Synthesis and biological evaluation of novel mono- and bivalent ASGP-R-targeted drug-conjugates

Rostislav A. Petrov, Svetlana Yu Maklakova, Yan A. Ivanenkov, Stanislav A. Petrov, Olga V. Sergeeva, Emil Yu Yamansarov, Irina V. Saltykova, Igor I. Kireev, Irina B. Alieva, Ekaterina V. Deyneka, Alina A. Sofronova, Anastasiia V. Aladinskaia, Alexandre V. Trofimenko, Renat S. Yamidanov, Sergey V. Kovalev, Victor E. Kotelianski, Timofey S. Zatsepin, Elena K. Beloglazkina, Alexander G. Majouga

    Research output: Contribution to journalArticlepeer-review

    10 Citations (Scopus)


    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.

    Original languageEnglish
    Pages (from-to)382-387
    Number of pages6
    JournalBioorganic and Medicinal Chemistry Letters
    Issue number3
    Publication statusPublished - 1 Feb 2018


    • ASGP-R
    • Cancer
    • Paclitaxel
    • Targeted drug delivery


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