| Assay Method Information | |
| | Competitive Inhibition Assay |
| Description: | PSMA binding affinities of the compounds were determined using a competitive inhibition assay as previously reported. Banerjee et al., 2011. FAP, prolyl endopeptidase (PREP), and dipeptidyl dipeptidase 4 (DPPIV) inhibition assays: Recombinant enzymes (FAP, PREP, DPPIV) were purchased from R&D Systems (Minneapolis, MN). FAPI-04 was used as a positive control. Z-Gly-Pro-AMC was used as a substrate for FAP and PREP. H-Gly-Pro-AMC was used as a substrate for DPPIV. The recombinant enzyme (0.4 μg/mL) was incubated with varying amounts of the test articles in the presence of the designated substrate (80 μM) for 10 min at room temperature. Fluorescence intensity was measured with 380 nm excitation and 460 nm emission using the Cytation 5 Cell Imaging Multi-Mode Reader (BioTek, Winooski, VT). IC50 and Ki values were obtained using a sigmoidal dose-response function. Cheng and Prusoff, 1973. |
| Affinity data for this assay | |
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