Division of Molecular and Cellular Pathology, Niigata University Graduate School of Medical and Dental Sciences, Niigata, Japan.
Cancer Sci. 2021 Jun;112(6):2118-2125. doi: 10.1111/cas.14909. Epub 2021 May 7.
Cell-penetrating peptides, such as antibodies, have gained great attention as tools for the development of specific delivery systems for payloads, which might be applied as non-invasive carriers in vivo. Among these, tumor-homing peptides recently have been studied for use in tumor medicine. Tumor-homing peptides are oligopeptides, usually consisting of 30 or fewer amino acids that are efficiently and specifically incorporated into tumor cells, suggesting their potential use in establishing novel non-invasive tumor imaging systems for diagnostic and therapeutic applications. Here, we briefly introduce the biological characteristics of our tumor-homing peptides, focusing especially on those developed using a random peptide library constructed using mRNA display technology. The advantage of the tumor-homing peptides is their biological safety, given that these molecules do not show significant cytotoxicity against non-neoplastic cells; lack serious antigenicity, which alternatively might evoke unfavorable immune responses and inflammation in vivo; and are rapidly incorporated into target cells/tissues, with rates exceeding those seen for antibodies. Given their small size, tumor-homing peptides also are easy to modify and redesign. Based on these merits, tumor-homing peptides are expected to find wide application in various aspects of tumor medicine, including imaging diagnostics (eg, with dye-conjugated probes for direct visualization of invasive/metastatic tumor lesions in vivo) and therapeutics (eg, using peptide-drug conjugates [PDCs] for tumor targeting). Although further evidence will be required to demonstrate their practical utility, tumor-homing peptides are expected to show great potential as a next-generation bio-tool contributing to precision medicine for cancer patients.
细胞穿透肽,如抗体,作为载药的特异性递药系统的工具得到了广泛关注,其可作为非侵入性载体在体内应用。其中,肿瘤归巢肽最近已被研究用于肿瘤医学。肿瘤归巢肽是由 30 个或更少的氨基酸组成的寡肽,能够有效地、特异性地被肿瘤细胞摄取,这表明它们可能用于建立新的非侵入性肿瘤成像系统,用于诊断和治疗应用。在这里,我们简要介绍了我们的肿瘤归巢肽的生物学特性,特别是使用基于 mRNA 展示技术构建的随机肽文库开发的肿瘤归巢肽。这些肿瘤归巢肽的优点在于其生物学安全性,因为这些分子对非肿瘤细胞没有明显的细胞毒性;缺乏严重的抗原性,否则可能会在体内引起不利的免疫反应和炎症;并且可以快速进入靶细胞/组织,其进入速度超过抗体。由于其体积小,肿瘤归巢肽也易于修饰和重新设计。基于这些优点,肿瘤归巢肽有望在肿瘤医学的各个方面得到广泛应用,包括成像诊断(例如,用染料偶联探针直接可视化体内侵袭性/转移性肿瘤病变)和治疗(例如,使用肽-药物偶联物 [PDC] 进行肿瘤靶向)。尽管还需要进一步的证据来证明其实际用途,但肿瘤归巢肽有望作为下一代生物工具,为癌症患者的精准医学做出巨大贡献。