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Non-internalizing antibody-drug conjugates display potent anti-cancer activity upon proteolytic release of monomethyl auristatin E in the subendothelial extracellular matrix.非内化抗体药物偶联物在蛋白水解作用下于内皮下细胞外基质中释放单甲基奥瑞他汀E后展现出强大的抗癌活性。
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DNA-encoded chemistry: enabling the deeper sampling of chemical space.DNA 编码化学:实现更深入的化学空间采样。
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Novel antibody-antibiotic conjugate eliminates intracellular S. aureus.新型抗体-抗生素偶联物消除细胞内金黄色葡萄球菌。
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细胞毒性药物的靶向递送:挑战、机遇与新进展

Targeted Delivery of Cytotoxic Drugs: Challenges, Opportunities and New Developments.

作者信息

Cazzamalli Samuele, Corso Alberto Dal, Neri Dario

机构信息

Department of Chemistry and Applied Biosciences Swiss Federal Institute of Technology (ETH Zurich) Vladimir-Prelog-Weg 4, CH-8093 Zurich.

Department of Chemistry and Applied Biosciences Swiss Federal Institute of Technology (ETH Zurich) Vladimir-Prelog-Weg 4, CH-8093 Zurich;, Email:

出版信息

Chimia (Aarau). 2017 Oct 25;71(10):712-715. doi: 10.2533/chimia.2017.712.

DOI:10.2533/chimia.2017.712
PMID:29070415
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC5844459/
Abstract

Cytotoxic drugs, which are commonly used for the pharmacotherapy of many forms of cancer, often cause substantial toxicity to the patient without being able to induce long-lasting remissions. Ligands specific to accessible tumor-associated targets, capable of selective localization at the neoplastic site, may facilitate the preferential delivery of anti-cancer drugs, boosting activity and helping spare normal organs. In this article, we present a critical analysis of the limitation of conventional anti-cancer drugs and we contrast monoclonal antibodies and small organic ligands, as vehicles for pharmacodelivery applications.

摘要

细胞毒性药物常用于多种癌症的药物治疗,但往往会给患者带来严重毒性,却无法诱导长期缓解。对可及的肿瘤相关靶点具有特异性的配体,能够选择性地定位于肿瘤部位,可能有助于抗癌药物的优先递送,增强活性并帮助保护正常器官。在本文中,我们对传统抗癌药物的局限性进行了批判性分析,并对比了单克隆抗体和有机小分子配体作为药物递送应用载体的情况。