| http://purl.uniprot.org/citations/26221874 | http://www.w3.org/1999/02/22-rdf-syntax-ns#type | http://purl.uniprot.org/core/Journal_Citation |
| http://purl.uniprot.org/citations/26221874 | http://www.w3.org/2000/01/rdf-schema#comment | "Human tumors exhibit increased glucose uptake and metabolism as a result of high demand for ATP and anabolic substrates and this metabolotype is a negative prognostic indicator for survival. Recent studies have demonstrated that cancer cells from several tissue origins and genetic backgrounds require the expression of 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase 4 (PFKFB4), a regulatory enzyme that synthesizes an allosteric activator of glycolysis, fructose-2,6-bisphosphate. We report the discovery of a first-in-class PFKFB4 inhibitor, 5-(n-(8-methoxy-4-quinolyl)amino)pentyl nitrate (5MPN), using structure-based virtual computational screening. We find that 5MPN is a selective inhibitor of PFKFB4 that suppresses the glycolysis and proliferation of multiple human cancer cell lines but not non-transformed epithelial cells in vitro. Importantly, 5MPN has high oral bioavailability and per os administration of a non-toxic dose of 5MPN suppresses the glucose metabolism and growth of tumors in mice."xsd:string |
| http://purl.uniprot.org/citations/26221874 | http://purl.org/dc/terms/identifier | "doi:10.18632/oncotarget.4534"xsd:string |
| http://purl.uniprot.org/citations/26221874 | http://purl.uniprot.org/core/author | "Clark J."xsd:string |
| http://purl.uniprot.org/citations/26221874 | http://purl.uniprot.org/core/author | "Trent J.O."xsd:string |
| http://purl.uniprot.org/citations/26221874 | http://purl.uniprot.org/core/author | "Chesney J."xsd:string |
| http://purl.uniprot.org/citations/26221874 | http://purl.uniprot.org/core/author | "Telang S."xsd:string |
| http://purl.uniprot.org/citations/26221874 | http://purl.uniprot.org/core/author | "Lanceta L."xsd:string |
| http://purl.uniprot.org/citations/26221874 | http://purl.uniprot.org/core/date | "2015"xsd:gYear |
| http://purl.uniprot.org/citations/26221874 | http://purl.uniprot.org/core/name | "Oncotarget"xsd:string |
| http://purl.uniprot.org/citations/26221874 | http://purl.uniprot.org/core/pages | "18001-18011"xsd:string |
| http://purl.uniprot.org/citations/26221874 | http://purl.uniprot.org/core/title | "Targeting the sugar metabolism of tumors with a first-in-class 6-phosphofructo-2-kinase (PFKFB4) inhibitor."xsd:string |
| http://purl.uniprot.org/citations/26221874 | http://purl.uniprot.org/core/volume | "6"xsd:string |
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