Far-Red Light-Activatable Prodrug of Paclitaxel for the Combined Effects of Photodynamic Therapy and Site-Specific Paclitaxel Chemotherapy.
Far-Red Light-Activatable Prodrug of Paclitaxel for the Combined Effects of Photodynamic Therapy and Site-Specific Paclitaxel Chemotherapy.
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紫杉醇的远红色轻度前药，用于光动力疗法和特定部位特异性紫杉醇化学疗法的综合作用。
DOI：
10.1021/acs.jmedchem.5b01971
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发表时间：
2016-04-14
影响因子：
7.3
通讯作者：
You, Youngjae
中科院分区：
文献类型：
--
作者：
Thapa, Pritam;Li, Mengjie;Bio, Moses;Rajaputra, Pallavi;Nkepang, Gregory;Sun, Yajing;Woo, Sukyung;You, Youngjae
紫杉醇 (PTX) 是最有用的化疗药物之一，被批准用于治疗多种癌症，包括卵巢癌、乳腺癌、胰腺癌和非小细胞肺癌。然而，当肠胃外给药时，它会引起全身副作用。光动力疗法（PDT）是一种利用光和光敏剂治疗局部癌症的新策略。不幸的是，由于肿瘤消融不完全，PDT 后常常会出现复发。为了克服这些问题，我们通过单线态氧可裂解的氨基丙烯酸酯连接体结合光敏剂，制备了远红光激活的 PTX 前药。微管蛋白聚合增强和前药的细胞毒性显着降低。然而，一旦用远红光照射，该前药就会通过 PDT 和局部释放的 PTX 的综合作用有效杀死 SKOV-3 卵巢癌细胞。我们的药物是第一个可以通过组织可穿透且临床上有用的远红光被单线态氧激活的 PTX 前药，通过 PDT 和位点特异性 PTX 化疗的联合作用杀死癌细胞。
Paclitaxel (PTX) is one of the most useful chemotherapeutic agents approved for several cancers, including ovarian, breast, pancreatic, and non-small cell lung cancer. However, it causes systemic side effects when administered parenterally. Photodynamic therapy (PDT) is a new strategy for treating local cancers using light and photosensitizer. Unfortunately, PDT is often followed by recurrence, due to incomplete ablation of tumors. To overcome these problems, we prepared the far-red light-activatable prodrug of PTX by conjugating photosensitizer via singlet oxygen-cleavable aminoacrylate linker. Tubulin polymerization enhancement and cytotoxicity of prodrugs were dramatically reduced. However, once illuminated with far-red light, the prodrug effectively killed SKOV-3 ovarian cancer cells through the combined effects of PDT and locally released PTX. Ours is the first PTX prodrug that can be activated by singlet oxygen using tissue penetrable and clinically useful far-red light, which kills the cancer cells through the combined effects of PDT and site-specific PTX chemotherapy.
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DOI：
10.3322/caac.20114
发表时间：
2011-07
期刊：
CA: a cancer journal for clinicians
影响因子：
--
作者：
Agostinis P;Berg K;Cengel KA;Foster TH;Girotti AW;Gollnick SO;Hahn SM;Hamblin MR;Juzeniene A;Kessel D;Korbelik M;Moan J;Mroz P;Nowis D;Piette J;Wilson BC;Golab J
通讯作者：
Golab J
通过原药的双重活化实现抗癌药物的可见光控制释放
影响因子：
4.2
作者：
Hossion, Abugafar M. L.;Bio, Moses;You, Youngjae
通讯作者：
You, Youngjae
影响因子：
4.7
作者：
Khandare, Jayant J.;Jayant, Sreeja;Minko, Tamara
通讯作者：
Minko, Tamara
影响因子：
5.8
作者：
Crown, J;O'Leary, M;Ooi, WS
通讯作者：
Ooi, WS
影响因子：
3.1
作者：
Gennari, Alessandra;Guarneri, Valentina;Conte, Pier Franco
通讯作者：
Conte, Pier Franco