Pseudoirreversible inhibition of prostate-specific membrane antigen by phosphoramidate peptidomimetics
| Autor: | Marat Kazak, Clifford E. Berkman, Yoko Toriyabe, Tiancheng Liu |
|---|---|
| Rok vydání: | 2008 |
| Předmět: |
Glutamate Carboxypeptidase II
Peptidomimetic media_common.quotation_subject urologic and male genital diseases Biochemistry Cell Line Prostate cancer Antigen Biomimetic Materials Glutamate carboxypeptidase II medicine Animals Humans Phosphoric Acids Enzyme Inhibitors Internalization Membrane antigen media_common Chemistry Phosphoramidate medicine.disease Amides Protein Transport Cell culture Antigens Surface Peptides |
| Zdroj: | Biochemistry. 47(48) |
| ISSN: | 1520-4995 |
| Popis: | The mode of inhibition for phosphoramidate peptidomimetic inhibitors of prostate-specific membrane antigen was determined by inhibition reversibility experiments. The results revealed that these inhibitors can be classified into three types: pseudoirreversible (compounds 1-3), moderately reversible (compounds 4-9), and rapidly reversible inhibitors (compounds 10 and 11). Representative compounds from each class were further evaluated for their ability to induce cellular internalization of PSMA. Results from these experiments revealed that the pseudoirreversible inhibitor 1 induced the greatest PSMA internalization. The discovery of pseudoirreversible PSMA inhibitors is expected to provide a new avenue of investigation and therapeutic applications for prostate cancer and neurological disorders. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|