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(S)-3-(Carboxyformamido)-2-(3-(carboxymethyl)ureido)propanoic Acid as A Novel PSMA Targeting Scaffold for Prostate Cancer Imaging.

08:00 EDT 24th March 2020 | BioPortfolio

Summary of "(S)-3-(Carboxyformamido)-2-(3-(carboxymethyl)ureido)propanoic Acid as A Novel PSMA Targeting Scaffold for Prostate Cancer Imaging."

In an effort to seek novel agents targeting prostate-specific membrane antigen (PSMA), sixteen ligands (L1-L16) with structural modifications in S1' binding pocket were synthesized and evaluated for PSMA inhibition. (S)-3-(Carboxyformamido)-2-(3-(carboxymethyl)ureido) propanoic acids proved potent PSMA ligands with Ki values ranging from 0.08 nM - 8.98 nM, which are in the range of or are higher in potency compared to previously published Glu-Urea-based ligands. Computational docking was performed to study the binding mode of the two most potent ligands discovered. FITC-conjugated L14 could selectively stain PSMA+ LNCaP cells over PSMA- PC3 cells. IRDye800CW conjugated L16 can effectively image tumors in a murine xenograft model of prostate cancer.

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This article was published in the following journal.

Name: Journal of medicinal chemistry
ISSN: 1520-4804
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