Parallel synthesis and splicing redirection activity of cell-penetrating peptide conjugate libraries of a PNA cargo† †Electronic supplementary information (ESI) available: MALDI mass-spectroscopy data for peptides and PNA705 conjugates of LB1 and LB2. Amino acid sequences, purity, synthesis and conjugation yields of LB2. Examples of HPLC-graphs and MALDI mass-spectra for peptides and conjugates. Luciferase readout of LB1 crude and purified PNA705 conjugates and single data-point splice correction assay of LB2–PNA705 conjugates. See DOI: 10.1039/c3ob41659c Click here for additional data file.

نویسندگان

  • Peter J. Deuss
  • Andrey A. Arzumanov
  • Donna L. Williams
  • Michael J. Gait
چکیده

A novel method for the parallel synthesis of peptide-biocargo conjugates was developed that utilizes affinity purification for fast isolation of the conjugates in order to avoid time consuming HPLC purification. The methodology was applied to create two libraries of cell-penetrating peptide (CPP)-PNA705 conjugates from parallel-synthesized peptide libraries. The conjugates were tested for their ability to induce splicing redirection in HeLa pLuc705 cells. The results demonstrate how the novel methodology can be applied for screening purposes in order to find suitable CPP-biocargo combinations and further optimization of CPPs.

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عنوان ژورنال:

دوره 11  شماره 

صفحات  -

تاریخ انتشار 2013