| http://purl.uniprot.org/citations/12848532 | http://www.w3.org/1999/02/22-rdf-syntax-ns#type | http://purl.uniprot.org/core/Journal_Citation |
| http://purl.uniprot.org/citations/12848532 | http://www.w3.org/2000/01/rdf-schema#comment | "Small molecule microarrays were screened to identify a small molecule ligand for Hap3p, a subunit of the yeast Hap2/3/4/5p transcription factor complex. The compound, named haptamide A, was determined to have a KD of 5.03 muM for binding to Hap3p using surface plasmon resonance analysis. Haptamide A also inhibited activation of a GDH1-lacZ reporter gene in a dose-dependent fashion. To explore structure-activity relationships, 11 derivatives of haptamide A were prepared using the same synthetic route that was developed for the original library synthesis. Analysis of dissociation constants and IC50 values for the reporter gene assay revealed a more potent inhibitor, haptamide B, with a KD of 330 nM. Whole-genome transcriptional profiling was used to compare effects of haptamide B with a hap3Delta yeast strain. Treatment with haptamide B, like the deletion mutant, reduced lactate-induced transcription of several genes from wild-type levels. Profiling the genetic "knockout" and the chemical genetic "knockdown" led to the identification of several genes that are regulated by Hap3p under nonfermentative conditions. These results demonstrate that a small molecule discovered using the small molecule microarray binding assay can permeate yeast cells and reach its target transcription factor protein in cells."xsd:string |
| http://purl.uniprot.org/citations/12848532 | http://purl.org/dc/terms/identifier | "doi:10.1021/ja0352698"xsd:string |
| http://purl.uniprot.org/citations/12848532 | http://purl.uniprot.org/core/author | "Schreiber S.L."xsd:string |
| http://purl.uniprot.org/citations/12848532 | http://purl.uniprot.org/core/author | "Shamji A.F."xsd:string |
| http://purl.uniprot.org/citations/12848532 | http://purl.uniprot.org/core/author | "Koehler A.N."xsd:string |
| http://purl.uniprot.org/citations/12848532 | http://purl.uniprot.org/core/date | "2003"xsd:gYear |
| http://purl.uniprot.org/citations/12848532 | http://purl.uniprot.org/core/name | "J Am Chem Soc"xsd:string |
| http://purl.uniprot.org/citations/12848532 | http://purl.uniprot.org/core/pages | "8420-8421"xsd:string |
| http://purl.uniprot.org/citations/12848532 | http://purl.uniprot.org/core/title | "Discovery of an inhibitor of a transcription factor using small molecule microarrays and diversity-oriented synthesis."xsd:string |
| http://purl.uniprot.org/citations/12848532 | http://purl.uniprot.org/core/volume | "125"xsd:string |
| http://purl.uniprot.org/citations/12848532 | http://www.w3.org/2004/02/skos/core#exactMatch | http://purl.uniprot.org/pubmed/12848532 |
| http://purl.uniprot.org/citations/12848532 | http://xmlns.com/foaf/0.1/primaryTopicOf | https://pubmed.ncbi.nlm.nih.gov/12848532 |
| http://purl.uniprot.org/uniprot/#_P13434-mappedCitation-12848532 | http://www.w3.org/1999/02/22-rdf-syntax-ns#object | http://purl.uniprot.org/citations/12848532 |
| http://purl.uniprot.org/uniprot/P13434 | http://purl.uniprot.org/core/mappedCitation | http://purl.uniprot.org/citations/12848532 |