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Synthesis and biological evaluation of novel mono- and bivalent ASGP-R-targeted drug-conjugates.
Petrov, Rostislav A; Maklakova, Svetlana Yu; Ivanenkov, Yan A; Petrov, Stanislav A; Sergeeva, Olga V; Yamansarov, Emil Yu; Saltykova, Irina V; Kireev, Igor I; Alieva, Irina B; Deyneka, Ekaterina V; Sofronova, Alina A; Aladinskaia, Anastasiia V; Trofimenko, Alexandre V; Yamidanov, Renat S; Kovalev, Sergey V; Kotelianski, Victor E; Zatsepin, Timofey S; Beloglazkina, Elena K; Majouga, Alexander G.
Afiliação
  • Petrov RA; Lomonosov Moscow State University, Chemistry Dept, Leninskie Gory, Building 1/3, GSP-1, Moscow 119991, Russian Federation.
  • Maklakova SY; Lomonosov Moscow State University, Chemistry Dept, Leninskie Gory, Building 1/3, GSP-1, Moscow 119991, Russian Federation.
  • Ivanenkov YA; Lomonosov Moscow State University, Chemistry Dept, Leninskie Gory, Building 1/3, GSP-1, Moscow 119991, Russian Federation; Moscow Institute of Physics and Technology (State University), 9 Institutskiy Lane, Dolgoprudny City, Moscow Region 141700, Russian Federation; National University of Science an
  • Petrov SA; Lomonosov Moscow State University, Chemistry Dept, Leninskie Gory, Building 1/3, GSP-1, Moscow 119991, Russian Federation.
  • Sergeeva OV; Lomonosov Moscow State University, Chemistry Dept, Leninskie Gory, Building 1/3, GSP-1, Moscow 119991, Russian Federation; Skolkovo Institute of Science and Technology, 100 Novaya St., 143025 Skolkovo, Russian Federation.
  • Yamansarov EY; Lomonosov Moscow State University, Chemistry Dept, Leninskie Gory, Building 1/3, GSP-1, Moscow 119991, Russian Federation.
  • Saltykova IV; Lomonosov Moscow State University, Chemistry Dept, Leninskie Gory, Building 1/3, GSP-1, Moscow 119991, Russian Federation.
  • Kireev II; Lomonosov Moscow State University, A.N. Belozersky Institute of Physico-Chemical Biology, Leninskye Gory, House 1, Building 40, Moscow 119992, Russian Federation.
  • Alieva IB; Lomonosov Moscow State University, A.N. Belozersky Institute of Physico-Chemical Biology, Leninskye Gory, House 1, Building 40, Moscow 119992, Russian Federation.
  • Deyneka EV; Moscow Institute of Physics and Technology (State University), 9 Institutskiy Lane, Dolgoprudny City, Moscow Region 141700, Russian Federation.
  • Sofronova AA; Lomonosov Moscow State University, Faculty of Bioengineering and Bioinformatics, Moscow, Russia.
  • Aladinskaia AV; Moscow Institute of Physics and Technology (State University), 9 Institutskiy Lane, Dolgoprudny City, Moscow Region 141700, Russian Federation.
  • Trofimenko AV; Moscow Institute of Physics and Technology (State University), 9 Institutskiy Lane, Dolgoprudny City, Moscow Region 141700, Russian Federation.
  • Yamidanov RS; Institute of Biochemistry and Genetics Ufa Science Centre Russian Academy of Sciences (IBG RAS), Prosp. Oktybrya 71, Ufa, Bashkortostan 450054, Russian Federation.
  • Kovalev SV; Lomonosov Moscow State University, Chemistry Dept, Leninskie Gory, Building 1/3, GSP-1, Moscow 119991, Russian Federation.
  • Kotelianski VE; Skolkovo Institute of Science and Technology, 100 Novaya St., 143025 Skolkovo, Russian Federation.
  • Zatsepin TS; Lomonosov Moscow State University, Chemistry Dept, Leninskie Gory, Building 1/3, GSP-1, Moscow 119991, Russian Federation; Skolkovo Institute of Science and Technology, 100 Novaya St., 143025 Skolkovo, Russian Federation.
  • Beloglazkina EK; Lomonosov Moscow State University, Chemistry Dept, Leninskie Gory, Building 1/3, GSP-1, Moscow 119991, Russian Federation.
  • Majouga AG; Lomonosov Moscow State University, Chemistry Dept, Leninskie Gory, Building 1/3, GSP-1, Moscow 119991, Russian Federation; National University of Science and Technology MISiS, 9 Leninskiy pr, Moscow 119049, Russian Federation; Dmitry Mendeleev University of Chemical Technology of Russia, Miusskaya S
Bioorg Med Chem Lett ; 28(3): 382-387, 2018 02 01.
Article em En | MEDLINE | ID: mdl-29269214
Asialoglycoprotein receptor (ASGP-R) is a promising biological target for drug delivery into hepatoma cells. Nevertheless, there are only few examples of small-molecule conjugates of ASGP-R selective ligand equipped by a therapeutic agent for the treatment of hepatocellular carcinoma (HCC). In the present work, we describe a convenient and versatile synthetic approach to novel mono- and multivalent drug-conjugates containing N-acetyl-2-deoxy-2-aminogalactopyranose and anticancer drug - paclitaxel (PTX). Several molecules have demonstrated high affinity towards ASGP-R and good stability under physiological conditions, significant in vitro anticancer activity comparable to PTX, as well as good internalization via ASGP-R-mediated endocytosis. Therefore, the conjugates with the highest potency can be regarded as a promising therapeutic option against HCC.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Paclitaxel / Carcinoma Hepatocelular / Receptor de Asialoglicoproteína / Bibliotecas de Moléculas Pequenas / Galactose / Neoplasias Hepáticas / Antineoplásicos Fitogênicos Limite: Humans Idioma: En Revista: Bioorg Med Chem Lett Ano de publicação: 2018 Tipo de documento: Article
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Paclitaxel / Carcinoma Hepatocelular / Receptor de Asialoglicoproteína / Bibliotecas de Moléculas Pequenas / Galactose / Neoplasias Hepáticas / Antineoplásicos Fitogênicos Limite: Humans Idioma: En Revista: Bioorg Med Chem Lett Ano de publicação: 2018 Tipo de documento: Article