药学学报, 2018, 53(3): 375-382
引用本文:
贾学丽, 张佳, 赵婷, 杜青, 曹德英, 向柏, 耿革霞, 齐宪荣. 低pH插入肽研究概况[J]. 药学学报, 2018, 53(3): 375-382.
JIA Xue-li, ZHANG Jia, ZHAO Ting, DU Qing, CAO De-ying, XIANG Bai, GENG Ge-xia, QI Xian-rong. Research situation of pH low insertion peptides[J]. Acta Pharmaceutica Sinica, 2018, 53(3): 375-382.

低pH插入肽研究概况
贾学丽1, 张佳1, 赵婷1, 杜青1, 曹德英1, 向柏1, 耿革霞2, 齐宪荣3
1. 河北医科大学药学院, 河北 石家庄 050017;
2. 河北省食品药品审评认证中心, 河北 石家庄 050091;
3. 北京大学药学院, 北京 100191
摘要:
许多疾病状态体内的新陈代谢往往导致细胞外酸化,如癌症、缺血性中风、神经外伤和感染。细胞外微酸环境已成为肿瘤等疾病诊断和治疗的有效靶点。低pH插入肽(pH low insertion peptides,pHLIPs)是一种可以靶向细胞外微酸环境的多肽载体,这种载体可将负载物以低pH依赖方式选择性转运至病变细胞。本文从单分子靶向转运和纳米载体靶向递送两方面,综述了pHLIP介导的靶向形式在疾病诊疗中的应用。
关键词:    低pH插入肽      细胞外微酸环境      诊疗      肿瘤      纳米载体     
Research situation of pH low insertion peptides
JIA Xue-li1, ZHANG Jia1, ZHAO Ting1, DU Qing1, CAO De-ying1, XIANG Bai1, GENG Ge-xia2, QI Xian-rong3
1. School of Pharmacy, Hebei Medical University, Shijiazhuang 050017, China;
2. Hebei Center For Food And Drug Evaluation and Certification, Shijiazhuang 050091, China;
3. School of Pharmaceutical Sciences, Peking University, Beijing 100191, China
Abstract:
Extracellular acidity has been associated with many pathological states, such as cancer, ischemic stroke, neurotrauma and infection, which makes it an effective target for therapy and diagnosis of such diseases. As a polypeptide vector, pH low insertion peptides (pHLIPs) are endowed with high sensitivity to extracellular acidic environment, which can insert the membrane and deliver payload to pathological cells in a pH dependent manner. Here, theranostic applications of pHLIP in disease, are reviewed in two aspects:pHLIP-mediated single-molecule transporter and nano-sized carrier.
Key words:    pH low insertion peptide    extracellular acidic environment    theranostic    tumor    nano-sized carrier   
收稿日期: 2017-08-30
DOI: 10.16438/j.0513-4870.2017-0830
基金项目: 国家自然科学基金资助项目(81773666,81302725);河北省自然科学基金资助项目(H2015206356).
通讯作者: 向柏,Tel/Fax:86-311-86266050,E-mail:baixiang@hebmu.edu.cn;耿革霞,Tel:86-311-67305769,Fax:86-311-67305763,E-mail:genggexia@126.com
Email: baixiang@hebmu.edu.cn;genggexia@126.com
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