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Comment
. 2010 Jul 22;466(7305):443-4.
doi: 10.1038/466443a.

Obesity: New life for antidiabetic drugs

Riekelt H Houtkooper, Johan Auwerx
Comment

Obesity: New life for antidiabetic drugs

Riekelt H Houtkooper et al. Nature. .

Abstract

Anti-diabetic drugs that activate the protein PPARγ had a bright start but soon lost appeal due to undesirable side effects. Subtle modifications may once again make them suitable for treating diabetes.

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Figures

Figure 1
Figure 1. Regulation of PPARγ activity
In the obese state, pro-inflammatory signals lead to the cleavage of the p35 protein to p25. p25 then translocates to the nucleus where it binds to CDK5 and activates it. Choi et al. show that, CDK5 in turn phosphorylates PPARγ on serine residue 273, thereby preventing the transcription of specific PPARγ targets that have anti-obesity effects. Anti-diabetic PPARγ ligands prevent serine 273 phosphorylation.
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References

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