FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2012310412> ?p ?o ?g. }

• W2012310412 endingPage "4141" @default.
• W2012310412 startingPage "4131" @default.
• W2012310412 abstract "Analogues of a novel class of template-competitive reverse transcriptase inhibitors (Li, K.; Lin, W.; Chong, K. H.; Moore, B. M.; Doughty, M. B. Bioorg. Med. Chem. 2002, 10, 507) were analyzed as photoprobes of HIV-1 reverse transcriptase (RT) heterodimer. The two photoprobes, 2-(4-azidophenacyl)thio-1,N6-etheno-2′-deoxyadenosine 5′-triphosphate 2 and the tetrafluoro analogue 2-(4-azido-2,3,5,6-tetrafluorophenacyl)thio-1,N6-etheno-2′-deoxyadenosine 5′-triphosphate 3, photodecomposed at 3500 Å with half-lives of 4.0 and 2.5 min, respectively. Analysis of the photoproducts of 2m demonstrated that the etheno group is stable but the azido decomposes primarily to the 2-(S-[3H-diazepinon-4-yl]thio)-1,N6-etheno-dAMP. Photolysis of both 2 and 3 with RT resulted in a time-dependent loss of activity, with maximum inactivation of 83 and 60%, respectively. Both 2 and 3 showed concentration-dependent photoinactivation of RT in the concentration range from 0 to 100 μM, with EC50s of 20 and 25 μM and maximum inactivation of 80 and 60%, respectively. Both the time and concentration dependent photoinactivation were strongly protected by template-primer, but only poorly inhibited by even high concentrations of TTP. Radiolabeled analogues [β,γ-32P]-2 and [β,γ-32P]-3 photoincorporated into the p66 subunit, an incorporation also protected by template primer. Identification of the site of incorporation was problematic for both photoprobes, but evidence presented is consistent with labeling sites for the phenacyl side chains of both 2 and 3 in the template grip. Nevertheless, the photoinactivation and incorporation data are consistent with our earlier conclusions from the kinetic data that these inhibitors are specific for the free form of RT in competition with template/primer, and thus represent a novel class of inhibitors." @default.
• W2012310412 created "2016-06-24" @default.
• W2012310412 creator A5017100408 @default.
• W2012310412 creator A5085433059 @default.
• W2012310412 creator A5088610360 @default.
• W2012310412 date "2002-12-01" @default.
• W2012310412 modified "2023-09-23" @default.
• W2012310412 title "Characterization of a Binding Site for Template Competitive Inhibitors of HIV-1 Reverse Transcriptase Using Photolabeling Derivatives" @default.
• W2012310412 cites W1594741329 @default.
• W2012310412 cites W1595932863 @default.
• W2012310412 cites W1973711348 @default.
• W2012310412 cites W1977955181 @default.
• W2012310412 cites W1984814223 @default.
• W2012310412 cites W1993061861 @default.
• W2012310412 cites W2003302824 @default.
• W2012310412 cites W2008002971 @default.
• W2012310412 cites W2008954911 @default.
• W2012310412 cites W2009581957 @default.
• W2012310412 cites W2011153626 @default.
• W2012310412 cites W2012867384 @default.
• W2012310412 cites W2019779254 @default.
• W2012310412 cites W2038650498 @default.
• W2012310412 cites W2040252184 @default.
• W2012310412 cites W2051254475 @default.
• W2012310412 cites W2052060136 @default.
• W2012310412 cites W2059002340 @default.
• W2012310412 cites W2069815958 @default.
• W2012310412 cites W2076284523 @default.
• W2012310412 cites W2079727617 @default.
• W2012310412 cites W2095725835 @default.
• W2012310412 cites W2951646711 @default.
• W2012310412 doi "https://doi.org/10.1016/s0968-0896(02)00259-6" @default.
• W2012310412 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/12413867" @default.
• W2012310412 hasPublicationYear "2002" @default.
• W2012310412 type Work @default.
• W2012310412 sameAs 2012310412 @default.
• W2012310412 citedByCount "7" @default.
• W2012310412 countsByYear W20123104122012 @default.
• W2012310412 countsByYear W20123104122013 @default.
• W2012310412 crossrefType "journal-article" @default.
• W2012310412 hasAuthorship W2012310412A5017100408 @default.
• W2012310412 hasAuthorship W2012310412A5085433059 @default.
• W2012310412 hasAuthorship W2012310412A5088610360 @default.
• W2012310412 hasConcept C104292427 @default.
• W2012310412 hasConcept C104317684 @default.
• W2012310412 hasConcept C107824862 @default.
• W2012310412 hasConcept C131140672 @default.
• W2012310412 hasConcept C156719811 @default.
• W2012310412 hasConcept C181199279 @default.
• W2012310412 hasConcept C185592680 @default.
• W2012310412 hasConcept C2780636463 @default.
• W2012310412 hasConcept C2781253882 @default.
• W2012310412 hasConcept C55493867 @default.
• W2012310412 hasConcept C67705224 @default.
• W2012310412 hasConcept C71240020 @default.
• W2012310412 hasConcept C82381507 @default.
• W2012310412 hasConceptScore W2012310412C104292427 @default.
• W2012310412 hasConceptScore W2012310412C104317684 @default.
• W2012310412 hasConceptScore W2012310412C107824862 @default.
• W2012310412 hasConceptScore W2012310412C131140672 @default.
• W2012310412 hasConceptScore W2012310412C156719811 @default.
• W2012310412 hasConceptScore W2012310412C181199279 @default.
• W2012310412 hasConceptScore W2012310412C185592680 @default.
• W2012310412 hasConceptScore W2012310412C2780636463 @default.
• W2012310412 hasConceptScore W2012310412C2781253882 @default.
• W2012310412 hasConceptScore W2012310412C55493867 @default.
• W2012310412 hasConceptScore W2012310412C67705224 @default.
• W2012310412 hasConceptScore W2012310412C71240020 @default.
• W2012310412 hasConceptScore W2012310412C82381507 @default.
• W2012310412 hasIssue "12" @default.
• W2012310412 hasLocation W20123104121 @default.
• W2012310412 hasLocation W20123104122 @default.
• W2012310412 hasOpenAccess W2012310412 @default.
• W2012310412 hasPrimaryLocation W20123104121 @default.
• W2012310412 hasRelatedWork W1975161429 @default.
• W2012310412 hasRelatedWork W2012310412 @default.
• W2012310412 hasRelatedWork W2057847316 @default.
• W2012310412 hasRelatedWork W2062456979 @default.
• W2012310412 hasRelatedWork W2066883758 @default.
• W2012310412 hasRelatedWork W2074320902 @default.
• W2012310412 hasRelatedWork W2079727617 @default.
• W2012310412 hasRelatedWork W2089118919 @default.
• W2012310412 hasRelatedWork W2137420965 @default.
• W2012310412 hasRelatedWork W4241923112 @default.
• W2012310412 hasVolume "10" @default.
• W2012310412 isParatext "false" @default.
• W2012310412 isRetracted "false" @default.
• W2012310412 magId "2012310412" @default.
• W2012310412 workType "article" @default.