Predicate |
Object |
assignee |
http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_91b7a64e0d0148c44bfed6a1476df644 http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_d33d3bd7e5a6eb9d29d4a9bf3f1918d2 http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_42585dd513ffecc03f37e398ee15aac2 http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_bc2b03342511abc88f60c63f2acd96d0 http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_45a30a23ec8041f752eb97e3c66957b8 |
classificationCPCInventive |
http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K47-645 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-7048 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-337 |
classificationIPCInventive |
http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K51-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-7048 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-337 |
filingDate |
2009-02-05-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
inventor |
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_07ef1856f774471f8bafa37b63bca204 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_812b22bb5951be05d9ef52f0f75dd503 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_72a4f469904723567c79dec2797609de http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_462495479101cccdf23c3aae8f0ba556 |
publicationDate |
2009-08-13-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationNumber |
WO-2009099636-A1 |
titleOfInvention |
Conjugation of small molecules to octaarginine transporters for overcoming multi-drug resistance |
abstract |
Many cancer therapeutic agents elicit resistance that renders them ineffective and often produces cross resistance to other drugs. One of the most common mechanisms of resistance involves P-glycoprotein (Pgp) mediated drug efflux. Here we provide compositions and methods that restore the efficacy of a therapeutic agent reduced by resistance by conjugation of the same agent to an oligoarginine transporter comprising from about 5 to about 25 guanidino or amidino moieties. We specifically show that the widely used chemotherapeutic agent taxol, ineffective against taxol-resistant human ovarian cancer cell lines, can be incorporated into an octaarginine conjugate that is effective against the same taxol-resistant cell lines. Significantly, the ability of the taxol conjugates to overcome taxol resistance is observed both in cell culture and in animal models of ovarian cancer. The generality and mechanistic basis for this effect were also explored with other Pgp substrate. This approach shows generality for overcoming the multidrug resistance elicited by small molecule cancer chemotherapeutics and could improve the prognosis for many cancer patients and fundamentally alter search strategies for novel therapeutic agents effective against resistant disease. |
isCitedBy |
http://rdf.ncbi.nlm.nih.gov/pubchem/patent/US-9816066-B2 http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CN-105037739-B http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CN-104370862-A http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CN-105396141-A http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CN-105396141-B http://rdf.ncbi.nlm.nih.gov/pubchem/patent/WO-2023023276-A1 http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CN-105037739-A |
priorityDate |
2008-02-07-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
type |
http://data.epo.org/linked-data/def/patent/Publication |