Compound class:
Synthetic organic
Comment: This compound is reported to disrupt the β-catenin/B-cell lymphoma 9 (BCL9) interaction, by binding to β-catenin [1]. It was designed to block Wnt signalling and expression of oncogenic Wnt target genes, as a mechanism to target colorectal cancer. Since approximately 80% of colorectal cancers carry activating Wnt/β-catenin pathway mutations, this pathway is an active molecular target for oncology therapeutic development.
The chemical structure shown here is used to represent the racemic mixture of (S)-41 and (R)-41. Experiments comparing the in vitro activities of the isolated enantiomers and the racemate, showed that the chiral centers in the molecule do not significantly alter its binding interaction with β-catenin [1]. |
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References |
1. Zhang H, Liu C, Chen Q, Shen LA, Xiao W, Li J, Wang Y, Zhu D, Zhang Q, Li J. (2023)
Discovery of Novel 3-Phenylpiperidine Derivatives Targeting the β-Catenin/B-Cell Lymphoma 9 Interaction as a Single Agent and in Combination with the Anti-PD-1 Antibody for the Treatment of Colorectal Cancer. J Med Chem, 66 (2): 1349-1379. [PMID:36630177] |