Invention Grant
US08673587B2 Methods for identifying allosteric and other novel acyl-coenzyme A:cholesterol acyltransferase inhibitors
失效
用于鉴别变构和其他新型酰基辅酶A：胆固醇酰基转移酶抑制剂的方法
- Patent Title: Methods for identifying allosteric and other novel acyl-coenzyme A:cholesterol acyltransferase inhibitors
- Patent Title (中): 用于鉴别变构和其他新型酰基辅酶A：胆固醇酰基转移酶抑制剂的方法
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Application No.: US13639141Application Date: 2011-05-03
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Publication No.: US08673587B2Publication Date: 2014-03-18
- Inventor: Ta-Yuan Chang , Catherine C. Y. Chang
- Applicant: Ta-Yuan Chang , Catherine C. Y. Chang
- Applicant Address: US NH Hanover
- Assignee: Trustees of Dartmouth College
- Current Assignee: Trustees of Dartmouth College
- Current Assignee Address: US NH Hanover
- Agency: Licata & Tyrrell P.C.
- International Application: PCT/US2011/034940 WO 20110503
- International Announcement: WO2011/140047 WO 20111110
- Main IPC: C12Q1/48
- IPC: C12Q1/48
Abstract:
The present invention is a method for identifying compounds that are allosteric and/or other novel ACAT inhibitors that is based on the novel finding that pregnenolone is a substrate for ACAT; esterification of pregnenolone by ACAT is dramatically activated when cholesterol is present in the assay. The method comprises measuring the esterification of pregnenolone by ACAT under two different conditions: with cholesterol, or without cholesterol. This method can be used to test and categorize various candidate ACAT inhibitors as allosteric or other novel ACAT inhibitors, or it can be used in high-throughput screening for identifying such ACAT inhibitors.
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