Targeting the Hypoxic and Acidic Tumor Microenvironment with pH-Sensitive Peptides

• Published in: Cells (Basel, Switzerland) Vol. 10; no. 3; p. 541
• Main Authors: Dharmaratne, Nayanthara U., Kaplan, Alanna R., Glazer, Peter M.
• Format: Journal Article
• Language: English
• Published: Switzerland MDPI AG 04.03.2021; MDPI
• Subjects: Acidity; Amino acids; Antigens; Bioavailability; Brain cancer; Cancer therapies; Chemical bonds; Drug dosages; Fluorescent indicators; Humans; Hydrogen-Ion Concentration; Hypoxia; Melanoma; Membranes; Metastasis; Nanoparticles; Nanoparticles - metabolism; peptide nucleic acids; Peptides; Peptides - metabolism; pH effects; pHLIP; Polyethylene glycol; Review; Toxicity; toxins; Tumor Microenvironment; tumor targeting; Tumors; hypoxia; tumor targeting; acidity; nanoparticles; pHLIP; toxins; imaging; peptide nucleic acids
• ISSN: 2073-4409; 2073-4409
• DOI: 10.3390/cells10030541

The delivery of cancer therapeutics can be limited by pharmacological issues such as poor bioavailability and high toxicity to healthy tissue. pH-low insertion peptides (pHLIPs) represent a promising tool to overcome these limitations. pHLIPs allow for the selective delivery of agents to tumors on the basis of pH, taking advantage of the acidity of the hypoxic tumor microenvironment. This review article highlights the various applications in which pHLIPs have been utilized for targeting and treating diseases in hypoxic environments, including delivery of small molecule inhibitors, toxins, nucleic acid analogs, fluorescent dyes, and nanoparticles.