| http://purl.uniprot.org/citations/23540839 | http://www.w3.org/1999/02/22-rdf-syntax-ns#type | http://purl.uniprot.org/core/Journal_Citation |
| http://purl.uniprot.org/citations/23540839 | http://www.w3.org/2000/01/rdf-schema#comment | "The fragment indole-6-carboxylic acid (1F1), previously identified as a flap site binder in a fragment-based screen against HIV protease (PR), has been cocrystallized with pepstatin-inhibited PR and with apo-PR. Another fragment, 3-indolepropionic acid (1F1-N), predicted by AutoDock calculations and confirmed in a novel inhibition of nucleation crystallization assay, exploits the same interactions in the flap site in two crystal structures. Both 1F1 and 1F1-N bind to the closed form of apo-PR and to pepstatin:PR. In solution, 1F1 and 1F1-N raise the Tm of apo-PR by 3.5-5 °C as assayed by differential scanning fluorimetry (DSF) and show equivalent low-micromolar binding constants to both apo-PR and pepstatin:PR, assayed by backscattering interferometry (BSI). The observed signal intensities in BSI are greater for each fragment upon binding to apo-PR than to pepstatin-bound PR, consistent with greater conformational change in the former binding event. Together, these data indicate that fragment binding in the flap site favors a closed conformation of HIV PR."xsd:string |
| http://purl.uniprot.org/citations/23540839 | http://purl.org/dc/terms/identifier | "doi:10.1021/cb300611p"xsd:string |
| http://purl.uniprot.org/citations/23540839 | http://purl.uniprot.org/core/author | "Finn M.G."xsd:string |
| http://purl.uniprot.org/citations/23540839 | http://purl.uniprot.org/core/author | "Lin Y.C."xsd:string |
| http://purl.uniprot.org/citations/23540839 | http://purl.uniprot.org/core/author | "Olson A.J."xsd:string |
| http://purl.uniprot.org/citations/23540839 | http://purl.uniprot.org/core/author | "Elder J.H."xsd:string |
| http://purl.uniprot.org/citations/23540839 | http://purl.uniprot.org/core/author | "Stout C.D."xsd:string |
| http://purl.uniprot.org/citations/23540839 | http://purl.uniprot.org/core/author | "Chang M.W."xsd:string |
| http://purl.uniprot.org/citations/23540839 | http://purl.uniprot.org/core/author | "Rhee J.K."xsd:string |
| http://purl.uniprot.org/citations/23540839 | http://purl.uniprot.org/core/author | "Forli S."xsd:string |
| http://purl.uniprot.org/citations/23540839 | http://purl.uniprot.org/core/author | "Baksh M.M."xsd:string |
| http://purl.uniprot.org/citations/23540839 | http://purl.uniprot.org/core/author | "Torbett B.E."xsd:string |
| http://purl.uniprot.org/citations/23540839 | http://purl.uniprot.org/core/author | "Tiefenbrunn T."xsd:string |
| http://purl.uniprot.org/citations/23540839 | http://purl.uniprot.org/core/author | "Perryman A.L."xsd:string |
| http://purl.uniprot.org/citations/23540839 | http://purl.uniprot.org/core/author | "Happer M."xsd:string |
| http://purl.uniprot.org/citations/23540839 | http://purl.uniprot.org/core/date | "2013"xsd:gYear |
| http://purl.uniprot.org/citations/23540839 | http://purl.uniprot.org/core/name | "ACS Chem Biol"xsd:string |
| http://purl.uniprot.org/citations/23540839 | http://purl.uniprot.org/core/pages | "1223-1231"xsd:string |
| http://purl.uniprot.org/citations/23540839 | http://purl.uniprot.org/core/title | "Small molecule regulation of protein conformation by binding in the Flap of HIV protease."xsd:string |
| http://purl.uniprot.org/citations/23540839 | http://purl.uniprot.org/core/volume | "8"xsd:string |
| http://purl.uniprot.org/citations/23540839 | http://www.w3.org/2004/02/skos/core#exactMatch | http://purl.uniprot.org/pubmed/23540839 |
| http://purl.uniprot.org/citations/23540839 | http://xmlns.com/foaf/0.1/primaryTopicOf | https://pubmed.ncbi.nlm.nih.gov/23540839 |
| http://purl.uniprot.org/uniprot/#_P12499-mappedCitation-23540839 | http://www.w3.org/1999/02/22-rdf-syntax-ns#object | http://purl.uniprot.org/citations/23540839 |
| http://purl.uniprot.org/uniprot/P12499 | http://purl.uniprot.org/core/mappedCitation | http://purl.uniprot.org/citations/23540839 |