| http://purl.uniprot.org/citations/20937817 | http://www.w3.org/1999/02/22-rdf-syntax-ns#type | http://purl.uniprot.org/core/Journal_Citation |
| http://purl.uniprot.org/citations/20937817 | http://www.w3.org/2000/01/rdf-schema#comment | "Chemical genetics is an emerging approach to investigate the biology of host-pathogen interactions. We screened several inhibitors of ATP-dependent DNA motors and detected the gyrase B inhibitor coumermycin A1 (C-A1) as a potent antiretroviral. C-A1 inhibited HIV-1 integration and gene expression from acutely infected cell, but the two activities mapped to distinct targets. Target discovery identified Hsp90 as the C-A1 target affecting viral gene expression. Chromatin immunoprecipitation revealed that Hsp90 associates with the viral promoter and may directly regulate gene expression. Molecular docking suggested that C-A1 binds to two novel pockets at the C terminal domain of Hsp90. C-A1 inhibited Hsp90 dimer formation, suggesting that it impairs viral gene expression by preventing Hsp90 dimerization at the C terminus. The inhibition of HIV-1 integration imposed by C-A1 was independent of Hsp90 and mapped to the capsid protein, and a point mutation at residue 105 made the virus resistant to this block. HIV-1 susceptibility to the integration block mediated by C-A1 was influenced by cyclophilin A. Our chemical genetic approach revealed an unexpected function of capsid in HIV-1 integration and provided evidence for a role of Hsp90 in regulating gene expression in mammalian cells. Both activities were amenable to inhibition by small molecules and represent novel antiretroviral drug targets."xsd:string |
| http://purl.uniprot.org/citations/20937817 | http://purl.org/dc/terms/identifier | "doi:10.1074/jbc.m110.155275"xsd:string |
| http://purl.uniprot.org/citations/20937817 | http://purl.uniprot.org/core/author | "Anderson I."xsd:string |
| http://purl.uniprot.org/citations/20937817 | http://purl.uniprot.org/core/author | "Zhou L."xsd:string |
| http://purl.uniprot.org/citations/20937817 | http://purl.uniprot.org/core/author | "Nyakatura E."xsd:string |
| http://purl.uniprot.org/citations/20937817 | http://purl.uniprot.org/core/author | "Jenner R.G."xsd:string |
| http://purl.uniprot.org/citations/20937817 | http://purl.uniprot.org/core/author | "Loh B."xsd:string |
| http://purl.uniprot.org/citations/20937817 | http://purl.uniprot.org/core/author | "Selwood D."xsd:string |
| http://purl.uniprot.org/citations/20937817 | http://purl.uniprot.org/core/author | "Fassati A."xsd:string |
| http://purl.uniprot.org/citations/20937817 | http://purl.uniprot.org/core/author | "Gane P.J."xsd:string |
| http://purl.uniprot.org/citations/20937817 | http://purl.uniprot.org/core/author | "Tribak M."xsd:string |
| http://purl.uniprot.org/citations/20937817 | http://purl.uniprot.org/core/author | "Vozzolo L."xsd:string |
| http://purl.uniprot.org/citations/20937817 | http://purl.uniprot.org/core/date | "2010"xsd:gYear |
| http://purl.uniprot.org/citations/20937817 | http://purl.uniprot.org/core/name | "J Biol Chem"xsd:string |
| http://purl.uniprot.org/citations/20937817 | http://purl.uniprot.org/core/pages | "39314-39328"xsd:string |
| http://purl.uniprot.org/citations/20937817 | http://purl.uniprot.org/core/title | "Gyrase B inhibitor impairs HIV-1 replication by targeting Hsp90 and the capsid protein."xsd:string |
| http://purl.uniprot.org/citations/20937817 | http://purl.uniprot.org/core/volume | "285"xsd:string |
| http://purl.uniprot.org/citations/20937817 | http://www.w3.org/2004/02/skos/core#exactMatch | http://purl.uniprot.org/pubmed/20937817 |
| http://purl.uniprot.org/citations/20937817 | http://xmlns.com/foaf/0.1/primaryTopicOf | https://pubmed.ncbi.nlm.nih.gov/20937817 |
| http://purl.uniprot.org/uniprot/#_A0A288CG13-mappedCitation-20937817 | http://www.w3.org/1999/02/22-rdf-syntax-ns#object | http://purl.uniprot.org/citations/20937817 |
| http://purl.uniprot.org/uniprot/#_B4DTA5-mappedCitation-20937817 | http://www.w3.org/1999/02/22-rdf-syntax-ns#object | http://purl.uniprot.org/citations/20937817 |
| http://purl.uniprot.org/uniprot/#_K9JA46-mappedCitation-20937817 | http://www.w3.org/1999/02/22-rdf-syntax-ns#object | http://purl.uniprot.org/citations/20937817 |
| http://purl.uniprot.org/uniprot/#_Q2VPJ6-mappedCitation-20937817 | http://www.w3.org/1999/02/22-rdf-syntax-ns#object | http://purl.uniprot.org/citations/20937817 |
| http://purl.uniprot.org/uniprot/#_Q86U12-mappedCitation-20937817 | http://www.w3.org/1999/02/22-rdf-syntax-ns#object | http://purl.uniprot.org/citations/20937817 |