http://rdf.ncbi.nlm.nih.gov/pubchem/patent/US-8202886-B2
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_b3127c0ebee3f865b211b019fac84286 http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_7eac85b57e6fe8ea4f3de6b635859314 http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_b1d71f19fb313aa3892d91f0a3567133 http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_59c6a921f33fe0adc58c2b6177184515 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D215-26 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-4709 |
| filingDate | 2010-08-31-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| grantDate | 2012-06-19-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_84fed194e0c92f3f47866caaa31b901c http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_12841952e1b5d990ea9a3a9e85abf35a |
| publicationDate | 2012-06-19-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | US-8202886-B2 |
| titleOfInvention | Small molecule E2F inhibitor |
| abstract | A small molecular inhibitor of E2F (HLM006474) was identified using a computer-based virtual screen and the known crystal structure of the DNA bound E2F4/DP2 heterodimer. Treatment of multiple cell lines resulted in the loss of intracellular E2F4 DNA-binding activity. Overnight exposure to HLM006474 resulted in down regulation of total E2F4 protein as well as several known E2F targets. The effects of treatment on different cell lines included a reduction in cell proliferation and an increase in apoptosis. Apoptosis was induced in a manner distinct from cisplatin and doxorubicin. E2F4-null MEFs (mouse embryo fibroblasts) were less sensitive than wildtype counterparts to the apoptosis-inducing activity of the compound revealing its biological specificity. A375 cells were extremely sensitive to the apoptosis-inducing activity of the compound in two-dimensional culture and HLM006474 was a potent inhibitor of melanocytes proliferation and subsequent invasion in a three-dimensional tissue culture model system. |
| isCitedBy | http://rdf.ncbi.nlm.nih.gov/pubchem/patent/US-9880150-B2 http://rdf.ncbi.nlm.nih.gov/pubchem/patent/US-11571483-B2 |
| priorityDate | 2008-03-18-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 294.