New ASGPR-targeted ligands based on glycoconjugated natural triterpenoids


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Аннотация

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.

Авторлар туралы

E. Yamansarov

Lomonosov Moscow State University

Хат алмасуға жауапты Автор.
Email: jamansar@gmail.com
Ресей, 1 Leninskie Gory, Moscow, 119991

D. Skvortsov

Lomonosov Moscow State University

Email: jamansar@gmail.com
Ресей, 1 Leninskie Gory, Moscow, 119991

A. Lopukhov

Lomonosov Moscow State University

Email: jamansar@gmail.com
Ресей, 1 Leninskie Gory, Moscow, 119991

S. Kovalev

Lomonosov Moscow State University

Email: jamansar@gmail.com
Ресей, 1 Leninskie Gory, Moscow, 119991

S. Evteev

Lomonosov Moscow State University

Email: jamansar@gmail.com
Ресей, 1 Leninskie Gory, Moscow, 119991

R. Petrov

Lomonosov Moscow State University

Email: jamansar@gmail.com
Ресей, 1 Leninskie Gory, Moscow, 119991

N. Klyachko

Lomonosov Moscow State University; Skolkovo Institute of Science and Technology

Email: jamansar@gmail.com
Ресей, 1 Leninskie Gory, Moscow, 119991; 100 ul. Novaya, Skolkovo, 143025

N. Zyk

Lomonosov Moscow State University

Email: jamansar@gmail.com
Ресей, 1 Leninskie Gory, Moscow, 119991

E. Beloglazkina

Lomonosov Moscow State University

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

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