共查询到20条相似文献,搜索用时 12 毫秒
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Benzoxazolone Carboxamides: Potent and Systemically Active Inhibitors of Intracellular Acid Ceramidase 下载免费PDF全文
Dr. Natalia Realini Dr. Andrea Armirotti Dr. Luisa Mengatto Dr. Inga Bauer Dr. Stefania Girotto Dr. Chiara Pagliuca Dr. Marco De Vivo Dr. Maria Summa Dr. Alison Ribeiro Prof. Daniele Piomelli 《Angewandte Chemie (International ed. in English)》2015,54(2):485-489
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. 相似文献
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Srijanani Bhaskar Jonathon Hitt Sei‐Won Laura Chang Joerg Lahann Prof. 《Angewandte Chemie (International ed. in English)》2009,48(25):4452-4452
Multicompartmental microcylinders can be produced by a combination of electrohydrodynamic co‐spinning and microsectioning, as described by J. Lahann et al. in their Communication on page 4589 ff. The number of individual compartments, relative compartment orientation, chemical composition and functionality, and aspect ratio can be precisely tuned. Each color in the longitudinal and cross‐sectional micrograph images depicts an individual compartment.
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Inside Cover: Trimethylaluminum: Bonding by Charge and Current Topology (Angew. Chem. Int. Ed. 46/2015) 下载免费PDF全文
Dr. Hans‐Georg Stammler M. Sc. Sebastian Blomeyer Priv.‐Doz. Dr. Raphael J. F. Berger Prof. Dr. Norbert W. Mitzel 《Angewandte Chemie (International ed. in English)》2015,54(46):13470-13470
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Inside Cover: Coordination Assembly of Discoid Nanoparticles (Angew. Chem. Int. Ed. 31/2015) 下载免费PDF全文
Dr. Kenji Hirai Dr. Bongjun Yeom Dr. Shu‐Hao Chang Dr. Hang Chi Dr. John F. Mansfield Dr. Byeongdu Lee Sungsik Lee Prof. Ctirad Uher Prof. Dr. Nicholas A. Kotov 《Angewandte Chemie (International ed. in English)》2015,54(31):8850-8850
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Cheng Fan WarrenE. Piers Masood Parvez 《Angewandte Chemie (International ed. in English)》2009,48(16):2808-2808
Perfluoroaryl boranes are an important class of organometallic Lewis acids. The synthesis of perfluorinated compounds brings special challenges to tried‐and‐true synthetic methodologies. In their Communication on page 2955 ff., W. E. Piers and co‐workers present the synthesis of a new, fully fluorinated heterocyclic borane that is also a member of the rare antiaromatic borole class of compounds. The route relies on normally facile transmetallation reactions made more difficult by the electron‐withdrawing C6F5 groups of the target product.
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Dr. Michael Georg Hoesl M. Sc. Stefan Oehm Dr. Patrick Durkin Dr. Elise Darmon Dr. Lauri Peil Dr. Hans‐Rudolf Aerni Prof. Dr. Juri Rappsilber Prof. Dr. Jesse Rinehart Prof. Dr. David Leach Prof. Dr. Dieter Söll Prof. Dr. Nediljko Budisa 《Angewandte Chemie (International ed. in English)》2015,54(34):9726-9726