{"database":"biostudies-literature","file_versions":[],"scores":null,"additional":{"submitter":["Siokatas C"],"funding":["European Union and Greek national funds"],"pagination":["3955-3968"],"full_dataset_link":["https://www.ebi.ac.uk/biostudies/studies/S-EPMC11650737"],"repository":["biostudies-literature"],"omics_type":["Unknown"],"volume":["7(12)"],"pubmed_abstract":["Although small-molecule inhibitors with moderate efficacy targeting MYC have been previously described, to this point, research efforts have failed to bring a suitable small-molecule MYC inhibitor to the clinic. Herein, the discovery of a series of novel MYC degraders bearing VHL to target the \"undruggable\" MYC is presented. The molecules are based on connecting a known MYC binder to a VHL ligand or pomalidomide to induce MYC degradation in various cancer cells known to express MYC. Representative compounds from our work induced MYC degradation in a time- and dose-dependent manner. Selected compounds, <b>CSI86</b> and <b>CSI107</b>, displayed antiproliferative activity (IC<sub>50</sub> values of 13-18 μM) against breast and prostate cancer cells. The lead molecules were further evaluated i"],"journal":["ACS pharmacology & translational science"],"pubmed_title":["Developing MYC Degraders Bearing the Von Hippel-Lindau Ligand to Target the \"Undruggable\" MYC."],"pmcid":["PMC11650737"],"funding_grant_id":["MIS 5028091","MIS5002691","MIS 5002550"],"pubmed_authors":["Lampropoulou A","Kontostathi M","Tamvakopoulos C","Smina A","Sarli V","Politou AS","Soupsana K","Karra AV","Christoforidis S","Karampelas T","Siokatas C"],"additional_accession":[]},"is_claimable":false,"name":"Developing MYC Degraders Bearing the Von Hippel-Lindau Ligand to Target the \"Undruggable\" MYC.","description":"Although small-molecule inhibitors with moderate efficacy targeting MYC have been previously described, to this point, research efforts have failed to bring a suitable small-molecule MYC inhibitor to the clinic. Herein, the discovery of a series of novel MYC degraders bearing VHL to target the \"undruggable\" MYC is presented. The molecules are based on connecting a known MYC binder to a VHL ligand or pomalidomide to induce MYC degradation in various cancer cells known to express MYC. Representative compounds from our work induced MYC degradation in a time- and dose-dependent manner. Selected compounds, <b>CSI86</b> and <b>CSI107</b>, displayed antiproliferative activity (IC<sub>50</sub> values of 13-18 μM) against breast and prostate cancer cells. The lead molecules were further evaluated i","dates":{"release":"2024-01-01T00:00:00Z","publication":"2024 Dec","modification":"2026-06-06T13:24:07.999Z","creation":"2026-05-31T03:07:27.315Z"},"accession":"S-EPMC11650737","cross_references":{"pubmed":["39698270"],"doi":["10.1021/acsptsci.4c00452"]}}