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

被引：4
|
作者：
Deng, Xin [1 ]
Qiu, Qianqian [1 ]
Ma, Ke [2 ]
Huang, Wenlong [1 ]
Qian, Hai [1 ]
机构：
[1] China Pharmaceut Univ, Ctr Drug Discovery, State Key Lab Nat Med, Nanjing 210009, Jiangsu, Peoples R China
[2] Nanjing Med Univ, Atherosclerosis Res Ctr, Key Lab Cardiovasc Dis & Mol Intervent, Nanjing 210009, Jiangsu, Peoples R China
来源：
AMINO ACIDS | 2015年 / 47卷 / 11期
基金：
中国国家自然科学基金;
关键词：
Anti-cancer; Apoptosis; Conjugation; Luteinizing hormone-releasing hormone; Peptide; PROSTATE-CANCER; CYTOCHROME-C; ANALOGS; RECEPTORS; APOPTOSIS; LHRH; TUMORS;
D O I：
10.1007/s00726-015-2021-2
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
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.
引用
收藏
页码：2359 / 2366
页数：8
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