Applications of pHLIP Technology for Cancer Imaging and Therapy.
Applications of pHLIP Technology for Cancer Imaging and Therapy.
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DOI：
10.1016/j.tibtech.2017.03.014
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发表时间：
2017-07
影响因子：
17.3
通讯作者：
Engelman DM
中科院分区：
文献类型：
--
作者：
Wyatt LC;Lewis JS;Andreev OA;Reshetnyak YK;Engelman DM
酸度是癌症的生物标志物，它不受削弱克隆选择效应的影响，这种效应会降低其他生物标志物技术（如抗体靶向）的功效。pH（低）插入肽（pHLIPs）为靶向酸性组织提供了新的机会。通过膜相关折叠的物理机制，酸性微环境触发pHLIP插入并跨越肿瘤细胞膜。pHLIP平台可应用于酸性组织成像，将细胞可渗透和不可渗透的分子递送到细胞质，并促进纳米颗粒的细胞摄取。由于酸中毒是肿瘤发展、进展和侵袭性的标志，因此pHLIP技术可能被证明可用于靶向癌细胞和转移灶，用于肿瘤诊断、成像和治疗。
Acidity is a biomarker of cancer that is not subject to the blunting clonal selection effects that reduce the efficacy of other biomarker technologies, like antibody targeting. The pH (Low) Insertion Peptides (pHLIPs) provide new opportunities for targeting acidic tissues. Through the physical mechanism of membrane-associated folding, pHLIPs are triggered by the acidic microenvironment to insert and span the membranes of tumor cells. The pHLIP platform can be applied to imaging acidic tissues, delivering cell-permeable and impermeable molecules to the cytoplasm, and promoting the cellular uptake of nanoparticles. Since acidosis is a hallmark of tumor development, progression, and aggressiveness, the pHLIP technology may prove useful in targeting cancer cells and metastases for tumor diagnosis, imaging, and therapy.