Cell-permeable covalent ligand that selectively modifies a non-catalytic, allosteric cysteine C23 in the K48 ubiquitin-specific deubiquitinase OTUB1
EN523 is a cell-permeable covalent ligand that selectively modifies a non-catalytic, allosteric cysteine C23 in the K48 ubiquitin-specific deubiquitinase OTUB1. EN523 does not inhibit OTUB1 deubiquitination activity and serves as OTUB1 recruiter.
Nature chemical biology, 18(4), 412-421 (2022-02-26)
Many diseases are driven by proteins that are aberrantly ubiquitinated and degraded. These diseases would be therapeutically benefited by targeted protein stabilization (TPS). Here we present deubiquitinase-targeting chimeras (DUBTACs), heterobifunctional small molecules consisting of a deubiquitinase recruiter linked to a
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