Gautam A, Kapoor P, Chaudhary K, Kumar R, Raghava G P S
Bioinformatics Centre, CSIRInstitute of Microbial Technology, Chandigarh-160036, India.
Curr Med Chem. 2014;21(21):2367-91. doi: 10.2174/0929867321666140217122100.
Cancer is one of the leading causes of mortality worldwide, with more than 10 million new cases each year. Despite the presence of several anticancer agents, cancer treatment is still not very effective. Main reasons behind this high mortality rate are the lack of screening tests for early diagnosis, and non-availability of tumor specific drug delivery system. Most of the current anticancer drugs are unable to differentiate between cancerous and normal cells, leading to systemic toxicity, and adverse side effects. In order to tackle this problem, a considerable progress has been made over the years to identify peptides, which specifically bind to the tumor cells, and tumor vasculature (tumor homing peptides). With the advances in phage display technology, and combinatorial libraries like one-bead one-compound library, several hundreds of tumor homing peptides, and their derivatives, which have potential to detect tumor in vivo, and deliver anticancer agents specifically to the tumor site, have been discovered. Currently, many tumor homing peptide-based therapies for cancer treatment and diagnosis are being tested in various phases of clinical trials. In this review, we have discussed the progress made so far in the identification of tumor homing peptides, and their applications in cancer therapeutics, diagnosis, and theranostics. In addition, a brief discussion on tumor homing peptide resource, and in silico designing of tumor homing peptides has also been provided.
癌症是全球主要的死亡原因之一,每年新增病例超过1000万。尽管有多种抗癌药物,但癌症治疗仍然效果不佳。高死亡率背后的主要原因是缺乏用于早期诊断的筛查测试,以及肿瘤特异性药物递送系统的不可用。目前大多数抗癌药物无法区分癌细胞和正常细胞,导致全身毒性和不良副作用。为了解决这个问题,多年来在鉴定能特异性结合肿瘤细胞和肿瘤脉管系统的肽(肿瘤归巢肽)方面取得了相当大的进展。随着噬菌体展示技术和单珠单化合物库等组合文库的发展,已经发现了数百种有潜力在体内检测肿瘤并将抗癌药物特异性递送至肿瘤部位的肿瘤归巢肽及其衍生物。目前,许多基于肿瘤归巢肽的癌症治疗和诊断疗法正在临床试验的各个阶段进行测试。在这篇综述中,我们讨论了到目前为止在肿瘤归巢肽鉴定方面取得的进展,以及它们在癌症治疗、诊断和治疗诊断学中的应用。此外,还简要讨论了肿瘤归巢肽资源以及肿瘤归巢肽的计算机辅助设计。