Advances in targeting the folate receptor in the treatment/imaging of cancers.

Advances in targeting the folate receptor in the treatment/imaging of cancers.
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DOI:
10.1039/c7sc04004k
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发表时间:
2018-01-28
期刊:
影响因子:
8.4
通讯作者:
Chudasama V
Chudasama V
中科院分区:
化学1区
文献类型:
--
作者:
Fernández M;Javaid F;Chudasama V

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叶酸受体(FR)是许多癌症的重要生物标志物,其在肿瘤上的过表达可用于靶向治疗,诊断和成像。叶酸受体(FR)是一种公认的肿瘤细胞生物标志物,因为它在大量肿瘤中过表达。因此,FR已被许多诊断和治疗工具利用,以允许靶向递送至癌细胞并对癌细胞成像。在本文中,我们描述了许多不同的方法,通过这些方法已经实现了这一点,包括将叶酸与有效的化疗药物连接以形成FR靶向小分子-药物缀合物(SMDC)、FR靶向抗体(作为单独的抗体和作为抗体-药物缀合物)和互补纳米技术-叶酸平台的形式;以及其成像变体。利用FR进行靶向治疗/成像的潜力有可能彻底改变几种癌症的治疗方式。这些FR靶向技术还可以为激发进一步复杂的药物缀合物铺平道路,特别是因为该受体正在通过使用几种互补技术(小分子、纳米颗粒和基于蛋白质的技术)来靶向,从而提供该领域广泛而独特的知识。
The folate receptor (FR) is an important biomarker for many cancers, and its overexpression on tumours can be exploited for targeted therapy, diagnosis and imaging. The folate receptor (FR) is a recognised biomarker for tumour cells due to its overexpression on a large number of tumours. Consequently, the FR has been exploited by many diagnostic and therapeutic tools to allow targeted delivery to, and imaging of, cancer cells. Herein, we describe the many different approaches by which this has been achieved, including the attachment of folate to potent chemotherapeutic drugs to form FR-targeting small molecule–drug conjugates (SMDCs), FR-targeting antibodies (as antibody alone and as an antibody–drug conjugate), and in the form of complementary nanotechnology–folate platforms; as well as imaging variants thereof. The potential of exploiting the FR for targeted therapy/imaging has the potential to revolutionise the way several cancers are treated. These FR-targeted technologies can also pave the way for inspiring further sophisticated drug conjugates, especially as this receptor is being targeted by use of several complementary technologies: small molecule, nanoparticle and protein-based – thus providing broad and distinct knowledge in the area.
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