发明名称 |
NOVEL COMPOUNDS THAT ENHANCE DIMERIZATION OF THE SUBUNITS OF HIV-1 REVERSE TRANSCRIPTASE HAVING MUTATIONS ASSOCIATED WITH RESISTANCE TO NONNUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS |
摘要 |
The invention provides novel compounds that enhance dimerization of the subunits of HIV-1 reverse transcriptase having mutations associated with resistance to nonnucleoside reverse transcriptase inhibitors (NNRTIs). Such compounds inhibit HIV-1 reverse transcriptase activity and as such, inhibit HIV-1, in particular HIV-1 resistant to conventional NNRTIs. The invention provides a method of determing whether a compound enhances formation of a complex between a p66 and p51 subunit polypeptides of HIV-1 reverse transcriptase, in which the p66 subunit has at least one or more mutations associated with resistance of HIV-1 to at least one NNRTI. The invention further provides methods of using a compound that enhances formation of a complex between a p66 subunit polypeptide having at least one mutation associated with resistance of HIV-1 to at least one NNRTI and a p51 subunit of HIV-1 reverse transcriptase. |
申请公布号 |
WO03053343(A3) |
申请公布日期 |
2003.10.23 |
申请号 |
WO2002US39218 |
申请日期 |
2002.12.06 |
申请人 |
PROGENICS PHARMACEUTICALS, INC. |
发明人 |
O'HARA, BRYAN, M. |
分类号 |
A61K31/00;A61K31/70;C12N5/02;C12N7/01 |
主分类号 |
A61K31/00 |
代理机构 |
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