http://rdf.ncbi.nlm.nih.gov/pubchem/patent/WO-2012135149-A9
Outgoing Links
Predicate | Object |
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assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_cea1ae5a9f4b7a04c56094c3014cdf49 http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_0787161ea274c9fa59b160d06747ca1b http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_626f5a4efb49df7703e7f453eb683c1c http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_658df3b9d24eb5224b37aaf605741db6 http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_89c0e841ebc3b867b6f3ae87ea71ea5d |
classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-5415 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-00 |
classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-5415 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-53 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P35-00 |
filingDate | 2012-03-26-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_29e4e97ae76660b67e9cb4e4a9495d15 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_f29d208f72cb9a5412a169e61fd6e204 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_f1ac1dfcbff995d1003f38663bcfa73e http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_310baa9fde303eb5aaae3824de936610 |
publicationDate | 2012-11-22-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationNumber | WO-2012135149-A9 |
titleOfInvention | Small molecule modulators of sirt1 activity activate p53 and suppress tumor growth |
abstract | Although -50 % of all types of human cancers harbor wild type TP 53, this p53 tumor suppressor is often deactivated through a concerted action by its abnormally elevated suppressors, MDM2, MDMX, or SIRT1. Reported herein are small molecules such as Inauhzin that effectively reactivates p53 by inhibiting SIRT1 activity, promotes p53 -dependent apoptosis of human cancer cells without causing apparently genotoxic stress. Moreover, Inauhzin stabilizes p53 by increasing p53 acetylation and preventing MDM2 -mediated ubiquitylation of p53 in cells, though not directly in vitro. Remarkably, Inauhzin inhibits cell proliferation, induces senescence and tumor-specific apoptosis, and represses the growth of xenograft tumors derived from p53- harboring H460 and HCT116 cells without causing apparent toxicity to normal tissues and the tumor-bearing SCID mice. As reported herein, Inauhzin is an anti-cancer therapeutic candidate that inhibits SIRT1 activity and activates p53. |
priorityDate | 2011-03-25-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 569.