http://rdf.ncbi.nlm.nih.gov/pubchem/patent/US-2005049309-A1
Outgoing Links
| Predicate | Object |
|---|---|
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-66 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-195 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-66 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C12N- |
| filingDate | 2004-07-14-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_0e76e72af61204a86714ab6a0e04aed4 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_75ed3d9899c569b0cf614333ba1033f7 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_4b2d00a4918ea6306d77eab69365ebe0 |
| publicationDate | 2005-03-03-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | US-2005049309-A1 |
| titleOfInvention | Regulation of HIF protein levels via deubiquitination pathway |
| abstract | The hypoxia inducible factor-1 (HIF-1) transcription factor is an important regulator of the cellular response to hypoxia. The activity of HIF-1 is regulated by the level of the HIF-1α subunit, HIF-1α, which is rapidly degraded under normoxic conditions by the ubiquitin-proteasome pathway. HIF-1α levels increase under hypoxic conditions. Many human cancers also show constitutively increased HIF-1α levels. PX-478 or S-2-amino-3-[4′-N,N,-bis(2-chloroethyl)amino]phenyl propionic acid N-oxide dihydrochloride, is a novel anticancer agent, and is capably of decreasing both constitutive and hypoxia induced HIF-1α protein levels and HIF-1 transactivation in vitro and in vivo. In method embodiments, the administration of PX-478 is independent of the pathways of HIF-1α regulation involving the von Hippel-Lindau protein and p53. PX-478 causes an increase in polyubiquitinated HIF-1α levels due to inhibition of HIF-1α deubiquitination. The levels of other proteins whose proteasomal breakdown is mediated by ubiquitination are not affected by PX-478. Deubiquitination is a novel pathway for the regulation of cellular HIF-1α levels and PX-478 is a specific inhibitor of the pathway. Therapeutic compounds for regulating cellular HIF-1α levels and methods of regulating cellular HIF-1α levels are herein provided. |
| isCitedBy | http://rdf.ncbi.nlm.nih.gov/pubchem/patent/US-2013064857-A1 http://rdf.ncbi.nlm.nih.gov/pubchem/patent/WO-2009102960-A1 http://rdf.ncbi.nlm.nih.gov/pubchem/patent/US-11225660-B2 http://rdf.ncbi.nlm.nih.gov/pubchem/patent/WO-2010005527-A1 http://rdf.ncbi.nlm.nih.gov/pubchem/patent/US-10308943-B2 |
| priorityDate | 2003-07-14-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 359.