From Tethered to Freestanding Stabilizers of 14‐3‐3 Protein‐Protein Interactions through Fragment Linking
Emira J. Visser,
Priyadarshini Jaishankar,
Eline Sijbesma
et al.
Abstract:Small‐molecule stabilization of protein‐protein interactions (PPIs) is a promising strategy in chemical biology and drug discovery. However, the systematic discovery of PPI stabilizers remains a largely unmet challenge. Herein we report a fragment‐linking approach targeting the interface of 14‐3‐3 and a peptide derived from the estrogen receptor alpha (ERα) protein. Two classes of fragments—a covalent and a noncovalent fragment—were co‐crystallized and subsequently linked, resulting in a noncovalent hybrid mol… Show more
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