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Inhibition of protein kinases by balanol: Specificity within the serine/threonine protein kinase subfamily

Academic Article
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Overview

authors

  • Setyawan, J.
  • Koide, K.
  • Diller, T. C.
  • Bunnage, M. E.
  • Taylor, S. S.
  • Nicolaou, K.C.
  • Brunton, L. L.

publication date

  • August 1999

journal

  • Molecular Pharmacology  Journal

abstract

  • Balanol is a potent inhibitor of cyclic AMP-dependent protein kinase and protein kinase C, acting competitively with ATP with an affinity 3000 times that of ATP. We tested the capacity of balanol to inhibit representative serine- and threonine-specific protein kinases from the protein kinase subfamily that shares a common conserved catalytic core with cyclic AMP-dependent protein kinase. Balanol's pattern of interactions indicates considerable diversity of the ATP/balanol-binding sites of protein kinases within familial groups and even among isoforms of the same kinase. We propose that balanol is a protean structure that may be modified to produce selective, high-affinity inhibitors and probes of the ATP-binding sites of serine/threonine protein kinases.

subject areas

  • Adenosine Triphosphate
  • Adenylyl Cyclases
  • Azepines
  • Calcium-Calmodulin-Dependent Protein Kinases
  • Catalytic Domain
  • Cells, Cultured
  • Enzyme Inhibitors
  • GTP-Binding Protein alpha Subunits, Gs
  • HeLa Cells
  • Humans
  • Hydroxybenzoates
  • Isoenzymes
  • Protein-Serine-Threonine Kinases
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Identity

International Standard Serial Number (ISSN)

  • 0026-895X

PubMed ID

  • 10419556
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Additional Document Info

start page

  • 370

end page

  • 376

volume

  • 56

issue

  • 2

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