http://rdf.ncbi.nlm.nih.gov/pubchem/patent/US-2007232684-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_9ded504b18a27b7d519fdb42769fa0b2 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D207-327 |
| classificationIPCAdditional | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D207-32 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D417-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D413-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-40 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D207-327 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D207-30 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K- |
| filingDate | 2007-05-24-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_4fc4eb4096fbf8253150234e43befc07 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_ba7daef0b7784308f1dc6bc9dc243f1d |
| publicationDate | 2007-10-04-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | US-2007232684-A1 |
| titleOfInvention | Compounds for inhibition of HIV infection by blocking HIV entry |
| abstract | A group of compounds that inhibit HIV replication by blocking HIV entry was identified. Two representative compounds, designated NB-2 and NB-64, inhibited HIV replication (p24 production) with IC 50 values <0.5 μg/ml. It was proved that NB-2 and NB-64 are HIV entry inhibitors by targeting the HIV gp41 since: 1) they inhibited HIV-mediated cell fusion; 2) they inhibited HIV replication only when they were added to the cells less than one hour after virus addition; 3) they did not block the gp120-CD4 binding; 4) they did not interact with the coreceptor CXCR4 since they failed to block anti-CXCR4 antibody binding to CXCR4-expressing cells; 5) they blocked the formation of the gp41 core that is detected by sandwich enzyme linked immunosorbent assay (ELISA) using a conformation-specific MAb NC-1; 6) they inhibited the formation of the gp41 six-helix bundle revealed by fluorescence native-polyacrylamide gel electrophoresis (FN-PAGE); and 7) they blocked binding of D-peptide to the hydrophobic cavity within gp41 coiled coil domain, modeled by peptide IQN17. These results suggested that NB-2 and NB-64 may interact with the hydrophobic cavity and block the formation of the fusion-active gp41 coiled coil domain, resulting in inhibition of HIV-1 mediated membrane fusion and virus entry. |
| isCitedBy | http://rdf.ncbi.nlm.nih.gov/pubchem/patent/US-2011190343-A1 http://rdf.ncbi.nlm.nih.gov/pubchem/patent/US-8455516-B2 |
| priorityDate | 2002-11-21-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 219.