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Related Concept Videos

Catenins01:23

Catenins

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Catenins are characterized by multiple binding domains and dynamic structures that allow them to function as linker proteins in cell junction complexes. All catenins, except α-catenin, contain a characteristic protein sequence called the armadillo repeat and are therefore also called armadillo proteins.
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The gene encoding the main signaling molecules of the Wnt signaling pathways (the Wnt proteins) was discovered almost four decades ago by Nüsslein-Volhard and Wieschaus. They identified and originally named the gene "wingless" (wg) after a phenotype discovered during their landmark genetic screen in Drosophila for body pattern defects. At around the same time, another researcher named Harold Varmus found that a murine tumor virus activates the mammalian wg homolog, Int-1, which...
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Many proteins’ biological role depends on their interactions with their ligands, small molecules that bind to specific locations on the protein known as ligand-binding sites. Ligand-binding sites are often conserved among homologous proteins as these sites are critical for protein function.
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Related Experiment Video

Updated: Nov 27, 2025

Biotinylated Cell-penetrating Peptides to Study Intracellular Protein-protein Interactions
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Getting a Grip on the Undrugged: Targeting β-Catenin with Fragment-Based Methods.

Dirk Kessler1, Moriz Mayer1, Stephan K Zahn1

  • 1Boehringer Ingelheim RCV GmbH & Co KG, Dr.-Boehringer-Gasse 5-11, 1121, Vienna, Austria.

Chemmedchem
|December 4, 2020
PubMed
Summary
This summary is machine-generated.

Researchers discovered a small molecule that binds to beta-catenin, a protein involved in cancer. This finding provides a foundation for developing new cancer therapies targeting beta-catenin degradation.

Keywords:
PROTACWaterLOGSYfragment-based screeningmicroscale thermophoresisβ-catenin

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Area of Science:

  • Oncology
  • Molecular Biology
  • Drug Discovery

Background:

  • Aberrant WNT pathway activation, characterized by nuclear beta-catenin accumulation, drives cancer progression.
  • Mutations in the APC tumor suppressor gene impair beta-catenin degradation, promoting its nuclear translocation and oncogenic activity.

Purpose of the Study:

  • To report the fragment-based discovery of a small molecule binder for beta-catenin.
  • To elucidate the binding mode of the identified small molecule using X-ray crystallography.

Main Methods:

  • Fragment-based drug discovery approach.
  • Iterative virtual screening and Nuclear Magnetic Resonance (NMR) screening.
  • X-ray crystallography for structural elucidation of the beta-catenin-ligand complex.

Main Results:

  • Identified a small molecule binder for beta-catenin, overcoming initial screening challenges.
  • Determined the binding site to be between armadillo repeats two and three, adjacent to BCL9 and TCF4 interaction sites.
  • Structural data and assays suggest limited potential for direct protein-protein interaction inhibition but offer a basis for PROTAC development.

Conclusions:

  • The discovered beta-catenin binder provides a starting point for therapeutic strategies.
  • Structural insights pave the way for developing beta-catenin proteolysis targeting chimeras (PROTACs) as a novel therapeutic modality.