EN171 is a covalent ligand that selectively modifies cysteine residues C38 and C96 on the 14-3-3 protein, thereby promoting its interactions with estrogen receptor α (ERα), YAP, and TAZ. This modulation leads to a reduction in transcriptional activity associated with both estrogen signaling and the Hippo pathway. EN171 serves as a molecular glue, enhancing native protein interactions, and acts as a covalent recruiter of 14-3-3 in heterobifunctional applications, facilitating the cytosolic sequestering of nuclear neo-substrates such as BRD4 and BCL6.
EN171 is a covalent ligand that selectively modifies cysteine residues C38 and C96 on the 14-3-3 protein, thereby promoting its interactions with estrogen receptor α (ERα), YAP, and TAZ. This modulation leads to a reduction in transcriptional activity associated with both estrogen signaling and the Hippo pathway. EN171 serves as a molecular glue, enhancing native protein interactions, and acts as a covalent recruiter of 14-3-3 in heterobifunctional applications, facilitating the cytosolic sequestering of nuclear neo-substrates such as BRD4 and BCL6.
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