Optimization of the dipeptide motifs in the PSMA ligands linker structure: synthesis and in vitro evaluation
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 IC 50 values were obtained. As an example, a conjugate with Sulfo-Cy...
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| Published in | Medicinal chemistry research Vol. 32; no. 1; pp. 32 - 37 |
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| Main Authors | , , , , , , , , , , , |
| Format | Journal Article |
| Language | English |
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New York
Springer US
01.01.2023
Springer Nature B.V |
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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 IC
50
values were obtained. As an example, a conjugate with Sulfo-Cy5 and MMAE was obtained and pre-studied.
Graphical Abstract |
|---|---|
| AbstractList | 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 IC
50
values were obtained. As an example, a conjugate with Sulfo-Cy5 and MMAE was obtained and pre-studied.
Graphical 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. |
| Author | Machulkin, Aleksei E. Uspenskaya, Anastasiia A. Skvortsov, Dmitry A. Zyk, Nikolay Y. Beloglazkina, Elena K. Evteev, Sergei A. Majouga, Alexander G. Nimenko, Ekaterina A. Ivanenkov, Yan A. Garanina, Anastasiia S. Shafikov, Radik R. Dashkova, Natalia S. |
| Author_xml | – sequence: 1 givenname: Anastasiia A. orcidid: 0000-0002-2451-8336 surname: Uspenskaya fullname: Uspenskaya, Anastasiia A. email: uspenskaya.n@gmail.com organization: Chemistry Department, Lomonosov Moscow State University – sequence: 2 givenname: Ekaterina A. surname: Nimenko fullname: Nimenko, Ekaterina A. organization: Chemistry Department, Lomonosov Moscow State University – sequence: 3 givenname: Radik R. surname: Shafikov fullname: Shafikov, Radik R. organization: Chemistry Department, Lomonosov Moscow State University, Shemyakin and Ovchinnikov Institute of Bioorganic Chemistry Russian Academy of Sciences – sequence: 4 givenname: Nikolay Y. surname: Zyk fullname: Zyk, Nikolay Y. organization: Chemistry Department, Lomonosov Moscow State University – sequence: 5 givenname: Sergei A. surname: Evteev fullname: Evteev, Sergei A. organization: The Federal State Unitary Enterprise Dukhov Automatics Research Institute – sequence: 6 givenname: Natalia S. surname: Dashkova fullname: Dashkova, Natalia S. organization: Chemistry Department, Lomonosov Moscow State University – sequence: 7 givenname: Yan A. surname: Ivanenkov fullname: Ivanenkov, Yan A. organization: Chemistry Department, Lomonosov Moscow State University, The Federal State Unitary Enterprise Dukhov Automatics Research Institute, National University of Science and Technology «MISiS», Institute of Biochemistry and Genetics Ufa Science Centre Russian Academy of Sciences (IBG RAS) – sequence: 8 givenname: Alexander G. surname: Majouga fullname: Majouga, Alexander G. organization: Chemistry Department, Lomonosov Moscow State University, National University of Science and Technology «MISiS», Dmitry Mendeleev University of Chemical Technology of Russia – sequence: 9 givenname: Dmitry A. surname: Skvortsov fullname: Skvortsov, Dmitry A. organization: Chemistry Department, Lomonosov Moscow State University – sequence: 10 givenname: Anastasiia S. surname: Garanina fullname: Garanina, Anastasiia S. organization: National University of Science and Technology «MISiS» – sequence: 11 givenname: Elena K. surname: Beloglazkina fullname: Beloglazkina, Elena K. organization: Chemistry Department, Lomonosov Moscow State University – sequence: 12 givenname: Aleksei E. surname: Machulkin fullname: Machulkin, Aleksei E. organization: Chemistry Department, Lomonosov Moscow State University |
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| Cites_doi | 10.1021/acs.jmedchem.1c01157 10.2174/0929867328666210804092200 10.1016/j.bmc.2018.11.022 10.1021/acs.jmedchem.0c01935 10.7150/thno.18719 10.1158/1078-0432.CCR-18-0803 10.1016/j.bmcl.2019.06.035 10.14309/ctg.0000000000000041 10.1093/annonc/mdx370 10.2967/jnumed.116.178533 10.1039/c0md00273a 10.1016/j.bioorg.2019.103154 10.3390/molecules25245784 10.1038/s41598-021-86551-1 10.3322/caac.21660 10.1158/1078-0432.CCR-14-0891 10.2967/jnumed.115.158550 10.1056/nejmoa2107322 10.1021/cr100048w |
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| Keywords | Monomethyl auristatin E Drug delivery Sulfo-Cy5 label Prostate cancer Prostate-specific membrane antigen |
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| Title | Optimization of the dipeptide motifs in the PSMA ligands linker structure: synthesis and in vitro evaluation |
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