Targeting acidity in diseased tissues: mechanism and applications of the membrane-inserting peptide, pHLIP.
Targeting acidity in diseased tissues: mechanism and applications of the membrane-inserting peptide, pHLIP.
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DOI：
10.1016/j.abb.2014.11.002
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发表时间：
2015-01-01
影响因子：
3.9
通讯作者：
Barrera, Francisco N.
中科院分区：
文献类型：
--
作者：
Deacon, John C.;Engelman, Donald M.;Barrera, Francisco N.
pHLIP是一个可溶性的~36个氨基酸的肽家族，其结合到膜表面。如果环境是酸性的，则pHLIP折叠并插入跨膜以形成稳定的跨膜螺旋，从而优先将其自身定位在酸性组织中。由于肿瘤和其他疾病组织是酸性的，pHLIPs的低pH靶向行为导致作为诊断和手术成像剂的载体的应用。膜插入的能量也可用于促进适度极性的、通常细胞不可渗透的货物穿过细胞膜插入靶细胞的胞质溶胶中，导致在治疗分子的肿瘤靶向递送中的应用。我们回顾了pHLIPs独特性质的生物化学和生物物理基础，诊断和治疗应用，以及翻译应用正在开发的原则。
pHLIPs are a family of soluble ~36 amino acid peptides, which bind to membrane surfaces. If the environment is acidic, a pHLIP folds and inserts across the membrane to form a stable transmembrane helix, thus preferentially locating itself in acidic tissues. Since tumors and other disease tissues are acidic, pHLIPs’ low-pH targeting behavior leads to applications as carriers for diagnostic and surgical imaging agents. The energy of membrane insertion can also be used to promote the insertion of modestly polar, normally cell-impermeable cargos across the cell membrane into the cytosol of targeted cells, leading to applications in tumor-targeted delivery of therapeutic molecules. We review the biochemical and biophysical basis of pHLIPs’ unique properties, diagnostic and therapeutic applications, and the principles upon which translational applications are being developed.
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影响因子：
5.6
作者：
Barrera, Francisco N.;Weerakkody, Dhammika;Engelman, Donald M.
通讯作者：
Engelman, Donald M.
影响因子：
3.8
作者：
Brown, Mia C.;Yakubu, Rauta A.;Cooley, Jason W.
通讯作者：
Cooley, Jason W.
影响因子：
6.8
作者：
Booth, Paula J.
通讯作者：
Booth, Paula J.
影响因子：
2.9
作者：
Fendos, Justin;Barrera, Francisco N.;Engelman, Donald M.
通讯作者：
Engelman, Donald M.
肿瘤微环境产生的酸度驱动局部侵袭。
影响因子：
11.2
作者：
Estrella V;Chen T;Lloyd M;Wojtkowiak J;Cornnell HH;Ibrahim-Hashim A;Bailey K;Balagurunathan Y;Rothberg JM;Sloane BF;Johnson J;Gatenby RA;Gillies RJ
通讯作者：
Gillies RJ