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Palau'amine and related oroidin alkaloids dibromophakellin and dibromophakellstatin inhibit the human 20s proteasome

Academic Article
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Overview

related to degree

  • Seiple, Ian, Ph.D. in Chemistry, Scripps Research 2006 - 2011

authors

  • Lansdell, T. A.
  • Hewlett, N. M.
  • Skoumbourdis, A. P.
  • Fodor, M. D.
  • Seiple, Ian
  • Su, S.
  • Baran, Phil
  • Feldman, K. S.
  • Tepe, J. J.

publication date

  • May 2012

journal

  • Journal of Natural Products  Journal

abstract

  • We report herein that the oroidin-derived alkaloids palau'amine (1), dibromophakellin (2), and dibromophakellstatin (3) inhibit the proteolytic activity of the human 20S proteasome as well as the (i)20S immunoproteasome catalytic core. Palau'amine is found to prevent the degradation of ubiquitinylated proteins, including IκBα, in cell culture, which may be indicative of the potential mechanism by which these agents exhibit their exciting cytotoxic and immunosuppressive properties.

subject areas

  • Alkaloids
  • Guanidines
  • HeLa Cells
  • Heterocyclic Compounds with 4 or More Rings
  • Humans
  • Imidazoles
  • Microscopy, Confocal
  • NF-kappa B
  • Proteasome Endopeptidase Complex
  • Proteasome Inhibitors
  • Pyrroles
  • Spiro Compounds
  • Stereoisomerism
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Identity

PubMed Central ID

  • PMC3367325

International Standard Serial Number (ISSN)

  • 0163-3864

Digital Object Identifier (DOI)

  • 10.1021/np300231f

PubMed ID

  • 22591513
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Additional Document Info

start page

  • 980

end page

  • 985

volume

  • 75

issue

  • 5

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