New ASGPR-targeted ligands based on glycoconjugated natural triterpenoids


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New ligands for targeted delivery to the liver based on glycoconjugated natural triterpenoids are proposed. Simple chemical transformations of starting lupane triterpenes led to betulin or betulinic acid conjugates with N-acetyl-d-galactosamine linked through an isopropenyl fragment of the terpene skeleton. The obtained compounds were non-toxic in vitro to a series of cancer cell lines and normal cells. Molecular docking in silico and surface plasmon resonance spectroscopy revealed a high specificity of the synthesized glycotriterpenoids to the asialogly-coprotein receptor of hepatocytes.

作者简介

E. Yamansarov

Lomonosov Moscow State University

编辑信件的主要联系方式.
Email: jamansar@gmail.com
俄罗斯联邦, 1 Leninskie Gory, Moscow, 119991

D. Skvortsov

Lomonosov Moscow State University

Email: jamansar@gmail.com
俄罗斯联邦, 1 Leninskie Gory, Moscow, 119991

A. Lopukhov

Lomonosov Moscow State University

Email: jamansar@gmail.com
俄罗斯联邦, 1 Leninskie Gory, Moscow, 119991

S. Kovalev

Lomonosov Moscow State University

Email: jamansar@gmail.com
俄罗斯联邦, 1 Leninskie Gory, Moscow, 119991

S. Evteev

Lomonosov Moscow State University

Email: jamansar@gmail.com
俄罗斯联邦, 1 Leninskie Gory, Moscow, 119991

R. Petrov

Lomonosov Moscow State University

Email: jamansar@gmail.com
俄罗斯联邦, 1 Leninskie Gory, Moscow, 119991

N. Klyachko

Lomonosov Moscow State University; Skolkovo Institute of Science and Technology

Email: jamansar@gmail.com
俄罗斯联邦, 1 Leninskie Gory, Moscow, 119991; 100 ul. Novaya, Skolkovo, 143025

N. Zyk

Lomonosov Moscow State University

Email: jamansar@gmail.com
俄罗斯联邦, 1 Leninskie Gory, Moscow, 119991

E. Beloglazkina

Lomonosov Moscow State University

Email: jamansar@gmail.com
俄罗斯联邦, 1 Leninskie Gory, Moscow, 119991

Ya. Ivanenkov

Institute of Biochemistry and Genetics, Ufa Scientific Center of the Russian Academy of Sciences; Moscow Institute of Physics and Technology (State University)

Email: jamansar@gmail.com
俄罗斯联邦, 71 prosp. Oktyabrya, Ufa, 450054; 9 Instituskiiper., Dolgoprudnyi, Moscow region, 141701

A. Majouga

Lomonosov Moscow State University; National University of Science and Technology MISiS; Dmitry Mendeleev University of Chemical Technology of Russia

Email: jamansar@gmail.com
俄罗斯联邦, 1 Leninskie Gory, Moscow, 119991; 4 Leninskiiprosp., Moscow, 119049; 1 Build., 9 Miusskaya pl., Moscow, 125047

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