PSN010, Glucokinase and Diabetes
Potential health benefits on diabetes and research finds   2007
PSN010, a member of glucokinase activators, is designed to lower
blood glucose levels by increasing glucose uptake in the liver and
helping the pancreas secrete more insulin.

Glucokinase is an enzyme that plays a central role in glycolysis,
glucose uptake, and glycogen synthesis, catalyzing the
phosphorylation to glucose-6 phosphate in both the liver and in
the pancreas, where it is predominantly expressed. It is a
rate-limiting step of glucose metabolism. [2]

Dietary glucose would be absorbed and converted to glucose-6
phosphate, resulting in enhanced hepatic glucose uptake and
decreased glucose production. Glucokinase plays a key role in the
glucose sensing in the pancreas that results in insulin secretion;
therefore, GK activation should result in production of insulin.

There is some human validation for both glucokinase activators
and glucagons receptor antagonists. [2] Activators of glucokinase
have been proposed for use in treating diabetes [3-7].

In addition, studies have demonstrated that pancreatic beta cell
glucokinase is expressed locally in rat brain, especially in the
ventromedial hypothalamus (VMH). These glucose-responsive
neurons are believed to play an important role in body weight
control. It is because administration of glucose into rat brain
reduces feeding consumption.

The mechanism of the glucose level-detecting system in the
ventromedial hypothalamus (VMH) is believed to be similar to that
for insulin secretion by pancreatic beta cells. Substances able to
activate glucokinase in the VMH probably can activate the
pancreatic beta cells. Thus, it exhibits a glucose rectifying effect
and also potentially rectifies obesity. [8]

This article is for reference only. Consult with your doctor for medical advice. ALL
RIGHTS RESERVED ZHION 2007
[1] Eli Lilly, OSI, form diabetes drug partnership Reuters Fri Jan 5, 2007 8:20am ET
[2] FDA/NIH Joint Symposium on Diabetes Targeting Safe and Effective Prevention
and Treatment May 13-14, 2004 National Institutes of Health Natcher Conference
Center Main Auditorium NIH Campus Bethesda, Maryland. [3-7] WO 00/58293, WO
01/44216, WO 01/83465, WO 01/83478, WO 01/85706, or WO 01/85707 and U.S.
Patent Application Publication US 2003/0138416 A1. [8] IIno; Tomoharu ; et al.
United States Patent Application 20060167053
Eli Lilly and Co. pays $25 million OSI Pharmaceuticals Inc. to acquire exclusive rights to PSN010
and related compounds [1]
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