Malik Noeen, Machulla Hans-Jürgen, Solbach Christoph, Winter Gordon, Reske Sven N, Zlatopolskiy Boris
Clinic for Nuclear Medicine, University Hospital, Ulm, Germany.
Appl Radiat Isot. 2011 Jul;69(7):1014-8. doi: 10.1016/j.apradiso.2011.03.041. Epub 2011 Apr 8.
Due to the specificity of expression of PSMA (prostate specific membrane antigen) particularly in prostate cancer cells (e.g. LNCaP), numerous PSMA ligands have been synthesized until now. In the current study, we synthesized DUPA-Pep having 2-[3-(1,3-dicarboxypropyl)ureido]pentanedioic acid (DUPA) linked via 8-aminooctanoic acid to two phenylalanine residues and chose 6-[(18)F]fluoronicotinic acid 2,3,5,6-tetrafluorophenyl ester [(18)F]FPy-TFP as a prosthetic group for coupling. [(18)F]FPy-DUPA-Pep was obtained in a radiochemical yield of 48±0.9% (decay uncorrected) within 50 min with a chemical purity of >98%.
由于前列腺特异性膜抗原（PSMA）表达的特异性，尤其是在前列腺癌细胞（如LNCaP）中的特异性，到目前为止已经合成了许多PSMA配体。在本研究中，我们合成了DUPA-Pep，它具有通过8-氨基辛酸连接到两个苯丙氨酸残基的2-[3-(1,3-二羧丙基)脲基]戊二酸（DUPA），并选择6-[(18)F]氟烟酸2,3,5,6-四氟苯酯[(18)F]FPy-TFP作为用于偶联的辅基。[(18)F]FPy-DUPA-Pep在50分钟内以48±0.9%（未校正衰变）的放射化学产率获得，化学纯度>98%。
