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Deprecated: Implicit conversion from float 245.2 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 ACS+Med+Chem+Lett 2013 ; 4 (2): 306-11 Nephropedia Template TP
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High-Throughput Selectivity Assays for Small-Molecule Inhibitors of ?-Catenin/T-Cell Factor Protein?Protein Interactions #MMPMID24900664
Zhang M; Catrow JL; Ji H
ACS Med Chem Lett 2013[Feb]; 4 (2): 306-11 PMID24900664show ga
Two homogeneous high-throughput assays, AlphaScreen and fluorescence polarization, were established to quantify inhibitor selectivity between different protein?protein complexes. As a first case study, they have been successfully applied to the key protein?protein interactions in the downstream sites of the canonical Wnt signaling pathway. The aberrant formation of the ?-catenin/T-cell factor (Tcf) complex is the major driving force for many cancers and fibroses. Crystallographic and biochemical studies reveal that the binding modes of Tcf, E-cadherin, and adenomatous polyposis coli (APC) to ?-catenin are identical and mutually exclusive. In the present study, two highly sensitive and robust assays were established to quantitatively evaluate inhibitor selectivity between ?-catenin/Tcf, ?-catenin/E-cadherin, and ?-catenin/APC interactions. A pilot screen demonstrated the feasibility of the assays and yielded four hits for the disruption of ?-catenin/Tcf interactions. A potent and dual-selective ?-catenin/Tcf inhibitor was identified.