Drug intelligence / Profile preview

difopein

Development stage
Unknown
Modality
Peptides
01

Overview

Difopein (DImeric FOurteen-three-three PEptide INhibitor) is a high-affinity, dimeric peptide inhibitor of 14-3-3 proteins. It is a dimeric version of the R18 peptide, designed to competitively inhibit 14-3-3-ligand interactions by occupying the amphipathic binding groove of 14-3-3 proteins. By blocking the ability of 14-3-3 to bind to its target proteins (such as Raf-1, Bad, and ASK1), difopein disrupts cell survival signaling pathways and induces apoptosis in various cancer cell lines, including glioma and breast cancer cells. It is widely used as a chemical biology tool to study 14-3-3 protein-protein interactions and as a potential strategy to sensitize cancer cells to chemotherapy.

Other names
DImeric FOurteen-three-three PEptide INhibitordifopein TFAdimeric R18dimeric R18 peptide
02

Targets

SFN (Protein kinase C inhibitor protein 1)

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