Literature DB >> 16685193

Can the dextroenantiomer of the aromatase inhibitor fadrozole be useful for clinical investigation of aldosterone-synthase inhibition?

Joël Ménard1, Leigh Pascoe.   

Abstract

The beneficial effects of spironolactone, eplerenone, amiloride and potassium in preventing cardiovascular damage in various experimental models of salt-induced hypertension can be dissociated from blood pressure effects, and have drawn attention to the direct genomic and non-genomic actions of aldosterone at the level of the vessels, the heart and the kidneys. Exposure to endogenous aldosterone could be decreased by direct and specific aldosterone-synthase inhibition. FAD 286A, the dextroenantiomer of the aromatase inhibitor fadrozole, might be a first candidate to investigate in humans, the physiological impact and therapeutic properties of aldosterone-synthase inhibition, especially in various forms of primary aldosteronism.

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Year:  2006        PMID: 16685193     DOI: 10.1097/01.hjh.0000226183.98439.b3

Source DB:  PubMed          Journal:  J Hypertens        ISSN: 0263-6352            Impact factor:   4.844


  3 in total

1.  Discovery and in Vivo Evaluation of Potent Dual CYP11B2 (Aldosterone Synthase) and CYP11B1 Inhibitors.

Authors:  Erik L Meredith; Gary Ksander; Lauren G Monovich; Julien P N Papillon; Qian Liu; Karl Miranda; Patrick Morris; Chang Rao; Robin Burgis; Michael Capparelli; Qi-Ying Hu; Alok Singh; Dean F Rigel; Arco Y Jeng; Michael Beil; Fumin Fu; Chii-Whei Hu; Daniel LaSala
Journal:  ACS Med Chem Lett       Date:  2013-10-17       Impact factor: 4.345

2.  Structural insights into aldosterone synthase substrate specificity and targeted inhibition.

Authors:  Natallia Strushkevich; Andrei A Gilep; Limin Shen; Cheryl H Arrowsmith; Aled M Edwards; Sergey A Usanov; Hee-Won Park
Journal:  Mol Endocrinol       Date:  2013-01-15

3.  Aldosterone synthase inhibition for the treatment of hypertension and the derived mechanistic requirements for a new therapeutic strategy.

Authors:  Christoph D Schumacher; Ronald E Steele; Hans R Brunner
Journal:  J Hypertens       Date:  2013-10       Impact factor: 4.844

  3 in total

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