Targeting acidity in diseased tissues: mechanism and applications of the membrane-inserting peptide, pHLIP
| Autor: | Donald M. Engelman, Francisco N. Barrera, John C. Deacon |
|---|---|
| Rok vydání: | 2014 |
| Předmět: |
Cell Membrane Permeability
Biophysics Peptide Biology Biochemistry Protein Structure Secondary Article Cell membrane Drug Delivery Systems Neoplasms medicine Animals Humans Molecular Biology chemistry.chemical_classification Cell Membrane Membrane Proteins Hydrogen-Ion Concentration Transmembrane protein Amino acid Cell biology Transmembrane domain Cytosol Membrane medicine.anatomical_structure Membrane protein chemistry |
| Zdroj: | Archives of biochemistry and biophysics. 565 |
| ISSN: | 1096-0384 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|
Full Text from ScienceDirect