Literature DB >> 24900591

A structurally simplified analogue of geldanamycin exhibits neuroprotective activity.

Manikandadas M Madathil1, Omar M Khdour1, Jennifer Jaruvangsanti1, Sidney M Hecht1.   

Abstract

The syntheses of a structurally simplified geldanamycin analogue 2 and two related compounds are described. Compound 2 conferred cytoprotection and quenched ROS and lipid peroxidation in a dose-dependent manner in Friedreich's ataxia (FRDA) lymphocytes at low micromolar concentrations. It also prevented ROS-induced damage of cellular lipid membranes and maintained the mitochondrial membrane potential of FRDA lymphocytes. In addition, 2 did not inhibit Hsp90 when tested at micromolar concentrations, exhibited no cytotoxicity, and afforded neuroprotection to differentiated SH-SY5Y cells under conditions of Aβ-induced cell toxicity.

Entities:  

Keywords:  Geldanamycin; lipid peroxidation; mitochondria; oxidative stress

Year:  2013        PMID： 24900591      PMCID： PMC4027499          DOI： 10.1021/ml400207m

Source DB:  PubMed          Journal:  ACS Med Chem Lett        ISSN： 1948-5875            Impact factor:   4.345


  41 in total

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Authors:  Gregor P C Drummen; Lydia C M van Liebergen; Jos A F Op den Kamp; Jan A Post
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Review 2.  Energy deficit in Huntington disease: why it matters.

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3.  Synthetic ansamycins prepared by a ring-expanding Claisen rearrangement. Synthesis and biological evaluation of ring and conformational analogues of the Hsp90 molecular chaperone inhibitor geldanamycin.

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Journal:  Org Biomol Chem       Date:  2007-01-04       Impact factor: 3.876

4.  A non-toxic Hsp90 inhibitor protects neurons from Abeta-induced toxicity.

Authors:  Sabah Ansar; Joseph A Burlison; M Kyle Hadden; Xiao Ming Yu; Kelly E Desino; Jennifer Bean; Len Neckers; Ken L Audus; Mary L Michaelis; Brian S J Blagg
Journal:  Bioorg Med Chem Lett       Date:  2007-01-17       Impact factor: 2.823

5.  Membrane potential can be determined in individual cells from the nernstian distribution of cationic dyes.

Authors:  B Ehrenberg; V Montana; M D Wei; J P Wuskell; L M Loew
Journal:  Biophys J       Date:  1988-05       Impact factor: 4.033

6.  Potent and specific inhibition of glutathione synthesis by buthionine sulfoximine (S-n-butyl homocysteine sulfoximine).

Authors:  O W Griffith; A Meister
Journal:  J Biol Chem       Date:  1979-08-25       Impact factor: 5.157

7.  Synthesis and evaluation of geldanamycin-estradiol hybrids.

Authors:  S D Kuduk; F F Zheng; L Sepp-Lorenzino; N Rosen; S J Danishefsky
Journal:  Bioorg Med Chem Lett       Date:  1999-05-03       Impact factor: 2.823

8.  Neuroprotective activity and evaluation of Hsp90 inhibitors in an immortalized neuronal cell line.

Authors:  Yuanming Lu; Sabah Ansar; Mary L Michaelis; Brian S J Blagg
Journal:  Bioorg Med Chem       Date:  2008-12-25       Impact factor: 3.641

9.  Toxic consequence of the abrupt depletion of glutathione in cultured rat hepatocytes.

Authors:  S Miccadei; M E Kyle; D Gilfor; J L Farber
Journal:  Arch Biochem Biophys       Date:  1988-09       Impact factor: 4.013

10.  Synthesis and biological activities of N-(3-carboxylpropyl)-5-amino-2-hydroxy-3-tridecyl-1,4-benzoquinone and analogues.

Authors:  Manikandadas M Madathil; Omar M Khdour; Jennifer Jaruvangsanti; Sidney M Hecht
Journal:  J Nat Prod       Date:  2012-11-28       Impact factor: 4.050
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  1 in total

1.  Functionally Optimized Neuritogenic Farinosone C Analogs: SAR-Study and Investigations on Their Mode of Action.

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Journal:  ACS Med Chem Lett       Date:  2013-12-06       Impact factor: 4.345
  1 in total

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