GPCR-ligands influence the short oligonucleotide transfection efficacy of the cell-penetrating peptide; Pepfect14
(English)Manuscript (preprint) (Other academic)
Cell-penetrating peptides can be used to deliver oligonucleotide-based cargoes into cells. We have previously shown that inhibition or knock-down of scavenger receptor type A results in a decreased oligonucleotide uptake. The remaining question is if the scavenger receptors are the only cell-surface receptors that can affect the uptake. By utilizing an optimized, higher throughput assay, for short oligonucleotide delivery using cell-penetrating peptides, and simultaneously adding a G-protein coupled receptor-ligand library. We show that two allosteric modulators (MPEP and VU 0357121) of metabotropic glutamate receptor type 5 and one histamine H3 receptor antagonist (Ciproxifan) have effects that can increase the transfection efficacy of PepFect in complex with a short single stranded oligonucleotide. Five different estrogen receptor ligands have negative effects on the transfection efficacy.
Biochemistry and Molecular Biology
Research subject Neurochemistry with Molecular Neurobiology
IdentifiersURN: urn:nbn:se:su:diva-120831OAI: oai:DiVA.org:su-120831DiVA: diva2:854774