Synthesis and Biological Evaluation of PSMA Ligands with Aromatic Residues and Fluorescent Conjugates Based on Them

• Published in: Journal of medicinal chemistry Vol. 64; no. 8; pp. 4532 - 4552
• Main Authors: Machulkin, Aleksei E, Shafikov, Radik R, Uspenskaya, Anastasia A, Petrov, Stanislav A, Ber, Anton P, Skvortsov, Dmitry A, Nimenko, Ekaterina A, Zyk, Nikolay U, Smirnova, Galina B, Pokrovsky, Vadim S, Abakumov, Maxim A, Saltykova, Irina V, Akhmirov, Rauf T, Garanina, Anastasiia S, Polshakov, Vladimir I, Saveliev, Oleg Y, Ivanenkov, Yan A, Aladinskaya, Anastasiya V, Finko, Alexander V, Yamansarov, Emil U, Krasnovskaya, Olga O, Erofeev, Alexander S, Gorelkin, Petr V, Dontsova, Olga A, Beloglazkina, Elena K, Zyk, Nikolay V, Khazanova, Elena S, Majouga, Alexander G
• Format: Journal Article
• Language: English
• Published: WASHINGTON American Chemical Society 22.04.2021; Amer Chemical Soc
• Subjects: Chemistry, Medicinal; Life Sciences & Biomedicine; Pharmacology & Pharmacy; Science & Technology; DESIGN; ACTIVE-SITE; GLUTAMATE-CARBOXYPEPTIDASE-II; CONTRAST; INHIBITORS; IMAGING AGENTS; MEMBRANE ANTIGEN PSMA; PRECLINICAL EVALUATION; PROBES

Prostate-specific membrane antigen (PSMA), also known as glutamate carboxypeptidase II (GCPII), is a suitable target for specific delivery of antitumor drugs and diagnostic agents due to its overexpression in prostate cancer cells. In the current work, we describe the design, synthesis, and biologic...