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 inMedicinal chemistry research Vol. 32; no. 1; pp. 32 - 37
Main Authors Uspenskaya, Anastasiia A., Nimenko, Ekaterina A., Shafikov, Radik R., Zyk, Nikolay Y., Evteev, Sergei A., Dashkova, Natalia S., Ivanenkov, Yan A., Majouga, Alexander G., Skvortsov, Dmitry A., Garanina, Anastasiia S., Beloglazkina, Elena K., Machulkin, Aleksei E.
Format Journal Article
LanguageEnglish
Published New York Springer US 01.01.2023
Springer Nature B.V
Subjects
Antigens
Biochemistry
Biomedical and Life Sciences
Biomedicine
Bioorganic Chemistry
Brief Report
Inorganic Chemistry
Ligands
Medicinal Chemistry
Optimization
Pharmacology/Toxicology
Monomethyl auristatin E
Drug delivery
Sulfo-Cy5 label
Prostate cancer
Prostate-specific membrane antigen
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Summary: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
Bibliography:ObjectType-Article-1
SourceType-Scholarly Journals-1
ObjectType-Feature-2
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ISSN:1054-2523
1554-8120
DOI:10.1007/s00044-022-03002-w