Assay screens compounds that target the endoplasmic reticulum

Researchers have developed an assay to monitor the effects of drug candidates on endoplasmic reticulum (pictured) function

The endoplasmic reticulum (ER) plays a critical role in protein, lipid and glucose metabolism, and interventions that target ER function may be useful therapeutic strategies for metabolic and other pathologies. Now, researchers have developed an assay to monitor the effects of drug candidates on ER function.

Using the new technology, researchers screened various compounds and found that a small molecule, which they named azoramide, was a potent modulator of ER function. They then evaluated azoramide in animal models of obesity and type 2 diabetes and found that the compound improved pancreatic beta-cell function and enhanced insulin sensitivity in peripheral tissues.

The results “provide proof-of-principle for the notion that specific ER modulators can be potential drug candidates for type 2 diabetes”, the researchers conclude in Science Translational Medicine
[1]
(online, 17 June 2015).

References

[1] Fu S, Yalcin A, Lee GY et al. Phenotypic assays identify azoramide as a small-molecule modulator of the unfolded protein response with antidiabetic activity. Science Translational Medicine 2015;7(292):292ra98. doi:10.1126/scitranslmed.aaa9134.

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Citation
The Pharmaceutical Journal, PJ, 27 June/4 July 2015, Vol 294, No 7868/9;294(7868):DOI:10.1211/PJ.2015.20068818