{"database":"biostudies-literature","file_versions":[],"scores":null,"additional":{"omics_type":["Unknown"],"volume":["21(1)"],"submitter":["Thomas SR"],"pubmed_abstract":["Proteolysis targeting chimeras (PROTACs) are bifunctional molecules designed to induce the degradation of specific proteins within a cell. While most PROTACs are noncovalent interactors, covalent PROTACs may benefit from improved selectivity and pharmacodynamics, yet remain largely understudied. Here, a covalent gold-based PROTAC (<b>AuPROTAC</b>) was synthesized, featuring a Au(III)-warhead, known to induce cysteine-arylation in a gold-templated two-step mechanism, linked to a cereblon binding moiety. The degradome of the <b>AuPROTAC</b> was characterized by establishing a cycloheximide chase assay in a nonproliferative steady-state HL-60 cell culture, enabling the identification of PROTAC degradation targets uncoupled from confounding effects originating from cell-cycle-dependent transla"],"journal":["ACS chemical biology"],"pagination":["170-186"],"full_dataset_link":["https://www.ebi.ac.uk/biostudies/studies/S-EPMC12813982"],"repository":["biostudies-literature"],"pubmed_title":["A Gold-PROTAC Degrades the Oncogenic Tyrosine Kinase MERTK: Insights into the Degradome from a Steady-State System."],"pmcid":["PMC12813982"],"pubmed_authors":["Casini A","Gerner C","Thomas SR","Meier-Menches SM","Park M","Iellici T","Bileck A","Klaus E"],"additional_accession":[]},"is_claimable":false,"name":"A Gold-PROTAC Degrades the Oncogenic Tyrosine Kinase MERTK: Insights into the Degradome from a Steady-State System.","description":"Proteolysis targeting chimeras (PROTACs) are bifunctional molecules designed to induce the degradation of specific proteins within a cell. While most PROTACs are noncovalent interactors, covalent PROTACs may benefit from improved selectivity and pharmacodynamics, yet remain largely understudied. Here, a covalent gold-based PROTAC (<b>AuPROTAC</b>) was synthesized, featuring a Au(III)-warhead, known to induce cysteine-arylation in a gold-templated two-step mechanism, linked to a cereblon binding moiety. The degradome of the <b>AuPROTAC</b> was characterized by establishing a cycloheximide chase assay in a nonproliferative steady-state HL-60 cell culture, enabling the identification of PROTAC degradation targets uncoupled from confounding effects originating from cell-cycle-dependent transla","dates":{"release":"2026-01-01T00:00:00Z","publication":"2026 Jan","modification":"2026-07-15T13:31:34.842Z","creation":"2026-07-05T03:08:34.868Z"},"accession":"S-EPMC12813982","cross_references":{"pubmed":["41486557"],"doi":["10.1021/acschembio.5c00860"]}}