Synthesis and in vitro anti-cancer evaluation of luteinizing hormone-releasing hormone-conjugated peptide.

Abstract

Luteinizing hormone-releasing hormone (LHRH) is a decapeptide hormone released from the hypothalamus and shows high affinity binding to the LHRH receptors. It is reported that several cancer cells also express LHRH receptors such as breast, ovarian, prostatic, bladder and others. In this study, we linked B1, an anti-cancer peptide, to LHRH and its analogs to improve the activity against cancer cells with LHRH receptor. Biological evaluation revealed that TB1, the peptide contains triptorelin sequence, present favorable anti-cancer activity as well as plasma stability. Further investigations disclosed that TB1 trigger apoptosis by activating the mitochondria-cytochrome c-caspase apoptotic pathway, it also exhibited the anti-migratory effect on cancer cells.

• Authors: Xin Deng, Qianqian Qiu, Ke Ma, Wenlong Huang, Hai Qian
• Journal: Amino acids (Amino Acids) Vol. 47 Issue 11 Pg. 2359-66 (Nov 2015) ISSN: 1438-2199 [Electronic] Austria
• PMID: 26058357 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Antineoplastic Agents
• Gonadotropin-Releasing Hormone

Topics

• Animals
• Antineoplastic Agents (chemical synthesis, chemistry, pharmacology)
• Apoptosis (drug effects)
• Drug Screening Assays, Antitumor
• Female
• Gonadotropin-Releasing Hormone (chemical synthesis, chemistry, pharmacology)
• HEK293 Cells
• HeLa Cells
• Humans
• K562 Cells
• MCF-7 Cells
• Male
• Neoplasms (drug therapy, metabolism, pathology)
• Rabbits