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CD44-Specific A6 Short Peptide Boosts Targetability and Anticancer Efficacy of Polymersomal Epirubicin to Orthotopic Human Multiple Myeloma.
Advanced Materials ( IF 27.4 ) Pub Date : 2019-09-27 , DOI: 10.1002/adma.201904742 Wenxing Gu 1, 2 , Jingnan An 3 , Hao Meng 1 , Na Yu 1 , Yinan Zhong 1 , Fenghua Meng 1 , Yang Xu 3 , Jeroen J L M Cornelissen 2 , Zhiyuan Zhong 1
Advanced Materials ( IF 27.4 ) Pub Date : 2019-09-27 , DOI: 10.1002/adma.201904742 Wenxing Gu 1, 2 , Jingnan An 3 , Hao Meng 1 , Na Yu 1 , Yinan Zhong 1 , Fenghua Meng 1 , Yang Xu 3 , Jeroen J L M Cornelissen 2 , Zhiyuan Zhong 1
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Chemotherapy is widely used in the clinic though its benefits are controversial owing to low cancer specificity. Nanovehicles capable of selectively transporting drugs to cancer cells have been energetically pursued to remodel cancer treatment. However, no active targeting nanomedicines have succeeded in clinical translation to date, partly due to either modest targetability or complex fabrication. CD44-specific A6 short peptide (KPSSPPEE) functionalized polymersomal epirubicin (A6-PS-EPI), which boosts targetability and anticancer efficacy toward human multiple myeloma (MM) in vivo, is described. A6-PS-EPI encapsulating 11 wt% EPI is small (≈55 nm), robust, reduction-responsive, and easy to fabricate. Of note, A6 decoration markedly augments the uptake and anticancer activity of PS-EPI in CD44-overexpressing LP-1 MM cells. A6-PS-EPI displays remarkable targeting ability to orthotopic LP-1 MM, causing depleted bone damage and striking survival benefits compared to nontargeted PS-EPI. Overall, A6-PS-EPI, as a simple and intelligent nanotherapeutic, demonstrates high potential for clinical translation.
中文翻译：
CD44特异的A6短肽增强了多聚表体表柔比星对原位人类多发性骨髓瘤的靶向性和抗癌功效。
尽管由于癌症特异性低，其益处尚存争议，但化学疗法已广泛用于临床。一直在努力地寻求能够将药物选择性地转移至癌细胞的纳米载体，以重塑癌症的治疗方法。然而，迄今为止，尚无有效的靶向纳米药物在临床上取得成功，部分原因是适度的靶向性或复杂的制备。描述了CD44特异性A6短肽（KPSSPPEE）功能化的聚合物表柔比星（A6-PS-EPI），可增强体内对人多发性骨髓瘤（MM）的靶向性和抗癌功效。封装了11 wt％EPI的A6-PS-EPI小（约55 nm），坚固，还原响应性强且易于制造。值得注意的是，A6修饰显着增强了CD44过表达的LP-1 MM细胞中PS-EPI的摄取和抗癌活性。与非靶向PS-EPI相比，A6-PS-EPI对原位LP-1 MM具有非凡的靶向能力，可导致骨耗竭和惊人的存活率。总体而言，A6-PS-EPI作为一种简单而智能的纳米治疗药物，具有很高的临床翻译潜力。
更新日期：2019-11-13
中文翻译：
CD44特异的A6短肽增强了多聚表体表柔比星对原位人类多发性骨髓瘤的靶向性和抗癌功效。
尽管由于癌症特异性低，其益处尚存争议，但化学疗法已广泛用于临床。一直在努力地寻求能够将药物选择性地转移至癌细胞的纳米载体，以重塑癌症的治疗方法。然而，迄今为止，尚无有效的靶向纳米药物在临床上取得成功，部分原因是适度的靶向性或复杂的制备。描述了CD44特异性A6短肽（KPSSPPEE）功能化的聚合物表柔比星（A6-PS-EPI），可增强体内对人多发性骨髓瘤（MM）的靶向性和抗癌功效。封装了11 wt％EPI的A6-PS-EPI小（约55 nm），坚固，还原响应性强且易于制造。值得注意的是，A6修饰显着增强了CD44过表达的LP-1 MM细胞中PS-EPI的摄取和抗癌活性。与非靶向PS-EPI相比，A6-PS-EPI对原位LP-1 MM具有非凡的靶向能力，可导致骨耗竭和惊人的存活率。总体而言，A6-PS-EPI作为一种简单而智能的纳米治疗药物，具有很高的临床翻译潜力。
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