http://rdf.ncbi.nlm.nih.gov/pubchem/patent/JP-2015536990-A
Outgoing Links
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classificationCPCAdditional | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/G01N2333-96466 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/G01N2500-20 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/G01N2500-04 |
classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-426 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C12Q1-37 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-4196 |
classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P35-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-426 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-4196 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P43-00 |
filingDate | 2013-11-08-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationDate | 2015-12-24-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationNumber | JP-2015536990-A |
titleOfInvention | Small molecule inhibitor of MALT1 |
abstract | MALT1 cleavage activity is associated with the pathogenesis of activated B-cell-like diffuse large B-cell lymphoma (ABC-DLBCL), a chemoresistant form of DLBCL. The present inventors developed a MALT1 activity assay and identified chemically diverse MALT1 inhibitors. The selected lead compound MI-2 was characterized by direct binding to MALT1 and inhibition of its protease function. MI-2 concentrated in human ABC-DLBCL cells and irreversibly inhibited cleavage of the MALT1 substrate. This was accompanied by suppression of NF-κB reporter activity, inhibition of c-REL nuclear localization and down-regulation of NF-κB target gene signature. Most notably, MI-2 was non-toxic to mice and showed potent and specific activity against ABC-DLBCL cell lines in vitro and ABC-DLBCL tumors xenografted in vivo . This compound was also effective ex vivo against primary human non-GCB-DLBCL. |
isCitedBy | http://rdf.ncbi.nlm.nih.gov/pubchem/patent/JP-7142022-B2 http://rdf.ncbi.nlm.nih.gov/pubchem/patent/WO-2018159650-A1 |
priorityDate | 2012-11-09-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 30.