{"database":"biostudies-literature","file_versions":[],"scores":null,"additional":{"submitter":["Gopinath P"],"funding":["Ministry of Science,Technology and space"],"pagination":["7079-7086"],"full_dataset_link":["https://www.ebi.ac.uk/biostudies/studies/S-EPMC5355956"],"repository":["biostudies-literature"],"omics_type":["Unknown"],"volume":["7(12)"],"pubmed_abstract":["Recent studies have suggested that selective targeting of overexpressed enzymes in cancer cells by small molecules that induce the formation of reactive oxygen species (ROS) could be a viable approach in cancer therapy. One such example is the inactivation of ubiquitin specific protease-2 (USP2)-an emerging drug target to combat prostate cancer-by β-lapachone, which has been identified to involve oxidation of the catalytic cysteine's thiol residue to sulfinic acid. A rational design of β-lapachone analogs with improved activity requires a much better understanding of the variables that determine ROS production by this class of molecules. This crucial aspect was addressed <i>via</i> modulation of its 1,2-naphthoquinone scaffold and establishment of a structure/activity relationship, regardi"],"journal":["Chemical science"],"pubmed_title":["Understanding and predicting the potency of ROS-based enzyme inhibitors, exemplified by naphthoquinones and ubiquitin specific protease-2."],"pmcid":["PMC5355956"],"funding_grant_id":["2021900"],"pubmed_authors":["Brik A","Gopinath P","Mahammed A","Ohayon S","Gross Z"],"additional_accession":[]},"is_claimable":false,"name":"Understanding and predicting the potency of ROS-based enzyme inhibitors, exemplified by naphthoquinones and ubiquitin specific protease-2.","description":"Recent studies have suggested that selective targeting of overexpressed enzymes in cancer cells by small molecules that induce the formation of reactive oxygen species (ROS) could be a viable approach in cancer therapy. One such example is the inactivation of ubiquitin specific protease-2 (USP2)-an emerging drug target to combat prostate cancer-by β-lapachone, which has been identified to involve oxidation of the catalytic cysteine's thiol residue to sulfinic acid. A rational design of β-lapachone analogs with improved activity requires a much better understanding of the variables that determine ROS production by this class of molecules. This crucial aspect was addressed <i>via</i> modulation of its 1,2-naphthoquinone scaffold and establishment of a structure/activity relationship, regardi","dates":{"release":"2016-01-01T00:00:00Z","publication":"2016 Dec","modification":"2025-05-29T19:21:15.2Z","creation":"2025-05-29T19:21:15.2Z"},"accession":"S-EPMC5355956","cross_references":{"pubmed":["28451143"],"doi":["10.1039/c6sc02758j"]}}