학술논문
Synthesis of Prostate-Specific Membrane Antigen-Targeted Bimodal Conjugates of Cytotoxic Agents and Antiandrogens and Their Comparative Assessment with Monoconjugates.
Document Type
Article
Author
Zyk, Nikolai Y.; Garanina, Anastasiia S.; Plotnikova, Ekaterina A.; Ber, Anton P.; Nimenko, Ekaterina A.; Dashkova, Natalia S.; Uspenskaia, Anastasiia A.; Shafikov, Radik R.; Skvortsov, Dmitry A.; Petrov, Stanislav A.; Pankratov, Andrey A.; Zyk, Nikolai V.; Majouga, Alexander G.; Beloglazkina, Elena K.; Machulkin, Aleksei E.
Source
Subject
*ANTIANDROGENS
*PROSTATE cancer
*ANDROGEN receptors
*CHEMICAL synthesis
*CANCER patients
*TUMOR growth
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Language
ISSN
1661-6596
Abstract
Prostate cancer is the second most common cancer among men. We designed and synthesized new ligands targeting prostate-specific membrane antigen and suitable for bimodal conjugates with diagnostic and therapeutic agents. In vitro studies of the affinity of the synthesized compounds to the protein target have been carried out. Based on these ligands, a series of bimodal conjugates with a combination of different mitosis inhibitors and antiandrogenic drugs were synthesized. The cytotoxicity of the compounds obtained in vitro was investigated on three different cell lines. The efficacy of the two obtained conjugates was evaluated in vivo in xenograft models of prostate cancer. These compounds have been shown to be highly effective in inhibiting the growth of PSMA-expressing tumors. [ABSTRACT FROM AUTHOR]