http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CN-105188376-B
Outgoing Links
| Predicate | Object |
|---|---|
| classificationCPCAdditional | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/G01N2500-20 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/G01N2500-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/G01N2333-96466 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C12Q1-37 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-426 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-4196 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A01N43-64 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-41 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-425 |
| filingDate | 2013-11-08-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| grantDate | 2017-12-01-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationDate | 2017-12-01-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | CN-105188376-B |
| titleOfInvention | Small molecule inhibitors of MALT1 |
| abstract | The cleavage activity of MALT1 is implicated in the pathogenesis of activated B-cell-like diffuse large B-cell lymphoma (ABC‑DLBCL), a chemotherapy-resistant form of DLBCL. We developed a MALT1 activity assay and identified chemically diverse MALT1 inhibitors. The selected lead compound, MI‑2, is characterized by directly binding to MALT1 and inhibiting its protease function. MI‑2 is enriched in human ABC‑DLBCL cells and irreversibly inhibits cleavage of MALT1 substrates. These effects were accompanied by inhibition of NF‑κB reporter activity, inhibition of c‑REL nuclear localization, and downregulation of NF‑κB target gene markers. Most notably, MI‑2 is avirulent in mice and exhibits potent and specific activity against ABC‑DLBCL cell lines in vitro, and against xenografted ABC‑DLBCL tumors in vivo. The compounds are also effective against primary human non-GCB-DLBCL in vitro. |
| 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: 410.