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Metabolic syndrome

Two for the price of one

Nature Reviews Drug Discovery volume 3, page 475 (2004)Cite this article

A study by Theodore Kurtz, Harrihar Pershadsingh, Mitchell Avery and colleagues, published in Hypertension, was prompted by three observations. First, clinical trials have shown that treating hypertensive patients with some antagonists of the angiotensin II type I receptor (ARBs) can reduce their risk of developing type 2 diabetes. Second, the blood pressure of diabetics treated with drugs that activate PPAR-γ — a transcriptional regulator of glucose and lipid metabolism — is often moderately reduced.When they also noted a structural resemblance between the ARB telmisartan and the PPAR-γ ligand pioglitazone, the authors set out to test the hypothesis that some molecules can modulate both angiotensin receptors and PPAR-γ.

Different ARBs were tested for their capacity to activate the expression of a reporter gene conjugated to murine PPAR-γ in cultured monkey fibroblasts.At physiological concentrations, only telmisartan induced a substantial response.With an EC50 of 4.5 μM, the authors classified telmisartan as a moderately potent, partial PPAR-γ agonist, by comparison to full agonists such as pioglitazone.

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References

ORIGINAL RESEARCH PAPERS

  1. Benson, S. C. et al. Identification of telmisartan as a unique angiotensin II receptor antagonist with selective PPARγ-modulating activity. Hypertension 43, 993–1002 (2004)

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  2. Schupp, M. et al. Angiotensin type I receptor blockers induce peroxisome proliferator-activated receptor-γ activity. Circulation 109, 2054–2057 (2004)

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FURTHER READING

  1. Zaman, M. A., Oparil, S. & Calhoun, D. A. Drugs targeting the renin–angiotensin–aldosterone system. Nature Rev. Drug Discov. 1, 621–636 (2002)

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Authors
  1. Suzanne Farley
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Farley, S. Two for the price of one. Nat Rev Drug Discov 3, 475 (2004). https://doi.org/10.1038/nrd1429

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  • DOI: https://doi.org/10.1038/nrd1429

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