{"database":"biostudies-literature","file_versions":[],"scores":null,"additional":{"submitter":["Zacharioudakis E"],"funding":["Pershing Square Sohn Cancer Research Alliance","NIA NIH HHS","Irma T. Hirschl Trust","NCI NIH HHS","NIH"],"pagination":["1023-1037"],"full_dataset_link":["https://www.ebi.ac.uk/biostudies/studies/S-EPMC9669135"],"repository":["biostudies-literature"],"omics_type":["Unknown"],"volume":["47(12)"],"pubmed_abstract":["Dynamic protein complexes function in all cellular processes, from signaling to transcription, using distinct conformations that regulate their activity. Conformational switching of proteins can turn on or off their activity through protein-protein interactions, catalytic function, cellular localization, or membrane interaction. Recent advances in structural, computational, and chemical methodologies have enabled the discovery of small-molecule activators and inhibitors of conformationally dynamic proteins by using a more rational design than a serendipitous screening approach. Here, we discuss such recent examples, focusing on the mechanism of protein conformational switching and its regulation by small molecules. We emphasize the rational approaches to control protein oligomerization wit"],"journal":["Trends in biochemical sciences"],"pubmed_title":["Targeting protein conformations with small molecules to control protein complexes."],"pmcid":["PMC9669135"],"funding_grant_id":["R01 CA178394","P30 AG038072","P30 CA013330","R01 CA238229","P01 AG031782"],"pubmed_authors":["Gavathiotis E","Zacharioudakis E"],"additional_accession":[]},"is_claimable":false,"name":"Targeting protein conformations with small molecules to control protein complexes.","description":"Dynamic protein complexes function in all cellular processes, from signaling to transcription, using distinct conformations that regulate their activity. Conformational switching of proteins can turn on or off their activity through protein-protein interactions, catalytic function, cellular localization, or membrane interaction. Recent advances in structural, computational, and chemical methodologies have enabled the discovery of small-molecule activators and inhibitors of conformationally dynamic proteins by using a more rational design than a serendipitous screening approach. Here, we discuss such recent examples, focusing on the mechanism of protein conformational switching and its regulation by small molecules. We emphasize the rational approaches to control protein oligomerization wit","dates":{"release":"2022-01-01T00:00:00Z","publication":"2022 Dec","modification":"2025-04-04T09:50:11.718Z","creation":"2025-02-19T01:17:39.426Z"},"accession":"S-EPMC9669135","cross_references":{"pubmed":["35985943"],"doi":["10.1016/j.tibs.2022.07.002"]}}