http://rdf.ncbi.nlm.nih.gov/pubchem/patent/EP-1034182-A1

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classificationCPCAdditional http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C12N2740-16322
classificationCPCInventive http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07K14-005
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filingDate 1998-11-26-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_98b27a159aed18109d4bff023e550670
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_7672bf30fab5647cfff4af5ac50d563c
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http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_f778ae8da13d42960885e18e70a9f535
publicationDate 2000-09-13-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber EP-1034182-A1
titleOfInvention Inhibition of nuclear import by backbone cyclic peptide analogs
abstract The design and the synthesis of backbone cyclic peptide analogs which functionally mimic the nuclear localization signal (NLS) region of macromolecules is disclosed. The principles of the invention are exemplified for the NLS sequences of the human immunodeficiency virus type 1 proteins MA, Vpr, Tat and NLS-like sequences of HIV-1 protein Vif. We disclose the discovery of a novel, highly potent backbone cyclic peptide, designated BCvir, which inhibits nuclear import with an IC50 value of 35 nM. This inhibitory potency is to be compared to 12νM exhibited by the linear parent HIV-1 MA NLS peptide. BCvir also reduced HIV-1 production by 75 % in infected non-dividing cultured human T-cells and was relatively resistant to tryptic digestion. These properties render backbone cyclic peptide analogs of NLS or NLS-like sequences as candidates for novel drugs based on blocking nuclear import of viral genomes.
priorityDate 1997-11-27-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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