Benzoxazolone Carboxamides: Potent and Systemically Active Inhibitors of Intracellular Acid Ceramidase
| العنوان: | Benzoxazolone Carboxamides: Potent and Systemically Active Inhibitors of Intracellular Acid Ceramidase |
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| المؤلفون: | Pizzirani, Daniela, Bach, Anders, Realini, Natalia, Armirotti, Andrea, Mengatto, Luisa, Bauer, Inga, Girotto, Stefania, Pagliuca, Chiara, De Vivo, Marco, Summa, Maria, Ribeiro, Alison, Piomelli, Daniele |
| المصدر: | Pizzirani, D; Bach, A; Realini, N; Armirotti, A; Mengatto, L; Bauer, I; et al.(2015). Benzoxazolone carboxamides: Potent and systemically active inhibitors of intracellular acid ceramidase. Angewandte Chemie-International Edition, 54(2), 485-489. doi: 10.1002/anie.201409042. UC Irvine: Retrieved from: http://www.escholarship.org/uc/item/3q84t552 Angewandte Chemie (International ed. in English), vol 54, iss 2 Angewandte Chemie (International Ed. in English) |
| بيانات النشر: | Wiley, 2014. |
| سنة النشر: | 2014 |
| مصطلحات موضوعية: | Benzoxazoles, acid ceramidase, Organic Chemistry, Chemical Sciences, Ceramidases, sphingosine-1-phosphate, cancer, ceramide, General Medicine, Enzyme Inhibitors, Amides, enzyme inhibition, Communications |
| الوصف: | © 2015 The Authors. Published by Wiley-VCH Verlag GmbH & Co. KGaA. The ceramides are a family of bioactive lipid-derived messengers involved in the control of cellular senescence, inflammation, and apoptosis. Ceramide hydrolysis by acid ceramidase (AC) stops the biological activity of these substances and influences survival and function of normal and neoplastic cells. Because of its central role in the ceramide metabolism, AC may offer a novel molecular target in disorders with dysfunctional ceramide-mediated signaling. Here, a class of benzoxazolone carboxamides is identified as the first potent and systemically active inhibitors of AC. Prototype members of this class inhibit AC with low nanomolar potency by covalent binding to the catalytic cysteine. Their metabolic stability and high in vivo efficacy suggest that these compounds may be used as probes to investigate the roles of ceramide in health and disease, and that this scaffold may represent a promising starting point for the development of novel therapeutic agents. |
| وصف الملف: | application/pdf |
| تدمد: | 0044-8249 |
| URL الوصول: | https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d57d7aea028accf6f034de83e84fef5f https://doi.org/10.1002/ange.201409042 |
| حقوق: | OPEN |
| رقم الأكسشن: | edsair.doi.dedup.....d57d7aea028accf6f034de83e84fef5f |
| قاعدة البيانات: | OpenAIRE |
| تدمد: | 00448249 |
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