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Inhibitors of beta-Catenin Signaling

Inhibitors of beta-Catenin Signaling

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ChemDiv’s Inhibitors of beta-Catenin Signaling Library contains 8,000 compounds.

β-Catenin is a fascinating protein with many important cellular and developmental functions. The roles of b-catenin are ‘classically’ defined: as an adhesion protein and as a signaling protein, transducing extracellular signals to the nucleus to modify gene expression. β -catenin has many binding partners that mediate a diverse set of cellular functions, and the protein probably acts as a ‘hub’ on which many cellular signaling networks impinge. Wnt/β-catenin signaling is a branch of a functional network that is involved in a broad range of biological systems including stem cells, embryonic development and adult organs. Deregulation of components involved in Wnt/β-catenin signaling has been implicated in a wide spectrum of diseases including a number of cancers and degenerative diseases.

ChemDiv proposes the new library of beta-catenin inhibitors/modulators. This library represents a selection of drug-like compounds aimed at modulating protein-protein interaction (PPI) of β-catenin with different proteins involved in significant physiological processes. Library has been assembled using in house structural biology insight, molecular stimulation-modeling, virtual screening of ChemDiv’s novel chemistries and medicinal chemistry filtering/ranking of the resulting hits. A representative example of a ‘druggable’ ‘hot spots’ included specific topological features of the β -catenin interaction.

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