TED-347 is an Irreversible and Covalent YAP-TEAD Protein-Protein Interaction Inhibitor
Yap1, also known as Yap, is a protein that acts as a transcription regulator by activating the transcription of genes involved in cell proliferation and inhibiting apoptosis. Specifically, Yap1 is inhibited in the hippopotamus signaling pathway, which can control organ size and inhibit tumors. Besides, hippopotamus signaling regulates Yap1...
MYCMI-6 is a Selective Endogenous MYC:MAX Inhibitor
The MYC family of oncogenes (MYC, MYCN, and MYCL), encodes basic helix-loop-helix leucine zipper (bHLHZip) transcription factors. Through the HLHZip domain, MYC heterodimerizes with the bHLHZip protein MAX, which enables the MYC:MAX complex to bind E-box regulatory DNA elements throughout the genome. Therefore, it controls the transcription of a...
SNDX-5613 is a Potent and Specific Menin-MLL Inhibitor
Mixed lineage leukemia (MLL) is a very aggressive blood cancer that predominantly occurs in pediatric patients. Especially, MLL is acute leukemia with poor prognosis. Spontaneous translocations at the MLL1 gene cause MLL. MLL fusions bind with a high affinity to the nuclear protein Menin. Menin-MLL interaction enables leukemic transformation...
ARCC-4 is a Highly Potent PROTAC Androgen Receptor Degrader
Androgen receptor (AR) signaling is crucial for normal prostate development. It also drives the growth and survival of prostate cancer cells. AR signaling suppression is a common strategy for treating prostate cancer. Like other occupancy-based inhibitors, the antiandrogen enzalutamide requires high saturating drug concentrations to achieve its clinical benefit....
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...