Synthesis and biological evaluation of novel mono- and bivalent ASGP-R-targeted drug-conjugates
Тип публикации: Journal Article
Дата публикации: 2018-02-01
scimago Q2
wos Q2
БС2
SJR: 0.472
CiteScore: 5.1
Impact factor: 2.2
ISSN: 0960894X, 14643405
PubMed ID:
29269214
Organic Chemistry
Drug Discovery
Biochemistry
Molecular Biology
Pharmaceutical Science
Clinical Biochemistry
Molecular Medicine
Краткое описание
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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Petrov R. A. 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.
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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. 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.
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TY - JOUR
DO - 10.1016/j.bmcl.2017.12.032
UR - https://linkinghub.elsevier.com/retrieve/pii/S0960894X17311927
TI - Synthesis and biological evaluation of novel mono- and bivalent ASGP-R-targeted drug-conjugates
T2 - Bioorganic and Medicinal Chemistry Letters
AU - Maklakova, Svetlana
AU - Ivanenkov, Yan
AU - Petrov, Stanislav B.
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.
PY - 2018
DA - 2018/02/01
PB - Elsevier
SP - 382-387
IS - 3
VL - 28
PMID - 29269214
SN - 0960-894X
SN - 1464-3405
ER -
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@article{2018_Petrov,
author = {Svetlana Maklakova and Yan Ivanenkov and Stanislav B. Petrov 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},
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://linkinghub.elsevier.com/retrieve/pii/S0960894X17311927},
number = {3},
pages = {382--387},
doi = {10.1016/j.bmcl.2017.12.032}
}
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MLA
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Petrov, Rostislav A., et al. “Synthesis and biological evaluation of novel mono- and bivalent ASGP-R-targeted drug-conjugates.” Bioorganic and Medicinal Chemistry Letters, vol. 28, no. 3, Feb. 2018, pp. 382-387. https://linkinghub.elsevier.com/retrieve/pii/S0960894X17311927.