Details

Autor(en) / Beteiligte

• 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.

Titel

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

Ist Teil von

• Bioorganic & medicinal chemistry letters, 2018-02, Vol.28 (3), p.382-387

Ort / Verlag

England: Elsevier Ltd

Erscheinungsjahr

2018

Quelle

Alma/SFX Local Collection

Beschreibungen/Notizen

• [Display omitted] 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.