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Functional expression of opioid receptors and other human GPCRs in yeast engineered to produce human sterols

Author(s): Bean BDM; Mulvihill CJ; Garge RK; Boutz DR; Rousseau O; Floyd BM; Cheney W; Gardner EC; Ellington AD; Marcotte EM; Gollihar JD; Whiteway M; Martin VJJ;

The yeast Saccharomyces cerevisiae is powerful for studying human G protein-coupled receptors as they can be coupled to its mating pathway. However, some receptors, including the mu opioid receptor, are non-functional, which may be due to the presence of the fungal sterol ergosterol instead of ch ...

Article GUID: 35610225


Discovery of new vascular disrupting agents based on evolutionarily conserved drug action, pesticide resistance mutations, and humanized yeast

Author(s): Garge RK; Cha HJ; Lee C; Gollihar JD; Kachroo AH; Wallingford JB; Marcotte EM;

Thiabendazole (TBZ) is an FDA-approved benzimidazole widely used for its antifungal and antihelminthic properties. We showed previously that TBZ is also a potent vascular disrupting agent and inhibits angiogenesis at the tissue level by dissociating vascular endothelial cells in newly formed blood vessels. Here, we uncover TBZ's molecular target and m ...

Article GUID: 34849907


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