Open-chain half-bastadins mimic the effects of cyclic bastadins on calcium homeostasis in cultured neurons

Constraining the catechol aryl ether moiety of bastadins by incorporation into a macrocyle is not necessary in order to mimic the effects of these marine natural products on neuronal calcium homeostasis. Simple, acyclic analogs that embody the ‘western’ or ‘eastern’ parts of bastadins were found to...

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Veröffentlicht in:	Bioorganic & medicinal chemistry 2008-11, Vol.18 (21), p.5734-5737
Hauptverfasser:	Zieminska, Elzbieta, Lazarewicz, Jerzy W., Couladouros, Elias A., Moutsos, Vassilios I., Pitsinos, Emmanuel N.
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Bastadins Biological and medical sciences Calcium - metabolism Calcium channels Cells, Cultured Cerebellar granule cells Cyclization Diaryl ether Halogenated Diphenyl Ethers - chemistry Halogenated Diphenyl Ethers - pharmacology Homeostasis - drug effects Medical sciences Miscellaneous Neurons - drug effects Neurons - metabolism Neuropharmacology Pharmacology. Drug treatments Protein Conformation Rats Ryanodine
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Zusammenfassung:	Constraining the catechol aryl ether moiety of bastadins by incorporation into a macrocyle is not necessary in order to mimic the effects of these marine natural products on neuronal calcium homeostasis. Simple, acyclic analogs that embody the ‘western’ or ‘eastern’ parts of bastadins were found to evoke comparable responses with bastadin 5.
ISSN:	0960-894X 0968-0896 1464-3405 1464-3391
DOI:	10.1016/j.bmcl.2008.09.080