私密直播全婐app免费大渔直播,国产av成人无码免费视频,男女同房做爰全过程高潮,国产精品自产拍在线观看

當(dāng)前位置:群英聚首 > 論文著作 > 正文
Taming the wildness of “Trojan-Horse” peptides by charge-guided masking and protease-triggered de-masking for the controlled delivery of anti-tumor agents
來源:時念秋教授個人網(wǎng)站 發(fā)布日期:2017-04-14
作者:Shi NQ, Qi XR
關(guān)鍵字:“Trojan-Horse” peptides, taming the wildness, charge-guided masking, protease-triggered demasking, controlled delivery
論文來源:期刊
具體來源:ACS Appl Mater Interfaces. 2017. Mar 29;9(12):10519-10529. (SCI, IF=7.145)
發(fā)表時間:2017年

Cell-penetrating peptide (CPP), also called “Trojan Horse” peptide, has become a successful approach to deliver various payloads into cells for achieving the intracellular access. However, the "Trojan Horse" peptide is too wild, not just to "Troy", but rather widely distributed in the body. Thus, there is an urgent need to tame the wildness of “Trojan Horse” peptide for targeted delivery of antineoplastic agents to the tumor site. To achieve this goal, we exploit a masked CPP-doxorubicin conjugate platform for targeted delivery of chemotherapeutic drugs using charge-guided masking and protease-triggered de-masking strategies. In this platform, the cell-penetrating function of the positively CPP (D-form

nonaarginine) is abrogated by a negatively shielding peptide (masked CPP), and between them is a cleavable substrate peptide by the protease (MMP-2/9). Protease-triggered

de-masking would occur when the masked CPP reached the MMP-2/9-riched tumor. The

CPP-doxorubicin conjugate (CPP-Dox) and the masked CPP-Dox conjugate (mCPP-Dox)

were used as models for the evaluation of masking and de-masking processes. It was found that exogenous MMP-2/9 could effectively trigger the reversion of CPP-cargo in this conjugate and this trigger adhered to Michaelis-Menten kinetics profile. This conjugate was sensitive to the trigger of endogenous MMP-2/9 and could induce enhanced cytotoxicity towards MMP-2/9-rich tumor cells. In vivo antitumor efficacy revealed that this masked conjugate had considerable antitumor activity and could inhibit the tumor growth at a higher level relative to CPP-cargo. Low toxicity in vivo showed the noticeably decreased

wildness of this conjugate towards normal tissues and more controllable entry of anti-tumor agents into “Troy”. Based on analyses in vitro and in vivo, this mCPP-cargo conjugate

delivery system held an improved selectivity towards MMP-2/9-rich tumors and would

be a promising strategy for tumor-targeted treatment.

Copyright © 2005 Polymer.cn All rights reserved
中國聚合物網(wǎng) 版權(quán)所有
經(jīng)營性網(wǎng)站備案信息

京公網(wǎng)安備11010502032929號

工商備案公示信息

京ICP證050801號

京ICP備12003651號

主站蜘蛛池模板: 德安县| 库尔勒市| 昌都县| 岑溪市| 电白县| 乌兰县| 龙里县| 墨脱县| 喜德县| 靖边县| 抚顺市| 灌云县| 榕江县| 科尔| 上饶市| 毕节市| 札达县| 仁化县| 扎囊县| 那坡县| 红桥区| 曲周县| 西林县| 元氏县| 牡丹江市| 舒兰市| 工布江达县| 安陆市| 湖北省| 库伦旗| 昆明市| 资中县| 依安县| 大关县| 周至县| 普陀区| 阳江市| 临城县| 齐河县| 碌曲县| 巨鹿县|