Journal
ACS MEDICINAL CHEMISTRY LETTERS
Volume 4, Issue 12, Pages 1203-1207Publisher
AMER CHEMICAL SOC
DOI: 10.1021/ml400324c
Keywords
Inhibitor; CYP11B2; aldosterone synthase; aldosterone; hypertension; enzyme; CYP11B1; Cushing's syndrome; cortisol
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Aldosterone is a key signaling component of the renin-angiotensin-aldosterone system and as such has been shown to contribute to cardiovascular pathology such as hypertension and heart failure. Aldosterone synthase (CYP11B2) is responsible for the final three steps of aldosterone synthesis and thus is a viable therapeutic target A series of imidazole derived inhibitors, including clinical candidate 7n, have been identified through design and structure-activity relationship studies both in vitro and in vivo. Compound 7n was also found to be a potent inhibitor of 11 beta-hydroxylase (CYP11B1), which is responsible for cortisol production. Inhibition of CYP11B1 is being evaluated in the clinic for potential treatment of hypercortisol diseases such as Cushing's syndrome.
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