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BioAssay: AID 504838

Broad Institute Inihibitors of the HDL Receptor, SR-BI Activator Probe Project

The end product of this project is to identify and use small molecules to analyze the mechanism of the HDL receptor which is specifically referred to as the Scavenger Receptor, class B, type I (SR-BI). The specific goal for this aspect of the project is to identify compounds that increase HDL uptake. Developing tools to permit the analysis of SR-BI function and mechanism of action, as well as more ..
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 Related BioAssays
 Related BioAssays
AID: 504838
Data Source: Broad Institute (2085_Activator_Project)
BioAssay Type: Summary, Candidate Probes/Leads with Supporting Evidence
Depositor Category: NIH Molecular Libraries Probe Production Network
BioAssay Version:
Deposit Date: 2011-06-22
Modify Date: 2011-12-19
Depositor Specified Assays
AIDNameTypeComment
504775HTS using DiI-HDL to assay lipid transfer in ldlA[SR-BI] cells Measured in Cell-Based System Using Plate Reader - 2085-01_Activator_SinglePoint_HTS_Activityscreening317297 HTS compounds at SinglePoint in 2085-01 01 DiI-HDL Cell Based Assay measuring Activity
602191HTS using DiI-HDL to assay lipid transfer in ldlA[SR-BI] cells Measured in Cell-Based System Using Plate Reader - 2085-01_Activator_Dose_CherryPick_Activityconfirmatory
Description:
Primary Collaborators:
Monty Krieger,MIT,krieger@mit.edu
Miao Yu,MIT,miaoyu@mit.edu

Project Goal:
The end product of this project is to identify and use small molecules to analyze the mechanism of the HDL receptor which is specifically referred to as the Scavenger Receptor, class B, type I (SR-BI). The specific goal for this aspect of the project is to identify compounds that increase HDL uptake. Developing tools to permit the analysis of SR-BI function and mechanism of action, as well as the manipulation of SR-BI's activity in vitro and in vivo, will have significant impact on our understanding of diverse areas of physiology and pathophysiology of considerable medical importance. Indeed, recent disappointments in attempts to develop HDL-focused pharmaceutical agents with other molecular targets highlight the importance of developing a deeper and broader understanding of all aspects of HDL metabolism, including those mediated by SR-BI. Pharmacologic agents that modulate SR-BI activity have potential clinical applicability (activators that stimulate atheroprotective lipoprotein metabolism), as well as their use as probes to understand the molecular mechanisms underlying SR-BI's multiple activities. Given the central role of SR-BI in lipid transfer and metabolism, activators of SR-BI function will be useful tools to further probe the mechanism of SR-BI.

HDL uptake, SR-B1, cholesterol
Biological Relevance: Developing tools to permit the analysis of SR-BI function and mechanism of action (see below), as well as the manipulation of SR-BI's activity in vitro and in vivo, will have significant impact on our understanding of diverse areas of physiology and pathophysiology of considerable medical importance. Indeed, recent disappointments in attempts to develop HDL-focused pharmaceutical agents with other molecular targets highlight the importance of developing a deeper and broader understanding of all aspects of HDL metabolism, including those mediated by SR-BI. Pharmacologic agents that modulate SR-BI activity have potential clinical applicability (inhibitors that block cellular uptake of pathogens (e.g., HCV) and activators that stimulate atheroprotective lipoprotein metabolism), as well as their use as probes to understand the molecular mechanisms underlying SR-BI's multiple activities. Given the central role of SR-BI in lipid transfer and metabolism, both activators and inhibitors of SR-BI function will be useful tools to further probe the mechanism of SR-BI.
Additional Information
Grant Number: 2 R01 HL052212-11

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