During this year we also developed assays to screen activities at two addiction-associated CAM targets. BRET assay for identifying possible antagonists of CDH13 homomeric binding displayed calcium dependence, antagonism by soluble CDH13 peptides and other features anticipated of a bona fide assay for CDH13 ligands. Recombinant PTPRD phosphatase domains were purified in modest amounts from expressing bacteria, and evinced phosphatase activities in colorimetric and fluorometric assays likely to allow screening of PTPRD phosphatase antagonists. We were able to obtain funding to allow collaborators to synthesize illudalic acid analogs that are likely to display activities at the PTPRD phosphatase domain, since they are active at the phosphatase domains of PTPRD family members in work reported by others. We used the CDH13 BRET assay to screen chemical libraries of compounds used in humans. Only leads that proved to be false positives were identified, in ways that fit with ideas that we might have known CDH13 antagonists due to their likely clinical profile for compounds that had been used in man.
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