Tag: PPI

F1324 is a High Affinity BCL6 Peptidic Inhibitor

B cell lymphoma 6 (BCL6) is a transcriptional repressor that interacts with its corepressors BcoR and SMRT. Since this protein-protein interaction (PPI) induces activation and differentiation of B lymphocytes, BCL6 is an attractive drug target for potential autoimmune disease treatments. In addition, BCL6 acts as a master regulator of...

BI-9321, a First-in-Class Chemical Probe, is a NSD3-PWWP1 Inhibitor

Post-translational modification of histones by histone-modifying enzymes represents a key element of epigenetic regulation. Epigenetic reader domains are structurally diverse. They include bromodomains, PHD domains, methyl-lysine- and/or methyl-arginine-binding domains, frequently co-locating within the same proteins. By interfering with the function of specific domains, selective chemical probes represent powerful tools...

NRX-252262, an Enhancer of β-catenin:β-TrCP Interaction

To develop small molecules that modulate protein-protein interactions (PPIs) displays a significant therapeutic potential. However, rational design of small molecule enhancers of PPIs remains elusive. A study from Kyle R. Simonetta, et al. reported the potent small molecules that enhance the interaction between an oncogenic transcription factor, β-Catenin, and...