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Trends Biotechnol. 2017 Jul;35(7):653-664. doi: 10.1016/j.tibtech.2017.03.014. Epub 2017 Apr 21.

Applications of pHLIP Technology for Cancer Imaging and Therapy.

Author information

1
Department of Physics, University of Rhode Island, Kingston, RI 02881, USA.
2
Department of Radiology, Memorial Sloan Kettering Cancer Center, 1275 York Avenue, New York, NY 10065, USA; Program in Molecular Pharmacology, Memorial Sloan Kettering Cancer Center, 1275 York Avenue, New York, NY 10065, USA; Weill Cornell Medical College, 1300 York Avenue, New York, NY 10065, USA.
3
Department of Physics, University of Rhode Island, Kingston, RI 02881, USA. Electronic address: reshetnyak@uri.edu.
4
Department of Molecular Biophysics and Biochemistry, Yale University, New Haven, CT 06520, USA. Electronic address: donald.engelman@yale.edu.

Abstract

Acidity is a biomarker of cancer that is not subject to the blunting clonal selection effects that reduce the efficacy of other biomarker technologies, such as antibody targeting. The pH (low) insertion peptides (pHLIP®s) 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.

KEYWORDS:

acidity; drug delivery; imaging; nanotechnology; tumor targeting

PMID:
28438340
PMCID:
PMC5492987
DOI:
10.1016/j.tibtech.2017.03.014
[Indexed for MEDLINE]
Free PMC Article

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