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Format of Original

6 p.

Publication Date



American Chemical Society

Source Publication

ACS Medicinal Chemistry Letters

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Original Item ID

DOI: 10.1021/ml500154q


A potent class of indolinyl-thiazole based inhibitors of cellular lipid uptake mediated by scavenger receptor, class B, type I (SR-BI) was identified via a high-throughput screen of the National Institutes of Health Molecular Libraries Small Molecule Repository (NIH MLSMR) in an assay measuring the uptake of the fluorescent lipid DiI from HDL particles. This class of compounds is represented by ML278 (1711), a potent (average IC50 = 6 nM) and reversible inhibitor of lipid uptake via SR-BI. ML278 is a plasma-stable, noncytotoxic probe that exhibits moderate metabolic stability, thus displaying improved properties for in vitro and in vivo studies. Strikingly, ML278 and previously described inhibitors of lipid transport share the property of increasing the binding of HDL to SR-BI, rather than blocking it, suggesting there may be similarities in their mechanisms of action.


Published version. ACS Medicinal Chemistry Letters, Vol. 6, No. 4 (2015): 375-380. DOI. © 2015 American Chemical Society. Used with permission.

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