Open Access
Synthesis and Preclinical Evaluation of Small-Molecule Prostate-Specific Membrane Antigen-Targeted Abiraterone Conjugate
Ekaterina A. Nimenko
1
,
Nikolay U Zyk
1
,
Anastasiia A Uspenskaia
1
,
Galina B. Smirnova
2
,
Irina I Khan
2, 3
,
Vadim S. Pokrovsky
2, 3
,
Alexander N. Vaneev
1, 4
,
Vugara V Mamed Nabizade
4
,
Vugara V. Mamed-Nabizade
4
,
Alexander Erofeev
1, 4
,
Peter Gorelkin
4
,
Alexander G. Majouga
1, 4, 5
,
Nikolay V. Zyk
1
,
Elena S Khazanova
6
,
5
6
LLC Izvarino-Pharma, v. Vnukovskoe, Vnukovskoe sh., 5th km., Building 1, 108817 Moscow, Russia
|
Тип публикации: Journal Article
Дата публикации: 2022-12-12
PubMed ID:
36557929
Organic Chemistry
Drug Discovery
Physical and Theoretical Chemistry
Pharmaceutical Science
Molecular Medicine
Analytical Chemistry
Chemistry (miscellaneous)
Краткое описание
Prostate cancer is the second most common type of cancer among men. The main method of its treatment is androgen deprivation therapy, which has a wide range of side effects. One of the solutions to this challenge is the targeted delivery of drugs to prostate cancer cells. In this study, we performed the synthesis of a novel small-molecule PSMA-targeted conjugate based on abiraterone. Cytotoxicity, the induction of intracellular reactive oxygen species, and P450-cytochrome species inhibition were investigated for this conjugate PSMA-abiraterone. The conjugate demonstrated a preferential effect on prostate tumor cells, remaining inactive at up to 100 µM in human fibroblast cells. In addition, it revealed preferential efficacy, specifically on PSMA-expressing lines with a 65% tumor growth inhibition level on 22Rv1 (PSMA+) xenografts after 14-fold oral administration of PSMA-Abi at a single dose of 500 mg/kg (7.0 g/kg total dose) was observed. This compound showed significantly reduced acute toxicity with comparable efficacy compared to AbiAc.
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Machulkin A. E. et al. Synthesis and Preclinical Evaluation of Small-Molecule Prostate-Specific Membrane Antigen-Targeted Abiraterone Conjugate // Molecules. 2022. Vol. 27. No. 24. p. 8795.
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Machulkin A. E., Nimenko E. A., Zyk N. U., Uspenskaia A. A., Smirnova G. B., Khan I. I., Pokrovsky V. S., Vaneev A. N., Timoshenko R. V., Mamed Nabizade V. V., Mamed-Nabizade V. V., Zavertkina M. V., Erofeev A., Gorelkin P., Majouga A. G., Zyk N. V., Khazanova E. S., Beloglazkina E. K. Synthesis and Preclinical Evaluation of Small-Molecule Prostate-Specific Membrane Antigen-Targeted Abiraterone Conjugate // Molecules. 2022. Vol. 27. No. 24. p. 8795.
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TY - JOUR
DO - 10.3390/molecules27248795
UR - https://www.mdpi.com/1420-3049/27/24/8795
TI - Synthesis and Preclinical Evaluation of Small-Molecule Prostate-Specific Membrane Antigen-Targeted Abiraterone Conjugate
T2 - Molecules
AU - Machulkin, Aleksei E.
AU - Nimenko, Ekaterina A.
AU - Zyk, Nikolay U
AU - Uspenskaia, Anastasiia A
AU - Smirnova, Galina B.
AU - Khan, Irina I
AU - Pokrovsky, Vadim S.
AU - Vaneev, Alexander N.
AU - Timoshenko, Roman V
AU - Mamed Nabizade, Vugara V
AU - Mamed-Nabizade, Vugara V.
AU - Zavertkina, Maria V
AU - Erofeev, Alexander
AU - Gorelkin, Peter
AU - Majouga, Alexander G.
AU - Zyk, Nikolay V.
AU - Khazanova, Elena S
AU - Beloglazkina, Elena K.
PY - 2022
DA - 2022/12/12
PB - MDPI
SP - 8795
IS - 24
VL - 27
PMID - 36557929
SN - 1420-3049
ER -
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@article{2022_Machulkin,
author = {Aleksei E. Machulkin and Ekaterina A. Nimenko and Nikolay U Zyk and Anastasiia A Uspenskaia and Galina B. Smirnova and Irina I Khan and Vadim S. Pokrovsky and Alexander N. Vaneev and Roman V Timoshenko and Vugara V Mamed Nabizade and Vugara V. Mamed-Nabizade and Maria V Zavertkina and Alexander Erofeev and Peter Gorelkin and Alexander G. Majouga and Nikolay V. Zyk and Elena S Khazanova and Elena K. Beloglazkina},
title = {Synthesis and Preclinical Evaluation of Small-Molecule Prostate-Specific Membrane Antigen-Targeted Abiraterone Conjugate},
journal = {Molecules},
year = {2022},
volume = {27},
publisher = {MDPI},
month = {dec},
url = {https://www.mdpi.com/1420-3049/27/24/8795},
number = {24},
pages = {8795},
doi = {10.3390/molecules27248795}
}
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Machulkin, Aleksei E., et al. “Synthesis and Preclinical Evaluation of Small-Molecule Prostate-Specific Membrane Antigen-Targeted Abiraterone Conjugate.” Molecules, vol. 27, no. 24, Dec. 2022, p. 8795. https://www.mdpi.com/1420-3049/27/24/8795.