12:00 AM
Dec 03, 2012
 |  BioCentury  |  Emerging Company Profile

Lipigon: LPL protectorate

Lipigon taking new approach to lipoprotein lipase to prevent atherosclerosis

Lipoprotein lipase has long been a desirable target to treat atherosclerosis, but direct-acting activators of the enzyme have failed. Lipigon Pharmaceuticals AB is taking a different tack, developing small molecules that protect the enzyme from inactivation by endogenous inhibitors.

Lipoprotein lipase (LPL) plays a central role in blood lipid metabolism. It hydrolyzes triglycerides - resulting in formation of pre-beta HDL - and delivers free fatty acids to peripheral tissues for use as energy or storage. The enzyme also facilitates receptor-mediated uptake of atherogenic lipoproteins.

Normally, LPL is secreted from tissues such as the heart, skeletal muscle and adipose tissue as a low-activity, non-covalent dimer. According to Chairman and CEO Stefan Nilsson, in this state, LPL "can hydrolyze about 3,000 ester bonds per minute."

But the rate is boosted soon after secretion, when LPL bonds to its substrate, triglyceride-rich lipoproteins that contain LPL's co-factor, apolipoprotein...

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