{"database":"biostudies-literature","file_versions":[],"scores":null,"additional":{"submitter":["Maslivetc VA"],"funding":["BLRD VA","NCI NIH HHS","National Institutes of Health"],"pagination":["129863"],"full_dataset_link":["https://www.ebi.ac.uk/biostudies/studies/S-EPMC11646455"],"repository":["biostudies-literature"],"omics_type":["Unknown"],"volume":["110"],"pubmed_abstract":["Glioblastoma (GBM) is the most common form of malignant primary brain tumor and is one of the most lethal cancers. The difficulty in treating GBM stems from its highly developed mechanisms of drug resistance. Our research team has recently identified the fungal secondary metabolite ophiobolin A (OpA) as an agent with significant activity against drug-resistant GBM cells. However, the OpA's mode of action is likely based on covalent modification of its intracellular target(s) and thus possible off-target reactivity needs to be addressed. This work involves the investigation of an acid-sensitive OpA analogue approach that exploits the elevated acidity of the GBM microenvironment to enhance the selectivity for tumor targeting. This project identified analogues that showed selectivity at killi"],"journal":["Bioorganic & medicinal chemistry letters"],"pubmed_title":["Ophiobolin A derivatives with enhanced activities under tumor-relevant acidic conditions."],"pmcid":["PMC11646455"],"funding_grant_id":["R15 CA227680","IK6 BX005647-01","IK6 BX005647","1R15CA227680-01A1"],"pubmed_authors":["Nabiul Hasan M","Maslivetc VA","Sun D","Zejnelovski A","Evidente A","Kornienko A","Boari A"],"additional_accession":[]},"is_claimable":false,"name":"Ophiobolin A derivatives with enhanced activities under tumor-relevant acidic conditions.","description":"Glioblastoma (GBM) is the most common form of malignant primary brain tumor and is one of the most lethal cancers. The difficulty in treating GBM stems from its highly developed mechanisms of drug resistance. Our research team has recently identified the fungal secondary metabolite ophiobolin A (OpA) as an agent with significant activity against drug-resistant GBM cells. However, the OpA's mode of action is likely based on covalent modification of its intracellular target(s) and thus possible off-target reactivity needs to be addressed. This work involves the investigation of an acid-sensitive OpA analogue approach that exploits the elevated acidity of the GBM microenvironment to enhance the selectivity for tumor targeting. This project identified analogues that showed selectivity at killi","dates":{"release":"2024-01-01T00:00:00Z","publication":"2024 Sep","modification":"2026-06-01T15:57:04.394Z","creation":"2026-04-08T13:57:21.764Z"},"accession":"S-EPMC11646455","cross_references":{"pubmed":["38942129"],"doi":["10.1016/j.bmcl.2024.129863"]}}