Article ; Online: Fluorinated aldosterone synthase (CYP11B2)-inhibitors for differential diagnosis between bilateral and unilateral conditions of primary aldosteronism.
Bioorganic & medicinal chemistry letters
2023 Volume 96, Page(s) 129501
Abstract: The enzyme aldosterone synthase (CYP11B2) is specifically expressed in aldosterone-producing tissue of the adrenal cortex and is overexpressed in aldosterone-producing adenomas (APA). It therefore represents an ideal target for molecular imaging, ... ...
| Abstract | The enzyme aldosterone synthase (CYP11B2) is specifically expressed in aldosterone-producing tissue of the adrenal cortex and is overexpressed in aldosterone-producing adenomas (APA). It therefore represents an ideal target for molecular imaging, particularly for the differential diagnosis between bilateral hyperplasia and unilateral APA in primary aldosteronism. However, the presence of the cortisol-producing enzyme 11β-hydroxylase (CYP11B1) in the adrenal cortex remains very challenging owing to its high homology to CYP11B2. Within this study, we efficiently synthesized a variety of disubstituted fluorinated pyridines and pyrazines by Suzuki coupling reactions. These compounds were evaluated for their ability to inhibit CYP11B1 and CYP11B2 in transfected Y1 cells and in NCI-h295 cells. Several compounds were found to exhibit excellent affinity (IC |
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| MeSH term(s) | Humans ; Cytochrome P-450 CYP11B2 ; Steroid 11-beta-Hydroxylase ; Aldosterone ; Hyperaldosteronism/diagnosis ; Diagnosis, Differential ; Adenoma | |||||
| Chemical Substances | Cytochrome P-450 CYP11B2 (EC 1.14.15.4) ; Steroid 11-beta-Hydroxylase (EC 1.14.15.4) ; Aldosterone (4964P6T9RB) | |||||
| Language | English | |||||
| Publishing date | 2023-10-05 | |||||
| Publishing country | England | |||||
| Document type | Journal Article ; Research Support, Non-U.S. Gov't | |||||
| ZDB-ID | 1063195-1 | |||||
| ISSN | 1464-3405 ; 0960-894X | |||||
| ISSN (online) | 1464-3405 | |||||
| ISSN | 0960-894X | |||||
| DOI | 10.1016/j.bmcl.2023.129501 | |||||
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| Database | MEDical Literature Analysis and Retrieval System OnLINE |
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