Current Medicinal Chemistry, volume 28, issue 2, pages 268-298
The importance of linkers in the structure of PSMA ligands
Publication type: Journal Article
Publication date: 2022-01-01
Journal:
Current Medicinal Chemistry
Quartile SCImago
Q1
Quartile WOS
Q2
Impact factor: 4.1
ISSN: 09298673, 1875533X
Organic Chemistry
Drug Discovery
Biochemistry
Pharmacology
Molecular Medicine
Abstract
:
Abstract: Cancer is one of the leading social problems of the modern world. Today prostate cancer is the second leading cause of cancer deaths among men. Targeted drug delivery is widely used to treat and diagnose prostate cancer. Conjugates selectively binding to prostate-specific membrane antigenbased on urea ligands are being actively developed against this disease. The linker has a significant influence on the biological activity of such conjugates. The linker performs a large number of functions, and its modification is one of the key methods for creating the best pharmacological profile. This review aims to discuss and analyze the main approaches to the method of introduction and synthesis of linkers for this type of conjugates without a description of the influence of biologically active molecules, as well as to establish the key modification methods that have a significant role on the structureactivity relationship. For this purpose, a review of the current scientific literature was performed, both for the conjugates under development and those already undergoing clinical trials. It was found that the optimal structure is a linker containing an aliphatic fragment near the vector-molecule (n(CH2) = 3-6), followed by a polypeptide chain consisting of 2 to 4 amino acid residues. The presence of a Phe-Phe dipeptide chain or the introduction of negatively charged groups also has a positive effect. Ongoing research in this field helps to establish the accurate effect of each linker fragment, and the development of solid-phase synthesis methods makes it much easier to achieve this goal.
Citations by journals
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1
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European Journal of Medicinal Chemistry
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1 publication, 12.5%
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1 publication, 12.5%
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Journal of Physical Chemistry C
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1 publication, 12.5%
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Medicinal Chemistry Research
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1 publication, 12.5%
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Bioconjugate Chemistry
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1 publication, 12.5%
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International Journal of Molecular Sciences
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International Journal of Molecular Sciences
1 publication, 12.5%
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Biochemistry (Moscow)
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Biochemistry (Moscow)
1 publication, 12.5%
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1
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Citations by publishers
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1
2
3
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American Chemical Society (ACS)
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American Chemical Society (ACS)
3 publications, 37.5%
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Elsevier
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Elsevier
1 publication, 12.5%
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Springer Nature
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Springer Nature
1 publication, 12.5%
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Multidisciplinary Digital Publishing Institute (MDPI)
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Multidisciplinary Digital Publishing Institute (MDPI)
1 publication, 12.5%
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Pleiades Publishing
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Pleiades Publishing
1 publication, 12.5%
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1
2
3
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- We do not take into account publications that without a DOI.
- Statistics recalculated only for publications connected to researchers, organizations and labs registered on the platform.
- Statistics recalculated weekly.
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Uspenskaya A. A. et al. The importance of linkers in the structure of PSMA ligands // Current Medicinal Chemistry. 2022. Vol. 28. No. 2. pp. 268-298.
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Uspenskaya A. A., Nimenko E. A., Machulkin A. E., Beloglazkina E. K., Majouga A. G. The importance of linkers in the structure of PSMA ligands // Current Medicinal Chemistry. 2022. Vol. 28. No. 2. pp. 268-298.
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TY - JOUR
DO - 10.2174/0929867328666210804092200
UR - https://doi.org/10.2174%2F0929867328666210804092200
TI - The importance of linkers in the structure of PSMA ligands
T2 - Current Medicinal Chemistry
AU - Uspenskaya, Anastasia A.
AU - Nimenko, Ekaterina A.
AU - Machulkin, Aleksei E.
AU - Beloglazkina, Elena K.
AU - Majouga, Alexander G.
PY - 2022
DA - 2022/01/01 00:00:00
PB - Bentham Science
SP - 268-298
IS - 2
VL - 28
SN - 0929-8673
SN - 1875-533X
ER -
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@article{2022_Uspenskaya,
author = {Anastasia A. Uspenskaya and Ekaterina A. Nimenko and Aleksei E. Machulkin and Elena K. Beloglazkina and Alexander G. Majouga},
title = {The importance of linkers in the structure of PSMA ligands},
journal = {Current Medicinal Chemistry},
year = {2022},
volume = {28},
publisher = {Bentham Science},
month = {jan},
url = {https://doi.org/10.2174%2F0929867328666210804092200},
number = {2},
pages = {268--298},
doi = {10.2174/0929867328666210804092200}
}
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Uspenskaya, Anastasia A., et al. āThe importance of linkers in the structure of PSMA ligands.ā Current Medicinal Chemistry, vol. 28, no. 2, Jan. 2022, pp. 268-298. https://doi.org/10.2174%2F0929867328666210804092200.