts must have a significant element of novelty, timeliness and urgency that merit rapid publication. Reports of crystallisation, and preliminary structure determinations of biologically important proteins are acceptable. Purely theoretical papers are also acceptable provided they provide new insight into the principles of protein/peptide structure and function.
  • Editorial Board
  • Information for Authors
  • Subscribe to this Title
  • Ingenta Connect is not responsible for the content or availability of external websites
  • Access Key
  • Free content
  • Partial Free content
  • New content
  • Open access content
  • Partial Open access content
  • Subscribed content
  • Partial Subscribed content
  • Free trial content
Cookie Policy
Cookie Policy
Ingenta Connect website makes use of cookies so as to keep track of data that you have filled in. I am Happy with this Find out more