Functional characterization of peanut serine/threonine/tyrosine protein kinase: molecular docking and inhibition kinetics with tyrosine kinase inhibitors

Biochemistry
Parvathi Rudrabhatla, Ram Rajasekharan

Abstract

Serine/threonine/tyrosine (STY) protein kinase from peanut is developmentally regulated and is induced by abiotic stresses. In addition, STY protein kinase activity is regulated by tyrosine phosphorylation. Kinetic mechanism of plant dual specificity protein kinases is not studied so far. Recombinant STY protein kinase occurs as a monomer in solution as shown by gel filtration chromatography. The relative phosphorylation rate of kinase against increasing enzyme concentrations follows a first-order kinetics indicating an intramolecular phosphorylation mechanism. Moreover, the active recombinant STY protein kinase could not transphosphorylate a kinase-deficient mutant of STY protein kinase. Molecular docking studies revealed that the tyrosine kinase inhibitors bind the protein kinase at the same region as ATP. STY protein kinase activity was inhibited by the tyrosine kinase inhibitors, and the inhibitor potency series against the recombinant STY protein kinase was tyrphostin > genistein > staurosporine. The inhibition constant (K(i)), and the IC(50) value of STY protein kinase for tyrosine kinase inhibitors with ATP and histone are discussed. All the inhibitors competed with ATP. Genistein was an uncompetitive inhibitor with hist...Continue Reading

References

Jan 16, 1987·Science·J M Bishop
Sep 1, 1995·Trends in Biochemical Sciences·R A Sayle, E J Milner-White
Nov 1, 1994·European Journal of Biochemistry·N Osherov, A Levitzki
Sep 1, 1994·European Journal of Biochemistry·J VeselýS Leclerc
Aug 1, 1996·Journal of Computer-aided Molecular Design·G M MorrisA J Olson
Jun 23, 1998·The Journal of Biological Chemistry·G SessaG B Martin

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Citations

Jan 24, 2006·Plant Molecular Biology·Parvathi RudrabhatlaRam Rajasekharan
Aug 23, 2007·PloS One·Sander H DiksMaikel P Peppelenbosch
Aug 13, 2009·PloS One·Tita RitsemaMaikel P Peppelenbosch
Feb 13, 2007·Archives of Biochemistry and Biophysics·Mamatha M Reddy, Ram Rajasekharan
Oct 24, 2006·Archives of Biochemistry and Biophysics·Mamatha M Reddy, Ram Rajasekharan
Jan 1, 2013·3 Biotech·Priya Batra, Anil K Sharma
Jun 2, 2011·Plant Signaling & Behavior·Thanos Ghelis

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