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

Theresa A. Lansdell; Nicole M. Hewlett; Amanda P. Skoumbourdis; Matthew D. Fodor; Ian B. Seiple; Shun Su; Phil S. Baran; Ken S. Feldman; Jetze J. Tepe

doi:10.1021/np300231f

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

Theresa A. Lansdell, Nicole M. Hewlett, Amanda P. Skoumbourdis, Matthew D. Fodor, Ian B. Seiple, Shun Su, Phil S. Baran, Ken S. Feldman, Jetze J. Tepe

Chemistry

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43 Scopus citations

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 ⁱ20S 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.

Original language	English (US)
Pages (from-to)	980-985
Number of pages	6
Journal	Journal of Natural Products
Volume	75
Issue number	5
DOIs	https://doi.org/10.1021/np300231f
State	Published - May 25 2012

All Science Journal Classification (ASJC) codes

Analytical Chemistry
Molecular Medicine
Pharmacology
Pharmaceutical Science
Drug Discovery
Complementary and alternative medicine
Organic Chemistry

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10.1021/np300231f

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title = "Palau'amine and related oroidin alkaloids dibromophakellin and dibromophakellstatin inhibit the human 20s proteasome",

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 i20S 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.",

author = "Lansdell, {Theresa A.} and Hewlett, {Nicole M.} and Skoumbourdis, {Amanda P.} and Fodor, {Matthew D.} and Seiple, {Ian B.} and Shun Su and Baran, {Phil S.} and Feldman, {Ken S.} and Tepe, {Jetze J.}",

year = "2012",

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doi = "10.1021/np300231f",

language = "English (US)",

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T1 - Palau'amine and related oroidin alkaloids dibromophakellin and dibromophakellstatin inhibit the human 20s proteasome

AU - Lansdell, Theresa A.

AU - Hewlett, Nicole M.

AU - Skoumbourdis, Amanda P.

AU - Fodor, Matthew D.

AU - Seiple, Ian B.

AU - Su, Shun

AU - Baran, Phil S.

AU - Feldman, Ken S.

AU - Tepe, Jetze J.

PY - 2012/5/25

Y1 - 2012/5/25

N2 - 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 i20S 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.

AB - 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 i20S 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.

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JO - Journal of Natural Products

JF - Journal of Natural Products

IS - 5

ER -

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

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