Structure-based design of a phosphotyrosine-masked covalent ligand targeting the E3 ligase SOCS2

Abstract The Src homology 2 (SH2) domain recognizes phosphotyrosine (pY) post translational modifications in partner proteins to trigger downstream signaling. Drug discovery efforts targeting the SH2 domains have long been stymied by the poor drug-like properties of phosphate and its mimetics. Here,...

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Hauptverfasser: Sarath Ramachandran, Nikolai Makukhin, Kevin Haubrich, Manjula Nagala, Beth Forrester, Dylan M. Lynch, Ryan Casement, Andrea Testa, Elvira Bruno, Rosaria Gitto, Alessio Ciulli
Format: Artigo
Sprache:Englisch
Veröffentlicht: 2023
Online-Zugang:https://doi.org/10.1038/s41467-023-41894-3
https://www.nature.com/articles/s41467-023-41894-3.pdf
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