摘要
恶性肿瘤(癌症)是尚未被攻克的重大疾病之一,主要原因之一是临床上抗肿瘤药物效用不大.具有抗肿瘤活性的阳离子肽(CAP)主要结合肿瘤细胞膜并破坏膜结构,这是通过肽的正电荷与肿瘤细胞膜的负电荷之静电吸引来实现的.与传统化疗药物相比,绕过肿瘤细胞的耐药机制是CAP最突出的优势.本文对抗肿瘤肽的主要结构特征、抗肿瘤效果和抗肿瘤机制(以鲎素为例)进行了综述.作者认为,寻找靶向肿瘤干细胞的CAP对于治愈肿瘤具有特别重要的意义.另外,通过化学改构和新剂型研制,CAP将具有高靶向性和低毒性,给抗肿瘤药物开发提供新的动力.
Malignant tumor is one of the intractable, deadly diseases, which threaten human lives, killing more than ten millions of people in the world per year. The main cause for that is the weak anticancer drug used in clinic. Cationic amphiphilic peptides with anti-cancer activity share a common membranolytic mode of action that result either in the selective disruption of the cancer cell membrane or permeation and swelling of mitochondria. The electrostatic attraction between the negatively charged components of cancer cells and the positively charged peptides is believed to play a major role in the strong binding and selective disruption of cancer cell membranes. The ability of the peptides to bypass established resistance mechanisms in cancer cells is the most significant advantage compared with traditional anti-cancer agents. The structural features of the peptides and the action mechanism for anti-cancer are summarized in the present paper. The authors suggest that spotting the peptides targeting cancer stem cells is very important for cancer treatment and endowing anticancer peptides with improved pharmacokinetic properties and low toxicity will open up new ways to fully exploit their therapeutic potential.
出处
《深圳职业技术学院学报》
CAS
2013年第1期28-34,共7页
Journal of Shenzhen Polytechnic
基金
广东省自然科学基金(编号:10151805501000007)
深圳市科技基金(编号:2111K3070010)资助项目
关键词
抗肿瘤阳离子肽
结构特征
作用机制
靶向性
cationic amphiphilic peptides
structural feature
action mechanism for anti-cancer
targeting
