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PSMA ligands bind prostate-specific membrane antigen (PSMA), a cell-surface glutamate carboxypeptidase. A complementary DNA encoding PSMA was cloned in 1993 from a human prostate carcinoma cell line. In 1996 the protein was shown to act as a hydrolase with the substrate and inhibitor profile of a neuropeptidase that cleaves N-acetylaspartylglutamate. The enzyme is also known as glutamate carboxypeptidase II and folate hydrolase 1 (FOLH1). Many compounds here carry a urea-linked glutamate motif that fits the active site, coupled to a chelator or labeling group. PSMA-11 carries a chelator for gallium-68, while PSMA-1007 and piflufolastat are fluorinated ligands. tert-Butyl-DCL is a protected inhibitor intermediate, and PSMA-ALB-56 adds an albumin-binding group.
Flotufolastat is a prostate-specific membrane antigen (PSMA) modulator that serves as a radiodiagnostic agent for imaging prostate cancer. This compound is instrumental in enhancing the detection and characterization of prostate cancer lesions. Flotufolastat is valuable for research applications focused on prostate cancer and other malignancies associated with PSMA expression.
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