Bioorganic and Medicinal Chemistry Letters, volume 28, issue 3, pages 382-387

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

Sergeeva Olga 2, 3
Saltykova Irina V 1
Kireev I. 4
Alieva Irina B. 4
Deyneka Ekaterina V. 5
Sofronova Alina A. 6
Aladinskaia Anastasiia V 5
Trofimenko Alexandre V 5
Yamidanov Renat S. 7
Kotelianski Victor E 8
Publication typeJournal Article
Publication date2018-02-01
Quartile SCImago
Q2
Quartile WOS
Q2
Impact factor2.7
ISSN0960894X, 14643405
Organic Chemistry
Drug Discovery
Biochemistry
Molecular Biology
Pharmaceutical Science
Clinical Biochemistry
Molecular Medicine
Abstract
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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GOST Copy
Maklakova S. et al. Synthesis and biological evaluation of novel mono- and bivalent ASGP-R-targeted drug-conjugates // Bioorganic and Medicinal Chemistry Letters. 2018. Vol. 28. No. 3. pp. 382-387.
GOST all authors (up to 50) Copy
Maklakova S., Ivanenkov Y., Petrov S. B., Sergeeva O., Yamansarov E. Yu., Saltykova I. V., Kireev I., Alieva I. B., Deyneka E. V., Sofronova A. A., Aladinskaia A. V., Trofimenko A. V., Yamidanov R. S., Kovalev S., Kotelianski V. E., Zatsepin T. S., Beloglazkina E. K., Majouga A. G. Synthesis and biological evaluation of novel mono- and bivalent ASGP-R-targeted drug-conjugates // Bioorganic and Medicinal Chemistry Letters. 2018. Vol. 28. No. 3. pp. 382-387.
RIS |
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RIS Copy
TY - JOUR
DO - 10.1016/j.bmcl.2017.12.032
UR - https://doi.org/10.1016%2Fj.bmcl.2017.12.032
TI - Synthesis and biological evaluation of novel mono- and bivalent ASGP-R-targeted drug-conjugates
T2 - Bioorganic and Medicinal Chemistry Letters
AU - Petrov, Stanislav B.
AU - Maklakova, Svetlana
AU - Ivanenkov, Yan
AU - Sergeeva, Olga
AU - Yamansarov, Emil Yu
AU - Saltykova, Irina V
AU - Kireev, I.
AU - Alieva, Irina B.
AU - Deyneka, Ekaterina V.
AU - Sofronova, Alina A.
AU - Aladinskaia, Anastasiia V
AU - Trofimenko, Alexandre V
AU - Yamidanov, Renat S.
AU - Kovalev, Sergey
AU - Kotelianski, Victor E
AU - Zatsepin, Timofei S.
AU - Beloglazkina, Elena K.
AU - Majouga, Alexander G.
PY - 2018
DA - 2018/02/01 00:00:00
PB - Elsevier
SP - 382-387
IS - 3
VL - 28
SN - 0960-894X
SN - 1464-3405
ER -
BibTex |
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BibTex Copy
@article{2018_Maklakova,
author = {Stanislav B. Petrov and Svetlana Maklakova and Yan Ivanenkov and Olga Sergeeva and Emil Yu Yamansarov and Irina V Saltykova and I. Kireev and Irina B. Alieva and Ekaterina V. Deyneka and Alina A. Sofronova and Anastasiia V Aladinskaia and Alexandre V Trofimenko and Renat S. Yamidanov and Sergey Kovalev and Victor E Kotelianski and Timofei S. Zatsepin and Elena K. Beloglazkina and Alexander G. Majouga},
title = {Synthesis and biological evaluation of novel mono- and bivalent ASGP-R-targeted drug-conjugates},
journal = {Bioorganic and Medicinal Chemistry Letters},
year = {2018},
volume = {28},
publisher = {Elsevier},
month = {feb},
url = {https://doi.org/10.1016%2Fj.bmcl.2017.12.032},
number = {3},
pages = {382--387},
doi = {10.1016/j.bmcl.2017.12.032}
}
MLA
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MLA Copy
Maklakova, Svetlana, et al. ā€œSynthesis and biological evaluation of novel mono- and bivalent ASGP-R-targeted drug-conjugates.ā€ Bioorganic and Medicinal Chemistry Letters, vol. 28, no. 3, Feb. 2018, pp. 382-387. https://doi.org/10.1016%2Fj.bmcl.2017.12.032.
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