Two for the price of one | Nature Reviews Drug Discovery

Access through your institution Buy or subscribe 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. This is a preview of subscription content, access via your institution ACCESS OPTIONS Access through your institution Subscribe

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customer support REFERENCES ORIGINAL RESEARCH PAPERS * 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) Article  CAS  Google Scholar  * Schupp, M. et al. Angiotensin type I receptor blockers induce peroxisome proliferator-activated receptor-γ

activity. _Circulation_ 109, 2054–2057 (2004) Article  CAS  Google Scholar  FURTHER READING * Zaman, M. A., Oparil, S. & Calhoun, D. A. Drugs targeting the renin–angiotensin–aldosterone

system. _Nature Rev. Drug Discov._ 1, 621–636 (2002) Article  CAS  Google Scholar  Download references Authors * Suzanne Farley View author publications You can also search for this author

inPubMed Google Scholar RIGHTS AND PERMISSIONS Reprints and permissions ABOUT THIS ARTICLE CITE THIS ARTICLE Farley, S. Two for the price of one. _Nat Rev Drug Discov_ 3, 475 (2004).

https://doi.org/10.1038/nrd1429 Download citation * Issue Date: 01 June 2004 * DOI: https://doi.org/10.1038/nrd1429 SHARE THIS ARTICLE Anyone you share the following link with will be able

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