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Machulkin, Aleksei E.; Nimenko, Ekaterina A.; Zyk, Nikolay U.; Uspenskaia, Anastasiia A.; Smirnova, Galina B.; Khan, Irina I.; Pokrovsky, Vadim S.; Vaneev, Alexander N.; Timoshenko, Roman V.; Mamed-Nabizade, Vugara V.; Zavertkina, Maria V.; Erofeev, Alexander; Gorelkin, Petr; Majouga, Alexander G.; Zyk, Nikolay V.; Khazanova, Elena S.; Beloglazkina, Elena K.

Synthesis and Preclinical Evaluation of Small-Molecule Prostate-Specific Membrane Antigen-Targeted Abiraterone Conjugate

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  • Medientyp: E-Artikel
  • Titel: Synthesis and Preclinical Evaluation of Small-Molecule Prostate-Specific Membrane Antigen-Targeted Abiraterone Conjugate
  • Beteiligte: Machulkin, Aleksei E.; Nimenko, Ekaterina A.; Zyk, Nikolay U.; Uspenskaia, Anastasiia A.; Smirnova, Galina B.; Khan, Irina I.; Pokrovsky, Vadim S.; Vaneev, Alexander N.; Timoshenko, Roman V.; Mamed-Nabizade, Vugara V.; Zavertkina, Maria V.; Erofeev, Alexander; Gorelkin, Petr; Majouga, Alexander G.; Zyk, Nikolay V.; Khazanova, Elena S.; Beloglazkina, Elena K.
  • Erschienen: MDPI AG, 2022
  • Erschienen in: Molecules
  • Sprache: Englisch
  • DOI: 10.3390/molecules27248795
  • ISSN: 1420-3049
  • Schlagwörter: Chemistry (miscellaneous) ; Analytical Chemistry ; Organic Chemistry ; Physical and Theoretical Chemistry ; Molecular Medicine ; Drug Discovery ; Pharmaceutical Science
  • Entstehung:
  • Anmerkungen:
  • Beschreibung: <jats:p>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.</jats:p>
  • Zugangsstatus: Freier Zugang