| http://purl.uniprot.org/citations/32142284 | http://www.w3.org/1999/02/22-rdf-syntax-ns#type | http://purl.uniprot.org/core/Journal_Citation |
| http://purl.uniprot.org/citations/32142284 | http://www.w3.org/2000/01/rdf-schema#comment | "Deoxyhypusine synthase (DHPS) utilizes spermidine and NAD as cofactors to incorporate a hypusine modification into the eukaryotic translation initiation factor 5A (eIF5A). Hypusine is essential for eIF5A activation, which, in turn, plays a key role in regulating protein translation of selected mRNA that are associated with the synthesis of oncoproteins, thereby enhancing tumor cell proliferation. Therefore, inhibition of DHPS is a promising therapeutic option for the treatment of cancer. To discover novel lead compounds that target DHPS, we conducted synthetic studies with a hit obtained via high-throughput screening. Optimization of the ring structures of the amide compound (2) led to bromobenzothiophene (11g) with potent inhibitory activity against DHPS. X-ray crystallographic analysis of 11g complexed with DHPS revealed a dramatic conformational change in DHPS, which suggests the presence of a novel allosteric site. These findings provide the basis for the development of novel therapy distinct from spermidine mimetic inhibitors."xsd:string |
| http://purl.uniprot.org/citations/32142284 | http://purl.org/dc/terms/identifier | "doi:10.1021/acs.jmedchem.9b01979"xsd:string |
| http://purl.uniprot.org/citations/32142284 | http://purl.uniprot.org/core/author | "Ogawa K."xsd:string |
| http://purl.uniprot.org/citations/32142284 | http://purl.uniprot.org/core/author | "Kimura H."xsd:string |
| http://purl.uniprot.org/citations/32142284 | http://purl.uniprot.org/core/author | "Ono K."xsd:string |
| http://purl.uniprot.org/citations/32142284 | http://purl.uniprot.org/core/author | "Tanaka Y."xsd:string |
| http://purl.uniprot.org/citations/32142284 | http://purl.uniprot.org/core/author | "Matsumoto S."xsd:string |
| http://purl.uniprot.org/citations/32142284 | http://purl.uniprot.org/core/author | "Klein M.G."xsd:string |
| http://purl.uniprot.org/citations/32142284 | http://purl.uniprot.org/core/author | "Yokota A."xsd:string |
| http://purl.uniprot.org/citations/32142284 | http://purl.uniprot.org/core/author | "Imamura S."xsd:string |
| http://purl.uniprot.org/citations/32142284 | http://purl.uniprot.org/core/author | "Uchiyama N."xsd:string |
| http://purl.uniprot.org/citations/32142284 | http://purl.uniprot.org/core/author | "Morishita D."xsd:string |
| http://purl.uniprot.org/citations/32142284 | http://purl.uniprot.org/core/author | "Kitazawa S."xsd:string |
| http://purl.uniprot.org/citations/32142284 | http://purl.uniprot.org/core/author | "Saito B."xsd:string |
| http://purl.uniprot.org/citations/32142284 | http://purl.uniprot.org/core/author | "Ambrus-Aikelin G."xsd:string |
| http://purl.uniprot.org/citations/32142284 | http://purl.uniprot.org/core/author | "Okaniwa M."xsd:string |
| http://purl.uniprot.org/citations/32142284 | http://purl.uniprot.org/core/author | "Kurasawa O."xsd:string |
| http://purl.uniprot.org/citations/32142284 | http://purl.uniprot.org/core/date | "2020"xsd:gYear |
| http://purl.uniprot.org/citations/32142284 | http://purl.uniprot.org/core/name | "J Med Chem"xsd:string |
| http://purl.uniprot.org/citations/32142284 | http://purl.uniprot.org/core/pages | "3215-3226"xsd:string |
| http://purl.uniprot.org/citations/32142284 | http://purl.uniprot.org/core/title | "Discovery of Novel Allosteric Inhibitors of Deoxyhypusine Synthase."xsd:string |
| http://purl.uniprot.org/citations/32142284 | http://purl.uniprot.org/core/volume | "63"xsd:string |
| http://purl.uniprot.org/citations/32142284 | http://www.w3.org/2004/02/skos/core#exactMatch | http://purl.uniprot.org/pubmed/32142284 |
| http://purl.uniprot.org/citations/32142284 | http://xmlns.com/foaf/0.1/primaryTopicOf | https://pubmed.ncbi.nlm.nih.gov/32142284 |