{"database":"biostudies-literature","file_versions":[],"scores":null,"additional":{"submitter":["Liu W"],"funding":["Swiss National Science Foundation"],"pagination":["954-962"],"full_dataset_link":["https://www.ebi.ac.uk/biostudies/studies/S-EPMC8227592"],"repository":["biostudies-literature"],"omics_type":["Unknown"],"volume":["7(6)"],"pubmed_abstract":["Sesquiterpenes are a rich source of covalent inhibitors with a long history in traditional medicine and include several important therapeutics and tool compounds. Herein, we report the total synthesis of 16 sesquiterpene lactones via a build/couple/pair strategy, including goyasensolide. Using an alkyne-tagged cellular probe and proteomics analysis, we discovered that goyazensolide selectively targets the oncoprotein importin-5 (IPO5) for covalent engagement. We further demonstrate that goyazensolide inhibits the translocation of RASAL-2, a cargo of IPO5, into the nucleus and perturbs the binding between IPO5 and two specific viral nuclear localization sequences."],"journal":["ACS central science"],"pubmed_title":["Identification of a Covalent Importin-5 Inhibitor, Goyazensolide, from a Collective Synthesis of Furanoheliangolides."],"pmcid":["PMC8227592"],"funding_grant_id":["188406","200020_169141"],"pubmed_authors":["Patouret R","Barluenga S","Plank M","Loewith R","Liu W","Winssinger N"],"additional_accession":[]},"is_claimable":false,"name":"Identification of a Covalent Importin-5 Inhibitor, Goyazensolide, from a Collective Synthesis of Furanoheliangolides.","description":"Sesquiterpenes are a rich source of covalent inhibitors with a long history in traditional medicine and include several important therapeutics and tool compounds. Herein, we report the total synthesis of 16 sesquiterpene lactones via a build/couple/pair strategy, including goyasensolide. Using an alkyne-tagged cellular probe and proteomics analysis, we discovered that goyazensolide selectively targets the oncoprotein importin-5 (IPO5) for covalent engagement. We further demonstrate that goyazensolide inhibits the translocation of RASAL-2, a cargo of IPO5, into the nucleus and perturbs the binding between IPO5 and two specific viral nuclear localization sequences.","dates":{"release":"2021-01-01T00:00:00Z","publication":"2021 Jun","modification":"2025-05-18T11:03:23.98Z","creation":"2025-05-18T11:03:23.98Z"},"accession":"S-EPMC8227592","cross_references":{"pubmed":["34235256"],"doi":["10.1021/acscentsci.1c00056"]}}