Suramin and the suramin analogue NF307 discriminate among calmodulin-binding sites

The Biochemical Journal
M KlingerM Hohenegger

Abstract

Calmodulin-binding sites on target proteins show considerable variation in primary sequence; hence compounds that block the access of calmodulin to these binding sites may be more selective than compounds that inactivate calmodulin. Suramin and its analogue NF307 inhibit the interaction of calmodulin with the ryanodine receptor. We have investigated whether inhibition of calmodulin binding to target proteins is a general property of these compounds. Suramin inhibited binding of [(125)I]calmodulin to porcine brain membranes and to sarcoplasmic reticulum from skeletal muscle (IC(50)=4.9+/-1.2 microM and 19.9+/-1.8 microM, respectively) and blocked the cross-linking of [(125)I]calmodulin to some, but not all, target proteins in brain membranes by [(125)I]calmodulin. Four calmodulin-binding proteins were purified [ryanodine receptor-1 (RyR1) from rabbit skeletal muscle, neuronal NO synthase (nNOS) from Sf9 cells, G-protein betagamma dimers (Gbetagamma) from porcine brain and a glutathione S-transferase-fusion protein comprising the C-terminal calmodulin-binding domain of the metabotropic glutamate receptor 7A (GST-CmGluR7A) from bacterial lysates]. Three of the proteins employed (Gbetagamma, GST-CmGluR7A and RyR1) display a compara...Continue Reading

Citations

Aug 2, 2005·British Journal of Pharmacology·Ilse WolnerMartin Hohenegger
Feb 18, 2009·British Journal of Pharmacology·C SigalasR Sitsapesan
Mar 27, 2012·Journal of Molecular Biology·Eloise MastrangeloMario Milani
Nov 10, 2011·Biophysical Journal·Tao GuoDonald M Bers
Sep 27, 2013·Applied Biochemistry and Biotechnology·Fuminori YamaguchiRyoji Kobayashi
Oct 5, 2002·The Journal of Biological Chemistry·Rao V L PapineniSusan L Hamilton
Dec 31, 2003·The Journal of Biological Chemistry·Angela F DulhuntyMarco G Casarotto
Aug 14, 2001·The Journal of Biological Chemistry·S SencerS L Hamilton
Mar 6, 2003·Cellular Signalling·Danton H O'Day

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