Emmerich, Juliette and van Koppen, Chris J. and Burkhart, Jens L. and Engeli, Roger T. and Hu, Qingzhong and Odermatt, Alex and Hartmann, Rolf W.. (2018) Accelerated skin wound healing by selective 11β²-Hydroxylase (CYP11B1) inhibitors. European journal of medicinal chemistry, 143. pp. 591-597.
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Official URL: https://edoc.unibas.ch/68084/
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Abstract
Previous studies have shown that inhibition of cortisol biosynthesis in skin leads to accelerated wound healing. Here, pyridylmethyl pyridine type 11β-hydroxylase (CYP11B1) inhibitors were optimized for topical application to avoid systemic side effects. The resulting very potent, non-toxic CYP11B1 inhibitor 14 (IC; 50; = 0.8 nM) exhibited good selectivity over 11β-HSD1, CYP17A1 and CYP19A1. The compound showed high stability toward human plasma (t; 1/2; = > 150 min, as a substitute for wound fluid) and low stability toward HLS9 (t; 1/2; = 19 min) for rapid metabolic clearance after absorption. Compound 14 was able to accelerate wound healing in human skin.
| Faculties and Departments: | 05 Faculty of Science > Departement Pharmazeutische Wissenschaften > Pharmazie > Molecular and Systems Toxicology (Odermatt) |
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| UniBasel Contributors: | Odermatt, Alex |
| Item Type: | Article, refereed |
| Article Subtype: | Research Article |
| ISSN: | 1768-3254 |
| Note: | Publication type according to Uni Basel Research Database: Journal article |
| Identification Number: |
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| Last Modified: | 15 Apr 2020 16:26 |
| Deposited On: | 15 Apr 2020 16:26 |
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