Tuning a Polar Molecule for Selective Cytoplasmic Delivery by a pH (Low) Insertion Peptide
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چکیده
منابع مشابه
Tuning a polar molecule for selective cytoplasmic delivery by a pH (Low) insertion peptide.
Drug molecules are typically hydrophobic and small in order to traverse membranes to reach cytoplasmic targets, but we have discovered that more polar molecules can be delivered across membranes using water-soluble, moderately hydrophobic membrane peptides of the pHLIP (pH low insertion peptide) family. Delivery of polar cargo molecules could expand the chemical landscape for pharmacological ag...
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What are the molecular events that occur when a peptide inserts across a membrane or exits from it? Using the pH-triggered insertion of the pH low insertion peptide to enable kinetic analysis, we show that insertion occurs in several steps, with rapid (0.1 sec) interfacial helix formation, followed by a much slower (100 sec) insertion pathway to give a transmembrane helix. The reverse process o...
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ژورنال
عنوان ژورنال: Biochemistry
سال: 2011
ISSN: 0006-2960,1520-4995
DOI: 10.1021/bi2009773