The use of therapeutic peptides to target and to kill cancer cells.
The use of therapeutic peptides to target and to kill cancer cells.
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DOI：
10.2174/092986712801661004
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发表时间：
2012
影响因子：
4.1
通讯作者：
Khaled AR
中科院分区：
文献类型：
--
作者：
Boohaker RJ;Lee MW;Vishnubhotla P;Perez JM;Khaled AR
肽治疗是一个有前途的领域，为新兴的抗癌药物。优点包括肽的容易和快速合成以及修饰能力。蛋白质结构和功能的现有和巨大的知识库可以用于新的肽设计。目前的研究重点是开发能够（1）作为肿瘤靶向部分和（2）渗透膜并产生细胞毒性后果的肽。对最近调查结果的一项调查显示了一些重大趋势。具有疏水性和阳离子残基簇的两亲性肽是抗微生物肽的特征，其赋予根除微生物的能力并显示出相当大的抗癌毒性。组装和形成孔的肽可以破坏细胞或细胞器膜并引起凋亡或坏死性死亡。细胞渗透性和肿瘤归巢肽可以将生物活性货物运送到肿瘤或肿瘤脉管系统。挑战在于开发治疗性肽的临床应用。改善对肿瘤的递送、最小化非特异性毒性作用和辨别药代动力学性质是生产用于癌症治疗的强大治疗肽的需求之一。
Peptide therapeutics is a promising field for emerging anti-cancer agents. Benefits include the ease and rapid synthesis of peptides and capacity for modifications. An existing and vast knowledge base of protein structure and function can be exploited for novel peptide design. Current research focuses on developing peptides that can (1) serve as tumor targeting moieties and (2) permeabilize membranes with cytotoxic consequences. A survey of recent findings reveals significant trends. Amphiphilic peptides with clusters of hydrophobic and cationic residues are features of anti-microbial peptides that confer the ability to eradicate microbes and show considerable anti-cancer toxicity. Peptides that assemble and form pores can disrupt cell or organelle membranes and cause apoptotic or necrotic death. Cell permeable and tumor-homing peptides can carry biologically active cargo to tumors or tumor vasculature. The challenge lies in developing the clinical application of therapeutic peptides. Improving delivery to tumors, minimizing non-specific toxic effects and discerning pharmacokinetic properties are high among the needs to produce a powerful therapeutic peptide for cancer treatment.