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

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 t...

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Published inCells (Basel, Switzerland) Vol. 10; no. 3; p. 541
Main Authors Dharmaratne, Nayanthara U., Kaplan, Alanna R., Glazer, Peter M.
Format Journal Article
LanguageEnglish
Published Switzerland MDPI AG 04.03.2021
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Abstract 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.
AbstractList 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.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.
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.
Author Dharmaratne, Nayanthara U.
Glazer, Peter M.
Kaplan, Alanna R.
AuthorAffiliation 2 Department of Genetics, Yale University, New Haven, CT 06520, USA
1 Department of Therapeutic Radiology, Yale University, New Haven, CT 06520, USA; peter.glazer@yale.edu
AuthorAffiliation_xml – name: 1 Department of Therapeutic Radiology, Yale University, New Haven, CT 06520, USA; peter.glazer@yale.edu
– name: 2 Department of Genetics, Yale University, New Haven, CT 06520, USA
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  surname: Dharmaratne
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  surname: Kaplan
  fullname: Kaplan, Alanna R.
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  givenname: Peter M.
  orcidid: 0000-0003-4525-5560
  surname: Glazer
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Issue 3
Keywords hypoxia
tumor targeting
acidity
nanoparticles
pHLIP
toxins
imaging
peptide nucleic acids
Language English
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Snippet The delivery of cancer therapeutics can be limited by pharmacological issues such as poor bioavailability and high toxicity to healthy tissue. pH-low insertion...
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SubjectTerms 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
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Title Targeting the Hypoxic and Acidic Tumor Microenvironment with pH-Sensitive Peptides
URI https://www.ncbi.nlm.nih.gov/pubmed/33806273
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Volume 10
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