作者: Marco A Deriu , Michela Cangiotti , Gianvito Grasso , Ginevra Licandro , Afsaneh Lavasanifar
DOI: 10.1021/ACS.LANGMUIR.7B03168
关键词: Polyethylene glycol 、 Pharmacophore 、 Nucleic acid 、 Conjugated system 、 Cytotoxicity 、 TLR7 、 Transmembrane protein 、 Dynamic light scattering 、 Biophysics 、 Chemistry
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...