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A galanin-mastoparan chimeric peptide activates the Na+,K(+)-ATPase and reverses its inhibition by ouabain

Academic Article
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Overview

authors

  • Langel, Ülo
  • Pooga, M.
  • Kairane, C.
  • Zilmer, M.
  • Bartfai, Tamas

publication date

  • April 1996

journal

  • Regulatory Peptides  Journal

abstract

  • The effect of the neuropeptide galanin, the wasp venom toxin amphiphilic peptide toxin mastoparan and the chimeric peptide, galparan, consisting of N-terminal 13 amino acids of neuropeptide galanin linked at C-terminus to mastoparan amide (and its inactive analog Mas17) on the activity of Na+,K(+)-ATPase has been studied. Mastoparan inhibits the activity of the Na+,K(+)-ATPase with IC50 = 7.5 microM and also reduces the cooperativity for Na+ and K+, respectively, while galanin has no effect on the Na+,K(+)-ATPase activity. The chimeric peptide, galanin(1-13)-mastoparan amide (galparan), exhibits biphasic interaction with Na+,K(+)-ATPase, it activates the enzyme at maximal stimulating concentration of 4 microM followed by inhibition of the enzyme with IC50 of 100 microM. At maximum stimulating concentration (4 microM), galparan partly reduces the cooperativity only for Na+ and it also counteracts the inhibitory effect of oubain on Na+,K(+)-ATPase. Galparan's stimulatory effect was influenced by ATP. The chimeric peptide [19Lys,26Leu]-galparan, containing the inactive analog of mastoparan (Mas17), has no effects on rat brain Na+,K(+)-ATPase activity. Both chimeric peptides galparan and [19Lys,26Leu]-galparan are high-affinity galanin receptor ligands with IC50 of 6.4 nM and 0.71 nM, respectively, while galanin (1-13) and mastoparan alone have significantly lower affinity for the galanin receptor, IC50 of 125 nM and 1 microM, respectively. The ability of chimeric peptides to bind to galanin receptors does not correlate with their effects on the Na+,K(+)-ATPase.

subject areas

  • Amino Acid Sequence
  • Animals
  • Binding Sites
  • Dose-Response Relationship, Drug
  • Enzyme Activation
  • Enzyme Inhibitors
  • Frontal Lobe
  • Galanin
  • Lethal Dose 50
  • Molecular Sequence Data
  • Ouabain
  • Peptides
  • Rats
  • Rats, Wistar
  • Receptors, Galanin
  • Receptors, Gastrointestinal Hormone
  • Recombinant Fusion Proteins
  • Sodium-Potassium-Exchanging ATPase
  • Swine
  • Wasp Venoms
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Research

keywords

  • Na+,K+-ATPase
  • amphiphilic helix
  • galanin
  • mastoparan
  • receptor
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Identity

International Standard Serial Number (ISSN)

  • 0167-0115

Digital Object Identifier (DOI)

  • 10.1016/0167-0115(96)00002-x

PubMed ID

  • 8738882
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Additional Document Info

start page

  • 47

end page

  • 52

volume

  • 62

issue

  • 1

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