{"database":"biostudies-literature","file_versions":[],"scores":null,"additional":{"omics_type":["Unknown"],"submitter":["Li YD"],"funding":["NCI NIH HHS"],"pubmed_abstract":["Small molecules that induce protein-protein interactions to exert proximity-driven pharmacology such as targeted protein degradation are a powerful class of therapeutics<sup>1-3</sup>. Molecular glues are of particular interest given their favorable size and chemical properties and represent the only clinically approved degrader drugs<sup>4-6</sup>. The discovery and development of molecular glues for novel targets, however, remains challenging. Covalent strategies could in principle facilitate molecular glue discovery by stabilizing the neo-protein interfaces. Here, we present structural and mechanistic studies that define a <i>trans</i>-labeling covalent molecular glue mechanism, which we term \"template-assisted covalent modification\". We found that a novel series of BRD4 molecular glue "],"journal":["bioRxiv : the preprint server for biology"],"pagination":["2023.02.14.528208"],"full_dataset_link":["https://www.ebi.ac.uk/biostudies/studies/S-EPMC9949066"],"repository":["biostudies-literature"],"pubmed_title":["Template-assisted covalent modification of DCAF16 underlies activity of BRD4 molecular glue degraders."],"pmcid":["PMC9949066"],"funding_grant_id":["K00 CA253754"],"pubmed_authors":["Lumpkin R","Qi J","Park PMC","Jin CY","Wang MY","Ebert BL","Slabicki M","Puvar K","Zou C","Hunkeler M","Yoon H","Ficarro SB","Sandoval B","Hassan MM","Fischer ES","Marto JA","Teng M","Sigua LH","Tavares I","Li YD","Tsai JM","Gray NS","Majewski FC","Nowak RP","Donovan KA","Xu S","Groendyke BJ","Ma MW"],"additional_accession":[]},"is_claimable":false,"name":"Template-assisted covalent modification of DCAF16 underlies activity of BRD4 molecular glue degraders.","description":"Small molecules that induce protein-protein interactions to exert proximity-driven pharmacology such as targeted protein degradation are a powerful class of therapeutics<sup>1-3</sup>. Molecular glues are of particular interest given their favorable size and chemical properties and represent the only clinically approved degrader drugs<sup>4-6</sup>. The discovery and development of molecular glues for novel targets, however, remains challenging. Covalent strategies could in principle facilitate molecular glue discovery by stabilizing the neo-protein interfaces. Here, we present structural and mechanistic studies that define a <i>trans</i>-labeling covalent molecular glue mechanism, which we term \"template-assisted covalent modification\". We found that a novel series of BRD4 molecular glue ","dates":{"release":"2023-01-01T00:00:00Z","publication":"2023 Feb","modification":"2025-04-04T11:26:47.349Z","creation":"2025-04-04T11:26:47.349Z"},"accession":"S-EPMC9949066","cross_references":{"pubmed":["36824856"],"doi":["10.1101/2023.02.14.528208"]}}