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A phosphatase and diabetes technology, applied in the field of phosphatase action and inhibition, can solve the problems of reducing liver glucose, increasing glucose utilization, and unclear mechanism

Inactive Publication Date: 2009-11-25
MEDICAL RESEARCH COUNCIL
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Problems solved by technology

Meformin reduces hepatic glucose production and increases glucose utilization through the activation of AMPK, but the mechanism of AMPK activation by meformin is unclear

Method used

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Embodiment Construction

[0040] Meformin is one of the main drugs in the treatment of type II diabetes. Although the mechanism of action is not clear, it can enhance the activity of AMPK. Normally AMPK is activated in response to increased levels of AMP by phosphorylation of threonine residues within the catalytic site of the alpha subunit. After incubation of HEK293 and HeLa cells with the meformin analogue phenformin, magnesium-dependent phenotypes with okadaic acid resistance were shown by protein phosphatase activity assays in response to phenformin or meformin The activity of casein phosphatase was reduced by about 20%. Further studies showed that the activities of two closely related PPM family protein phosphatases, PPM1E and PPM1F, were also inhibited after HEK293 was incubated with phenformol, revealing that they may be directly and / or indirectly regulated by phenformin. targeting, and leads to an increase in AMPK activity. The present invention is based on these surprising discoveries.

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Abstract

The invention relates to a method for identifying a candidate agent for use in a medicament for diabetes or obesity the method comprising (i) providing a candidate inhibitor of PPM phosphatase, (ii) providing a first and a second sample comprising PPM phosphatase, (iii) contacting the candidate inhibitor with the first sample comprising PPM phosphatase, and (iv) assaying the first and second samples for PPM phosphatase activity, wherein the PPM phosphatase is selected from the group consisting of PPM1E, PPM1F, PPM1J, PPM1K, PPM1L and PPM1M, wherein if the PPM phosphatase activity is lower in the first sample than in the second sample then the candidate inhibitor is identified as a candidate agent for use in a medicament for diabetes or obesity, preferably type II diabetes. The invention also relates to the use of metformin and phenformin as inhibitors of PPM phosphatases.

Description

technical field [0001] The present invention relates to the field of phosphatase action and inhibition, and also to diseases related to glucose metabolism / regulation, such as diabetes and obesity. Background technique [0002] Metformin is a biguanide compound known to be used in the treatment of diabetes. The target of methformin is unknown. Meformin acts as a mitochondrial toxin. [0003] Phenformin is an analog of meformin and is also a biguanide compound. Phenylformin has been used in the treatment of diabetes. The target of phenformin is unknown. Phenylformin is a potent mitochondrial toxin. Phenylform showed side effects including severe lactic acidosis. This can be fatal and has been shown to be fatal. The presence of these side effects, such as lactic acidosis, has led to the withdrawal of phenformin as a diabetes treatment in most countries of the world. [0004] AMP-activated protein kinase (AMP-activated protein kinase) has been considered as a key regulat...

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Application Information

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IPC IPC(8): A61P3/04A61P3/10A61K45/06C12Q1/42
Inventor 帕特丽夏·汤森·韦德·科恩
Owner MEDICAL RESEARCH COUNCIL
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