http://rdf.ncbi.nlm.nih.gov/pubchem/patent/US-9561215-B2

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assignee http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_13df093a57439361f9c81cfbd47e73c8
classificationCPCInventive http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-437
http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-495
http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-496
http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-282
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classificationIPCInventive http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-495
http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-437
http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-282
filingDate 2015-01-05-04:00^^<http://www.w3.org/2001/XMLSchema#date>
grantDate 2017-02-07-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_0ffb736d05809f4b7a1e78b19a721161
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_146e7034d376dd500ffdf79a90f830ad
publicationDate 2017-02-07-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber US-9561215-B2
titleOfInvention BAX-activating cancer therapeutics
abstract The pro-apoptotic Bcl-2 protein Bax initiates apoptosis in almost all apoptotic paradigms. Agents facilitating disruptive Bax insertion into mitochondrial membranes have potential as cancer therapeutics. Small molecule compounds associating with the hydrophobic groove of the pro-apoptotic Bcl-2 protein Bax have been identified and found to promote Bax-dependent, but not Bak-dependent, apoptosis. The compounds alter Bax protein stability in vitro and promote Bax insertion into mitochondria, leading to Bax-dependent mitochondrial outer membrane permeabilization and apoptosis. The compounds activating the pro-apoptotic Bcl-2 protein Bax inhibit the growth of tumors by inducing apoptosis. Pharmaceutical compositions comprising the compounds that activate Bax and induce Bax-dependent apoptosis are useful as anti-cancer therapeutic agents alone or with other anti-cancer agents. Methods for inducing apoptosis and for treating cancer involve administering the compounds to a patient in need thereof.
priorityDate 2014-01-03-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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