AI Article Synopsis
- Researchers designed tripodal peptide analogues based on the Src SH2 domain's phosphotyrosine binding pocket to target fluorescein-labeled phosphopeptides.
- LPA4, one of the linear peptide analogues, demonstrated effective binding to fluorescein-labeled GpYEEI and showed potential for cellular delivery.
- Fluorescence microimaging and flow cytometry confirmed that LPA4 can facilitate the uptake of phosphopeptides into cells, indicating its usefulness as a delivery tool.
Article Abstract
Tripodal peptide analogues were designed on the basis of the phosphotyrosine binding pocket of the Src SH2 domain and assayed for their ability to bind to fluorescein-labeled phosphopeptides. Fluorescence polarization assays showed that a number of amphipathic linear peptide analogues (LPAs), such as LPA4, bind to fluorescein-labeled GpYEEI (F-GpYEEI). LPA4 was evaluated for potential application in cellular delivery of phosphopeptides. Fluorescence microimaging cellular uptake studies with fluorescein-attached LPA4 (F-LPA4) alone or with the mixture of LPA4 and F-GpYEEI in BT-20 cells showed dramatic increase of the fluorescence intensity in cytosol of cells, indicating that LPA4 can function as a delivery tool of F-GpYEEI across the cell membrane. Fluorescent flow cytometry studies showed the cellular uptake of F-LPA4 in an energy-independent pathway and confirmed the cellular uptake of F-GpYEEI in the presence of LPA4. These studies suggest that amphipathic tripodal peptide analogues, such as LPA4, can be used for cellular delivery of phosphopeptides.
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| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2539070 | PMC |
| http://dx.doi.org/10.1021/jm070416o | DOI Listing |
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