title: Studies of anti-fibrillogenic activity of phthalocyanines of zirconium containing out-of-plane ligands.
abstract: Series of phthalocyanines of zirconium containing lysine, citric, nonanoic acid residues and dibenzolylmethane groups as out-of-plane ligands are firstly studied as inhibitors of fibrillogenesis using cyanine-based fluorescent inhibitory assay. It was shown that studied phthalocyanines at concentration of 20μM inhibited aggregation reaction on 38.5-57.6% and inhibitory activity of phthalocyanines depended on the chemical nature of out-of-plane ligand. For the most active compound PcZrLys(2) (zirconium phthalocyanine containing lysine fragment) the efficient inhibitor concentration was estimated to be 37μM. AFM studies have shown that in the presence of PcZrLys(2) the inhibition of fibrils formation and formation of spherical oligomeric aggregates took place. Due to the ability of phthalocyanines to decrease efficiently protein aggregation into the amyloid fibrils, modification of phthalocyanine molecules via out-of-plane substitutions was proposed as approach for design of anti-fibrillogenic agents with required properties.
authors.affiliation: Institute of Molecular Biology and Genetics, National Academy of Sciences of Ukraine, 150 Zabolotnogo St., 03143 Kyiv, Ukraine. v.b.kovalska@imbg.org.ua
authors.forename: Vladyslava
authors.initials: V
authors.lastname: Kovalska
authors.forename: Mykhaylo
authors.initials: M
authors.lastname: Losytskyy
authors.forename: Viktor
authors.initials: V
authors.lastname: Chernii
authors.forename: Kateryna
authors.initials: K
authors.lastname: Volkova
authors.forename: Iryna
authors.initials: I
authors.lastname: Tretyakova
authors.forename: Vsevolod
authors.initials: V
authors.lastname: Cherepanov
authors.forename: Sergiy
authors.initials: S
authors.lastname: Yarmoluk
authors.forename: Sergiy
authors.initials: S
authors.lastname: Volkov
mesh_terms: D000682:Amyloid / Q000037:antagonists & inhibitors* / Q000378:metabolism; D007211:Indoles / Q000737:chemistry*; D054833:Isoindoles; D008024:Ligands; D008239:Lysine / Q000737:chemistry; D018625:Microscopy, Atomic Force; D015040:Zirconium / Q000737:chemistry*
chemical_list: D000682:Amyloid; D007211:Indoles; D054833:Isoindoles; D008024:Ligands; D015040:Zirconium; D008239:Lysine; C013647:phthalocyanine