Pseudoirreversible inhibition of prostate-specific membrane antigen by phosphoramidate peptidomimetics.

The molecular pruning of a phosphoramidate peptidomimetic inhibitor of prostate-specific membrane antigen.

To identify the pharmacophore of a phosphoramidate peptidomimetic inhibitor of prostate-specific membrane antigen (PSMA), a small analog library was designed and screened for inhibitory potency against PSMA. The design of the lead inhibitor was based upon N-acyl derivatives of endogenous substrate folyl-gamma-Glu and incorporates a phosphoramidate group to interact with the PSMA catalytic zinc ...

68Ga–Prostate-Specific Membrane Antigen: A Potential Radiopharmaceutical in PET/CT To detect primary Cholangiocarcinoma

68Ga Prostate-specific membrane antigen (PSMA) is an increasingly popular radiopharmaceutical tracer in prostate cancer and is becoming increasingly researched in other cancers such as breast cancer, renal cell carcinoma, glioblastoma multiforme, among others. Cholangiocarcinoma is the second most common primary hepatic malignant tumor; it is an aggressive tumor with a 5-year surviva...

Role of Phosphoramidate Antisense in Specific Inhibition of K562 Leukemic Cell Line

Engineered Jurkat Cells for Targeting Prostate-Specific Membrane Antigen on Prostate Cancer Cells by Nanobody-Based Chimeric Antigen Receptor

Background: Recently, modification of T cells with chimeric antigen receptor (CAR) has been an attractive approach for adoptive immunotherapy of cancers. Typically, CARs contain a single-chain variable domain fragment (scFv). Most often, scfvs are derived from a monoclonal antibody of murine origin and may be a trigger for host immune system that leads to the T-cell clearance. Nanobody is a spe...

Expression of Prostate-Specific Membrane Antigen (PSMA) in Brain Glioma and its Correlation with Tumor Grade

Background & Objective Angiogenesis is an essential component of tumor growth. Expression of PSMA on the neo-vasculature of many solid tumors, including glioblastoma multi-form, has been determined. The pattern of expression suggests that PSMA may play a functional role in angiogenesis. Methods: expression of PSMA in dif...