High-Throughput Selectivity Assays for Small-Molecule Inhibitors of β-Catenin/T-Cell Factor Protein–Protein Interactions
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چکیده
منابع مشابه
High-throughput assays for promiscuous inhibitors.
High-throughput screening (HTS) searches large libraries of chemical compounds for those that can modulate the activity of a particular biological target; it is the dominant technique used in early-stage drug discovery. A key problem in HTS is the prevalence of nonspecific or 'promiscuous' inhibitors. These molecules have peculiar properties, act on unrelated targets and can dominate the result...
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Small-molecules that inhibit interactions between specific pairs of proteins have long represented a promising avenue for therapeutic intervention in a variety of settings. Structural studies have shown that in many cases, the inhibitor-bound protein adopts a conformation that is distinct from its unbound and its protein-bound conformations. This plasticity of the protein surface presents a maj...
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ژورنال
عنوان ژورنال: ACS Medicinal Chemistry Letters
سال: 2013
ISSN: 1948-5875,1948-5875
DOI: 10.1021/ml300367f