Version 1
: Received: 11 May 2024 / Approved: 13 May 2024 / Online: 13 May 2024 (09:00:28 CEST)
How to cite:
Petrov, S. A.; Grigoriev, G. P.; Orlov, G. А.; Zyk, N. Y.; Grishin, Y. K.; Roznyatovsky, V. A.; Beloglazkina, M. A.; Kuznetsova, J. V.; Machulkin, A. E.; Beloglazkina, E. K. Routes to PSMA/GRPr Targeted Heterobivalent Conjugates: Synthetic Strategies and Their Evaluation. Preprints2024, 2024050810. https://doi.org/10.20944/preprints202405.0810.v1
Petrov, S. A.; Grigoriev, G. P.; Orlov, G. А.; Zyk, N. Y.; Grishin, Y. K.; Roznyatovsky, V. A.; Beloglazkina, M. A.; Kuznetsova, J. V.; Machulkin, A. E.; Beloglazkina, E. K. Routes to PSMA/GRPr Targeted Heterobivalent Conjugates: Synthetic Strategies and Their Evaluation. Preprints 2024, 2024050810. https://doi.org/10.20944/preprints202405.0810.v1
Petrov, S. A.; Grigoriev, G. P.; Orlov, G. А.; Zyk, N. Y.; Grishin, Y. K.; Roznyatovsky, V. A.; Beloglazkina, M. A.; Kuznetsova, J. V.; Machulkin, A. E.; Beloglazkina, E. K. Routes to PSMA/GRPr Targeted Heterobivalent Conjugates: Synthetic Strategies and Their Evaluation. Preprints2024, 2024050810. https://doi.org/10.20944/preprints202405.0810.v1
APA Style
Petrov, S. A., Grigoriev, G. P., Orlov, G. А., Zyk, N. Y., Grishin, Y. K., Roznyatovsky, V. A., Beloglazkina, M. A., Kuznetsova, J. V., Machulkin, A. E., & Beloglazkina, E. K. (2024). Routes to PSMA/GRPr Targeted Heterobivalent Conjugates: Synthetic Strategies and Their Evaluation. Preprints. https://doi.org/10.20944/preprints202405.0810.v1
Chicago/Turabian Style
Petrov, S. A., Aleksei E. Machulkin and Elena K. Beloglazkina. 2024 "Routes to PSMA/GRPr Targeted Heterobivalent Conjugates: Synthetic Strategies and Their Evaluation" Preprints. https://doi.org/10.20944/preprints202405.0810.v1
Abstract
Heterodimeric approach has emerged as a promising method for simultaneously targeting multiple receptors on tumor cells using a single molecule. Simultaneous targeting of the prostate-specific membrane antigen (PSMA) and the gastrin-releasing peptide receptor (GRPr) holds the potential to improve the accuracy of prostate cancer diagnosis. This study aimed to develop and compare six alternative routes for stereoselective synthesis of heterobivalent conjugates designed to deliver the chelating agent DOTA to PSMA/GRPr receptors. The comparison of these alternative synthetic approach, considered such factors as efficiency, complexity, synthesis and purification characteristics, as well as yields of the target compounds has been made. Optimal conditions for the stereoselective synthesis of heterobivalent ligands to PSMA and GRP, which could serve as molecular platforms for the targeted delivery of therapeutic and/or diagnostic agents to these receptors, were determined. For synthesized heterobivalent ligand 26x and heterobivalent conjugate with DOTA 27 complete signal assignment in 1H, 13C, and 15N NMR spectra was achieved using 2D NMR techniques. Based on these data, comprehensive signal assignments were provided for all final compounds in their NMR spectra.
Chemistry and Materials Science, Organic Chemistry
Copyright:
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
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