发明名称 |
Methods of modulating ubiquitin ligase activity |
摘要 |
Methods are provided for modulating the activity of multimeric ubiquitin-protein E3 ligases including, but not limited to, E6AP ligase activities. The methods reduce the level of oligomer formation such as homotrimeric E6AP ligase to reduce the enzyme activity. Alternatively, agents are provided that can promote the association of the ligase monomers, thereby increasing the ligase activity. Accordingly, novel therapeutic strategies are provided that are useful for the treatment of pathologies resulting from mutations in the genes encoding the ligases and which adversely increase or decrease a ubiquitination reaction. |
申请公布号 |
US9328341(B2) |
申请公布日期 |
2016.05.03 |
申请号 |
US201514685865 |
申请日期 |
2015.04.14 |
申请人 |
Board of Supervisors of Louisiana State University and Agricultural and Mechanical College |
发明人 |
Haas Arthur L.;Ronchi Virginia P. |
分类号 |
C12N9/00;C12N9/99;A61K31/165 |
主分类号 |
C12N9/00 |
代理机构 |
Thomas | Horstemeyer, LLP |
代理人 |
Thomas | Horstemeyer, LLP |
主权项 |
1. A method of modulating the activity of a ubiquitin-protein E3 ligase comprising the step of inhibiting the formation of an E6-Associated Protein (E6AP) polypeptide trimer by contacting the E6AP polypeptide with an agent that binds to the E6AP polypeptide, wherein the agent is N-acetyl-L-phenylalanylamide, and thereby reducing the generation of a ubiquitin-protein E3 lipase activity. |
地址 |
Baton Rouge LA US |