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Influence of the dipeptide linker configuration on the activity of PSMA ligands

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Uspenskaia A. A. et al. Influence of the dipeptide linker configuration on the activity of PSMA ligands // Mendeleev Communications. 2020. Vol. 30. No. 6. pp. 756-759.
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Uspenskaia A. A., Machulkin A. È., Nimenko E. A., Shafikov R. R., Petrov S. A., Skvortsov D. A., Beloglazkina E. K., Majouga A. G. Influence of the dipeptide linker configuration on the activity of PSMA ligands // Mendeleev Communications. 2020. Vol. 30. No. 6. pp. 756-759.
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TY - JOUR
DO - 10.1016/j.mencom.2020.11.022
UR - https://mendcomm.colab.ws/publications/10.1016/j.mencom.2020.11.022
TI - Influence of the dipeptide linker configuration on the activity of PSMA ligands
T2 - Mendeleev Communications
AU - Uspenskaia, Anastasiia Alekseevna
AU - Machulkin, Aleksei Èduardovich
AU - Nimenko, Ekaterina Alekseevna
AU - Shafikov, Radik R
AU - Petrov, Stanislav Alexandrovich
AU - Skvortsov, Dmitry Aleksandrovich
AU - Beloglazkina, Elena Kimovna
AU - Majouga, Alexander Georgievich
PY - 2020
DA - 2020/11/03
PB - Mendeleev Communications
SP - 756-759
IS - 6
VL - 30
ER -
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@article{2020_Uspenskaia,
author = {Anastasiia Alekseevna Uspenskaia and Aleksei Èduardovich Machulkin and Ekaterina Alekseevna Nimenko and Radik R Shafikov and Stanislav Alexandrovich Petrov and Dmitry Aleksandrovich Skvortsov and Elena Kimovna Beloglazkina and Alexander Georgievich Majouga},
title = {Influence of the dipeptide linker configuration on the activity of PSMA ligands},
journal = {Mendeleev Communications},
year = {2020},
volume = {30},
publisher = {Mendeleev Communications},
month = {Nov},
url = {https://mendcomm.colab.ws/publications/10.1016/j.mencom.2020.11.022},
number = {6},
pages = {756--759},
doi = {10.1016/j.mencom.2020.11.022}
}
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Uspenskaia, Anastasiia Alekseevna, et al. “Influence of the dipeptide linker configuration on the activity of PSMA ligands.” Mendeleev Communications, vol. 30, no. 6, Nov. 2020, pp. 756-759. https://mendcomm.colab.ws/publications/10.1016/j.mencom.2020.11.022.

Keywords

amides
peptide synthesis
prostate cancer
prostate specific membrane antigen
solid-phase synthesis
target drug delivery

Abstract

Selective ligands of an urea-based prostate specific membrane antigen with a phenylalanine/tyrosine-based dipeptide linker and with a mingled chiral centers configuration and/or substituted aromatic fragments were prepared in seven steps by liquid- and in six steps by solid-phase synthesis. In vitro test for inhibiting the cleavage of N-acetylaspartylglutamate revealed the optimum linker containing l-phenylalanine in the structure on the N-terminus of a dipeptide chain.

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