{"database":"biostudies-literature","file_versions":[],"scores":null,"additional":{"submitter":["Patwardhan CA"],"funding":["NIGMS NIH HHS"],"pagination":["223-9"],"full_dataset_link":["https://www.ebi.ac.uk/biostudies/studies/S-EPMC4836055"],"repository":["biostudies-literature"],"omics_type":["Unknown"],"volume":["20(2)"],"pubmed_abstract":["Hsp90 and its co-chaperones are known to be important for cancer cell survival. The N-terminal inhibitors of Hsp90 that are in ongoing clinical trials as antitumor agents have unfortunately shown disappointing efficacies in the clinic. Thus, novel inhibitors of the Hsp90 machine with a different mechanism of action are urgently needed. We report here the development of a novel high-throughput screening assay platform to identify small-molecule inhibitors of Hsp90 and its co-chaperones. This assay quantitatively measures the ability of Hsp90 and its co-chaperones to refold/protect the progesterone receptor, a physiological client of Hsp90, in a 96-well plate format. We screened the National Institutes of Health clinical collection drug library and identified capsaicin as a hit molecule. Cap"],"journal":["Journal of biomolecular screening"],"pubmed_title":["Progesterone receptor chaperone complex-based high-throughput screening assay: identification of capsaicin as an inhibitor of the Hsp90 machine."],"pmcid":["PMC4836055"],"funding_grant_id":["R01 GM102443","GM102443-01"],"pubmed_authors":["Patwardhan CA","Chadli A","Alfa E","Lu S"],"additional_accession":[]},"is_claimable":false,"name":"Progesterone receptor chaperone complex-based high-throughput screening assay: identification of capsaicin as an inhibitor of the Hsp90 machine.","description":"Hsp90 and its co-chaperones are known to be important for cancer cell survival. The N-terminal inhibitors of Hsp90 that are in ongoing clinical trials as antitumor agents have unfortunately shown disappointing efficacies in the clinic. Thus, novel inhibitors of the Hsp90 machine with a different mechanism of action are urgently needed. We report here the development of a novel high-throughput screening assay platform to identify small-molecule inhibitors of Hsp90 and its co-chaperones. This assay quantitatively measures the ability of Hsp90 and its co-chaperones to refold/protect the progesterone receptor, a physiological client of Hsp90, in a 96-well plate format. We screened the National Institutes of Health clinical collection drug library and identified capsaicin as a hit molecule. Cap","dates":{"release":"2015-01-01T00:00:00Z","publication":"2015 Feb","modification":"2025-04-04T11:40:58.784Z","creation":"2019-03-27T02:11:53Z"},"accession":"S-EPMC4836055","cross_references":{"pubmed":["25184514"],"doi":["10.1177/1087057114549147"]}}