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

[Display omitted] 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 s...

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Published inMendeleev communications Vol. 30; no. 6; pp. 756 - 759
Main Authors Uspenskaya, Anastasiya A., Machulkin, Alexey E., Nimenko, Ekaterina A., Shafikov, Radik R., Petrov, Stanislav A., Skvortsov, Dmitry A., Beloglazkina, Elena K., Majouga, Alexander G.
Format Journal Article
LanguageEnglish
Published Elsevier B.V 01.11.2020
Subjects
amides
peptide synthesis
prostate cancer
prostate specific membrane antigen
solid-phase synthesis
target drug delivery
target drug delivery
prostate cancer
amides
prostate specific membrane antigen
solid-phase synthesis
peptide synthesis
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Summary:[Display omitted] 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.
ISSN:0959-9436
DOI:10.1016/j.mencom.2020.11.022