Characterization and regulation of the expression of scyllatoxin (Leiurotoxin I) receptors in the human neuroblastoma cell line NB-OK 1

125I-[Tyr 2]scyllatoxin allowed to label a single class of high-affinity receptors in membranes from the human neuroblastoma cell line NB-OK 1. The K d of these receptors was 60 pM for scyllatoxin (Leiurotoxin I) and 20 pM for apamin and the B max was low (3.8 fmol/mg membrane protein). K + increase...

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Veröffentlicht in:	FEBS letters 1991-07, Vol.285 (2), p.271-274
Hauptverfasser:	Gossen, Denis, Gesquière, Jean-Claude, Tastenoy, Michèle, Neef, Philippe De, Waelbroeck, Magali, Christophe, Jean
Format:	Artikel
Sprache:	eng
Schlagworte:	1C50 Amino Acid Sequence Apamin Apamin - antagonists & inhibitors Apamin - metabolism Biological and medical sciences Butyrate Butyrates - pharmacology Butyric Acid Ca 2+-activated K + channel Ca2+-activated K+ channel Calcium - metabolism Cell Membrane - metabolism Cell receptors Cell structures and functions concentration required for half-maximal inhibition of tracer binding concentration required for half-maximal occupancy of binding sites with tracer Cycloheximide - pharmacology Fundamental and applied biological sciences. Psychology Gene Expression Regulation - drug effects Guanidine Guanidines - metabolism Human neuroblastoma cell line NB-OK 1 Humans K d Kinetics Miscellaneous Molecular and cellular biology Molecular Sequence Data Neuroblastoma Potassium - metabolism Potassium Channels Radioligand Assay Receptors, Cholinergic - drug effects Receptors, Cholinergic - metabolism Scorpion Venoms - metabolism scyllatoxin Scyllatoxin (Leiurotoxin I) Sodium - metabolism Tumor Cells, Cultured
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Zusammenfassung:	125I-[Tyr 2]scyllatoxin allowed to label a single class of high-affinity receptors in membranes from the human neuroblastoma cell line NB-OK 1. The K d of these receptors was 60 pM for scyllatoxin (Leiurotoxin I) and 20 pM for apamin and the B max was low (3.8 fmol/mg membrane protein). K + increased toxin binding at low concentrations but exerted opposite effects at high concentrations. Ca 2+, guanidinium and Na + exerted only inhibitory effects on binding. Scyllatoxin binding sites were overexpressed 2.5-fold after a 24-h cell pretreatment with 2 mM butyrate. This effect was suppressed by cycloheximide.
ISSN:	0014-5793 1873-3468
DOI:	10.1016/0014-5793(91)80815-K