公开(公告)号：WO2011140047A1

公开(公告)日：2011-11-10

申请号：PCT/US2011/034940

申请日：2011-05-03

Applicant: TRUSTEES OF DARTMOUTH COLLEGE ,  CHANG, Ta-Yuan ,  CHANG, Catherine, C.Y.

Inventor： CHANG, Ta-Yuan ,  CHANG, Catherine, C.Y.

IPC: C12N5/00

CPC classification number: C12Q1/48 ,  G01N2333/91057 ,  G01N2500/02

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.

Abstract translation: 本发明是一种鉴别化合物的方法，该化合物是基于新戊酸烯醇酮是ACAT底物的新发现的变构型和/或其它新型ACAT抑制剂。 当胆固醇存在于测定中时，ACAT的孕烯醇酮酯化剧烈活化。 该方法包括通过ACAT在两种不同条件下测定孕烯醇酮的酯化：用胆固醇或不含胆固醇。 该方法可用于测试和分类各种候选ACAT抑制剂作为变构或其他新型ACAT抑制剂，或者可用于高通量筛选鉴定此类ACAT抑制剂。

公开(公告)号：WO2013019932A1

公开(公告)日：2013-02-07

申请号：PCT/US2012/049290

申请日：2012-08-02

Applicant: TRUSTEES OF DARTMOUTH COLLEGE ,  CHANG, Ta-yuan ,  CHANG, Catherine, C.Y. ,  HUANG, Paul, Li-Hau

Inventor： CHANG, Ta-yuan ,  CHANG, Catherine, C.Y. ,  HUANG, Paul, Li-Hau

IPC: C12N15/113 ,  A61K31/7088

CPC classification number: A61K31/713 ,  A61K31/7105 ,  A61K45/06 ,  C12N15/1137 ,  C12N2310/14 ,  C12N2310/141 ,  C12N2330/51 ,  C12Y203/01009

Abstract: The present invention includes methods for increasing white blood cell counts through administration of inhibitors of acyl -coenzyme A : cholesterol acyltransferase 1 (ACAT1). ACAT inhibitors are used to treat symptoms of immunosuppression, either alone or in combination with other treatments.

Abstract translation: 本发明包括通过施用酰基辅酶A：胆固醇酰基转移酶1（ACAT1）的抑制剂来增加白细胞计数的方法。 ACAT抑制剂用于单独或与其他治疗组合治疗免疫抑制症状。