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Optimization of the dipeptide motifs in the PSMA ligands linker structure: synthesis and in vitro evaluation

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Abstract

An improved series of ligands targeting prostatic specific membrane antigen has been reported. Varying compounds and their biological parameters were due to changes in the linker structure. Highly selective compounds with nanomolar IC50 values were obtained. As an example, a conjugate with Sulfo-Cy5 and MMAE was obtained and pre-studied.

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Acknowledgements

The research was carried out with the financial support of Russian Science Foundation Grant No. 22-15-00098 (PSMA ligands design, synthesis and physico-chemical characterization) and Russian Foundation for Basic Research, Grant No. 20-34-90150 (inhibition of the N-acetylaspartylglutamate cleavage).

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Author notes

  1. These authors contributed equally: Anastasiia A. Uspenskaya, Ekaterina A. Nimenko, Radik R. Shafikov

Authors and Affiliations

  1. Chemistry Department, Lomonosov Moscow State University, Leninskie Gory, Building 1/3, GSP-1, Moscow, 119991, Russian Federation

    Anastasiia A. Uspenskaya, Ekaterina A. Nimenko, Radik R. Shafikov, Nikolay Y. Zyk, Natalia S. Dashkova, Yan A. Ivanenkov, Alexander G. Majouga, Dmitry A. Skvortsov, Elena K. Beloglazkina & Aleksei E. Machulkin

  2. Shemyakin and Ovchinnikov Institute of Bioorganic Chemistry Russian Academy of Sciences, GSP-7, Ulitsa Miklukho-Maklaya, 16/10, Moscow, 117997, Russian Federation

    Radik R. Shafikov

  3. The Federal State Unitary Enterprise Dukhov Automatics Research Institute, St. Sushchevskaya, 22, Moscow, 127055, Russian Federation

    Sergei A. Evteev & Yan A. Ivanenkov

  4. National University of Science and Technology «MISiS», Leninskiy Prospekt, 4, Moscow, 119049, Russian Federation

    Yan A. Ivanenkov, Alexander G. Majouga & Anastasiia S. Garanina

  5. Institute of Biochemistry and Genetics Ufa Science Centre Russian Academy of Sciences (IBG RAS), Oktyabrya Prospekt 71, Ufa, 450054, Russian Federation

    Yan A. Ivanenkov

  6. Dmitry Mendeleev University of Chemical Technology of Russia, Miusskaya Sq. 9, Moscow, 125047, Russian Federation

    Alexander G. Majouga

Authors
  1. Anastasiia A. Uspenskaya
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  2. Ekaterina A. Nimenko
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  3. Radik R. Shafikov
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  4. Nikolay Y. Zyk
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  5. Sergei A. Evteev
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  6. Natalia S. Dashkova
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  7. Yan A. Ivanenkov
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  8. Alexander G. Majouga
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  9. Dmitry A. Skvortsov
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  10. Anastasiia S. Garanina
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  11. Elena K. Beloglazkina
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  12. Aleksei E. Machulkin
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Correspondence to Anastasiia A. Uspenskaya.

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Uspenskaya, A.A., Nimenko, E.A., Shafikov, R.R. et al. Optimization of the dipeptide motifs in the PSMA ligands linker structure: synthesis and in vitro evaluation. Med Chem Res 32, 32–37 (2023). https://doi.org/10.1007/s00044-022-03002-w

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  • DOI: https://doi.org/10.1007/s00044-022-03002-w

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