Flurizan modulates the APP-gamma secretase

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Myriad Genetics, Inc. (NASDAQ: MYGN) announced that the mechanism of action of Flurizan® (tarenflurbil) -- its drug candidate for the treatment of Alzheimer's disease, Previous studies, in vitro, in animal models and in humans, have demonstrated that Flurizan selectively lowers toxic amyloid beta 42, and is the first member of a new class of drugs known as selective amyloid lowering agents (SALAs). Further, Flurizan has been shown to modify the processing of the amyloid precursor protein (APP) by the gamma secretase enzyme. The specific way in which Flurizan accomplishes this reduction in the toxic amyloid beta 42 had remained a mystery until now.

The Nature paper confirms the SALA properties of Flurizan and establishes the mechanism by which Flurizan modulates the APP-gamma secretase interaction. The authors demonstrate that the molecular target of Flurizan is the amyloid precursor protein itself -- the substrate of gamma secretase. Flurizan modifies the conformation of the APP molecule as it is bound to the gamma secretase complex. This change in the shape and/or position of APP in the complex results in cleavage by gamma secretase that produces shorter length, non-toxic amyloid beta fragments, such as amyloid beta 38 and amyloid beta 40. This exciting finding is novel in that most drugs target enzymes, blocking their function directly, but the substrate of an enzyme has not generally been seen as a drug target. These new findings are consistent with previous studies that show that Flurizan selectively lowers amyloid beta 42 by shifting the conformation of the APP/gamma secretase complex through allosteric binding.

"The article in Nature adds to the understanding of the mechanism of action of Flurizan, providing a molecular basis for its ability to slow the progression of Alzheimer's disease, as was demonstrated in previous human clinical studies," said Adrian Hobden, Ph.D., President of Myriad Pharmaceuticals, Inc. "The findings help explain why compounds like Flurizan can have a dramatic effect on lowering amyloid beta 42, the initiator of plaque formation in the human brain, and offer hope for the treatment of patients who suffer from Alzheimer's disease." ...http://www.nutraingredients.com

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