Self-Assembled Ligands Targeting TLR7: A Molecular Level Investigation.

作者: Marco A Deriu , Michela Cangiotti , Gianvito Grasso , Ginevra Licandro , Afsaneh Lavasanifar

DOI: 10.1021/ACS.LANGMUIR.7B03168

关键词: Polyethylene glycolPharmacophoreNucleic acidConjugated systemCytotoxicityTLR7Transmembrane proteinDynamic light scatteringBiophysicsChemistry

摘要: Toll-like receptors (TLRs) are pattern recognition transmembrane proteins that play an important role in innate immunity. In particular, TLR7 plays a detecting nucleic acids derived from viruses and bacteria. The huge number of pathologies which is involved has led to increasing interest developing new compounds targeting this protein. Several conjugation strategies were proposed for agonists increase the potency while maintaining low toxicity. work, we focus attention on two promising classes same pharmacophore conjugated with phospholipid polyethylene glycol (PEG). A multidisciplinary investigation been carried out by molecular dynamics (MD), dynamic light scattering (DLS), electron paramagnetic resonance (EPR), cytotoxicity assessment. DLS MD indicated how only provides compound abilities self-assemble orderly fashion maximal exposition sol...

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