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

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

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, we use structure-based design to target the SH2 domain of the E3 ligase suppressor of cytokine signaling 2 (SOCS2).

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

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

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