Synthesis and evaluation of a library of 2,5-bisdiamino-benzoquinone derivatives as probes to modulate protein-protein interactions in prions
| Autor: | Salvatore Bongarzone, Maria Laura Bolognesi, Giuseppe Legname, Hoang Ngoc Ai Tran, Paolo Carloni |
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| Přispěvatelé: | Tran HNA, Bongarzone S, Carloni P, Legname G, Bolognesi ML |
| Jazyk: | angličtina |
| Rok vydání: | 2010 |
| Předmět: |
Prion diseases
Prions Clinical Biochemistry Pharmaceutical Science Phenylalanine Plasma protein binding Biochemistry Cell Line chemistry.chemical_compound Drug Discovery Benzoquinones Molecular Biology Alanine chemistry.chemical_classification Methionine Chemistry Organic Chemistry Tryptophan Proteins Conformational diseases Library design and synthesis Benzoquinone Amino acid Molecular Probes Molecular Medicine Isoleucine Protein Binding |
| Popis: | A small library combining two different benzoquinone cores with seven (L) amino acid methyl esters (alanine, Nomega-nitro-arginine, Nepsilon-BOC-lysine, isoleucine, methionine, phenylalanine and tryptophan) was prepared and tested for prion replication inhibition in ScGT1 cells. The most potent hit, 6a, displayed an EC(50) value of 0.87 microM, which is very close to that of quinacrine (0.4 microM). |
| Databáze: | OpenAIRE |
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