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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 ...

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 ...

Article GUID: 34849907


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