发明名称 |
METHODS FOR IDENTIFYING CHEMICAL MODULATORS OF RAS SUPERFAMILY GTPASE ACTIVITY |
摘要 |
The present invention provides a method of identifying a compound having the ability to modulate the guanine nucleotide exchange cycle of a Ras superfamily GTPase, comprising: a) contacting the compound with a guanine nucleotide exchange factor and a GTPase and obtaining a baseline fluorescence measurement; b) contacting the guanine nucleotide exchange factor and the GTPase without the compound and obtaining a baseline fluorescence measurement; c) adding a fluorophore-conjugated GTP to the components of (a) and (b), respectively; d) obtaining fluorescence measurements of the respective components of (c) over time; e) subtracting the respective baseline fluorescence measurements of (a) and (b) from each fluorescence measurement of (d); and f) comparing the resulting fluorescence values of (e), wherein a decrease or increase in the rate of fluorescence change with the compound as compared with the rate of fluorescence change without the compound identifies a compound having the ability to modulate the guanine nucleotide exchange cycle of a Ras superfamily GTPase. Further provided are compounds of the invention and pharmaceutical compositions comprising compounds of the invention useful for the treatment of cancer and neurological disorders. |
申请公布号 |
WO2005115482(A2) |
申请公布日期 |
2005.12.08 |
申请号 |
WO2005US13444 |
申请日期 |
2005.04.19 |
申请人 |
THE UNIVERSITY OF NORTH CAROLINA AT CHAPEL HILL;SONDEK, JOHN;ROJAS, RAFAEL |
发明人 |
SONDEK, JOHN;ROJAS, RAFAEL |
分类号 |
A61K49/00;C12Q1/34;C12Q1/68 |
主分类号 |
A61K49/00 |
代理机构 |
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代理人 |
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主权项 |
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地址 |
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