Related Experiment Video

Updated: Nov 9, 2025

Development of Inhibitors of Protein-protein Interactions through REPLACE: Application to the Design and Development Non-ATP Competitive CDK Inhibitors
10:33

Development of Inhibitors of Protein-protein Interactions through REPLACE: Application to the Design and Development Non-ATP Competitive CDK Inhibitors

Published on: October 26, 2015

11.6K

Recent advances in β-catenin/BCL9 protein-protein interaction inhibitors

Hao Zhang1,2, Ya Bao1,3, Chenglong Liu2

  • 1Novel Technology Center of Pharmaceutical Chemistry, Shanghai Institute of Pharmaceutical Industry, China State Institute of Pharmaceutical Industry, Shanghai, 201203, China.

Future Medicinal Chemistry
|April 14, 2021
PubMed

Insights

Targeting the Wnt/β-catenin pathway by inhibiting the β-catenin/BCL9 protein-protein interaction (PPI) shows promise for treating diseases like cancer. This review summarizes current progress and future directions for developing these crucial inhibitors.

Area of Science:

  • Molecular Biology
  • Drug Discovery
  • Biochemistry

Background:

  • Wnt/β-catenin signaling is vital for embryonic development and organismal homeostasis.
  • Dysregulation of Wnt signaling is implicated in various pathologies, including cancer and fibrosis.
  • Targeting the β-catenin/BCL9 protein-protein interaction (PPI) offers a novel strategy to inhibit the Wnt pathway.

Purpose of the Study:

  • To review the discovery and development of β-catenin/BCL9 PPI inhibitors.
  • To explore drug design, structure-activity relationships, and biological properties of these inhibitors.
  • To provide perspectives on future research and development in this area.

Main Methods:

  • Literature review of published research on β-catenin/BCL9 PPI inhibitors.
  • Analysis of drug design strategies and structure-activity relationships.
  • Evaluation of biological and biochemical data for identified inhibitors.

Main Results:

  • Understanding the β-catenin/BCL9 complex structure and mechanism aids inhibitor discovery.
  • Few β-catenin/BCL9 PPI inhibitors have been reported to date.
  • This review consolidates existing knowledge on inhibitor development.

Conclusions:

  • Directly targeting the β-catenin/BCL9 PPI is a viable therapeutic strategy.
  • Further research is needed to expand the repertoire of β-catenin/BCL9 PPI inhibitors.
  • Future development holds promise for novel treatments for Wnt-related diseases.
Keywords:
Wnt signalinginhibitorsprotein–protein interactionβ-catenin/BCL9

More Related Videos

Reconstitution Of β-catenin Degradation In Xenopus Egg Extract09:41

Reconstitution Of β-catenin Degradation In Xenopus Egg Extract

Published on: June 17, 2014

12.3K
Identifying Protein-protein Interaction Sites Using Peptide Arrays07:44

Identifying Protein-protein Interaction Sites Using Peptide Arrays

Published on: November 18, 2014

18.3K

Related Concept Videos

Catenins01:23

Catenins

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.
Catenins in Cell Junctions
Catenins bind to cell adhesion molecules such as cadherins and link them to different cytoskeletal proteins depending on the type of cell junction. At the...
2.7K
Inhibition of Cdk Activity02:34

Inhibition of Cdk Activity

The orderly progression of the cell cycle depends on the activation of Cdk protein by binding to its cyclin partner. However, the cell cycle must be restricted when undergoing abnormal changes. Most cancers correlate to the deregulated cell cycle, and since Cdks are a central component of the cell cycle, Cdk inhibitors are extensively studied to develop anticancer agents. For instance, cyclin D associates with several Cdks, such as Cdk 4/6, to form an active complex. The cyclin D-Cdk4/6 complex...
5.2K
Protein-protein Interfaces02:04

Protein-protein Interfaces

Many proteins form complexes to carry out their functions, making protein-protein interactions (PPIs) essential for an organism's survival. Most PPIs are stabilized by numerous weak noncovalent chemical forces. The physical shape of the interfaces determines the way two proteins interact. Many globular proteins have closely-matching shapes on their surfaces, which form a large number of weak bonds. Additionally, many PPIs occur between two helices or between a surface cleft and a...
14.1K