http://purl.uniprot.org/citations/19505953 | http://www.w3.org/1999/02/22-rdf-syntax-ns#type | http://purl.uniprot.org/core/Journal_Citation |
http://purl.uniprot.org/citations/19505953 | http://www.w3.org/2000/01/rdf-schema#comment | "ELOVL6, a member of the elongation of very long-chain fatty acids (ELOVL) family, has recently been identified as the rate-limiting enzyme for the elongation of palmitoyl-CoA. ELOVL6 deficient mice are protected from high-fat diet induced insulin resistance, suggesting that ELOVL6 might be a promising target for the treatment of metabolic disorders. Despite the increasing interest in Elovl6 as a therapeutic target, the lack of chemical tools for this enzyme has limited further elucidation of the biochemical and pharmacological properties of ELOVL6. We have identified Compound-A, a potent inhibitor for ELOVL6, by screening our company library and subsequently optimizing hit compounds. Compound-A potently inhibited human and mouse ELOVL6 and displayed >100-fold greater selectivity for ELOVL6 over other ELOVL family members. Consistent with its potent and selective inhibitory activity toward ELOVL6, [(3)H]Compound-A bound to ELOVL6 with high affinity while showing no specific binding to other ELOVL enzymes. The observation that [(3)H]Compound-A bound to ELOVL6 in a palmitoyl-CoA-dependent manner in the absence of malonyl-CoA and NADPH suggests that Compound-A might recognize an enzyme-substrate complex, e.g. an acyl-enzyme intermediate. Collectively, these observations demonstrate that Compound-A and its tritiated form are useful tools for biochemical and pharmacological characterization of ELOVL6."xsd:string |
http://purl.uniprot.org/citations/19505953 | http://purl.org/dc/terms/identifier | "doi:10.1093/jb/mvp088"xsd:string |
http://purl.uniprot.org/citations/19505953 | http://purl.uniprot.org/core/author | "Nagase T."xsd:string |
http://purl.uniprot.org/citations/19505953 | http://purl.uniprot.org/core/author | "Sato N."xsd:string |
http://purl.uniprot.org/citations/19505953 | http://purl.uniprot.org/core/author | "Takahashi H."xsd:string |
http://purl.uniprot.org/citations/19505953 | http://purl.uniprot.org/core/author | "Tang C."xsd:string |
http://purl.uniprot.org/citations/19505953 | http://purl.uniprot.org/core/author | "Dean D."xsd:string |
http://purl.uniprot.org/citations/19505953 | http://purl.uniprot.org/core/author | "Kitazawa H."xsd:string |
http://purl.uniprot.org/citations/19505953 | http://purl.uniprot.org/core/author | "Miyamoto Y."xsd:string |
http://purl.uniprot.org/citations/19505953 | http://purl.uniprot.org/core/author | "Shimamura K."xsd:string |
http://purl.uniprot.org/citations/19505953 | http://purl.uniprot.org/core/author | "Nagumo A."xsd:string |
http://purl.uniprot.org/citations/19505953 | http://purl.uniprot.org/core/author | "Tokita S."xsd:string |
http://purl.uniprot.org/citations/19505953 | http://purl.uniprot.org/core/date | "2009"xsd:gYear |
http://purl.uniprot.org/citations/19505953 | http://purl.uniprot.org/core/name | "J Biochem"xsd:string |
http://purl.uniprot.org/citations/19505953 | http://purl.uniprot.org/core/pages | "429-437"xsd:string |
http://purl.uniprot.org/citations/19505953 | http://purl.uniprot.org/core/title | "Identification and characterization of a selective radioligand for ELOVL6."xsd:string |
http://purl.uniprot.org/citations/19505953 | http://purl.uniprot.org/core/volume | "146"xsd:string |
http://purl.uniprot.org/citations/19505953 | http://www.w3.org/2004/02/skos/core#exactMatch | http://purl.uniprot.org/pubmed/19505953 |
http://purl.uniprot.org/citations/19505953 | http://xmlns.com/foaf/0.1/primaryTopicOf | https://pubmed.ncbi.nlm.nih.gov/19505953 |
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http://purl.uniprot.org/uniprot/#_Q9HB03-mappedCitation-19505953 | http://www.w3.org/1999/02/22-rdf-syntax-ns#object | http://purl.uniprot.org/citations/19505953 |
http://purl.uniprot.org/uniprot/A1L3X0 | http://purl.uniprot.org/core/mappedCitation | http://purl.uniprot.org/citations/19505953 |
http://purl.uniprot.org/uniprot/Q9HB03 | http://purl.uniprot.org/core/mappedCitation | http://purl.uniprot.org/citations/19505953 |