National Repository of Grey Literature 6 records found  Search took 0.00 seconds. 
Reaction of prion protein with quinacrine
Zawada, Zbigniew ; Šafařík, Martin ; Šebestík, Jaroslav ; Stibor, Ivan ; Bouř, Petr
Prion protein is supposed to cause Creutzfeld–Jakob disease, which can be treated in cell culture by quinacrine. In this work we study acridinylation reaction of prion protein. We also investigate this reaction theoretically on simple models and calculate activation energies for a large ensemble of acridine derivatives. Found correlation between the reactivity and geometry can enhance the design of the new acridine compounds, particularly for medical purposes.
Synthetic scan of C-domain from prion proteins
Šebestík, Jaroslav ; Zawada, Zbigniew ; Šafařík, Martin ; Hlaváček, Jan
Prions are suspected as culprits of several neuropathogenic diseases. A combination of chemical and recombinant syntheses is a powerful tool for studying prion role in pathogenesis of neurodegenerative diseases. Due to the presence of “difficult” sequences in the prion protein molecule, chemical ligation procedure using peptide thioesters as key building blocks is a method of choice. Therefore, a synthetic scan of peptides constituting the mouse prion protein (MoPrP) C-domain 93-231 was carried out. The synthesis on chlorotritylchloride resin was the most promising for most peptides. Only the octadecapeptide MoPrP195-212 could not be synthesized by automated peptide synthesis even using the β-sheet breaking dipeptides. This difficulty was overcome by manual peptide synthesis with careful monitoring of coupling and Fmoc removal.
Nukleofilní substituce na akridinu - možný viník za interakci akridinu s prionovým proteinem
Šebestík, Jaroslav ; Pavlíček, A. ; Šafařík, Martin ; Holada, K. ; Hlaváček, Jan ; Stibor, I.
Covalent modification of lysine residue side chains in the hydrophobic core of prion protein aggregates could explain the discrepancy between the ability of the acridine drug quinacrine to reduce efficiently the incidence of prion protein in cell culture and its weak prion binding affinity.
Racionální návrh konjugátů bis-akridinu s peptidy vážícími se k dsDNA
Šebestík, Jaroslav ; Hlaváček, Jan ; Stibor, I.
From the prepared library of bis-9-aminoacridine peptide conjugates, one compound exerting two orders of magnitude higher binding constant than that of 9-aminoacridine was identified.
May bis-intercalator-peptides influence prion aggregation?
Šebestík, Jaroslav ; Hlaváček, Jan ; Stibor, I.
The synthesis of peptide libraries functionalized with 9-aminoacridines (Acr-NH2) was described as well as an assay based on precipitation of amyloidogenic dye from buffer solution HV monitoring of positional-scanning combinatorial libraries.

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