Synthetic anisomycin analogues activating the JNK/SAPK1 and p38/SAPK2 pathways.

Org Biomol Chem

MRC Protein Phosphorylation Unit, Division of Cell Signalling, School of Life Sciences, University of Dundee, Dundee, UKDD1 5EH.

Published: January 2004

AI Article Synopsis

  • - The study focuses on creating analogues of anisomycin, a compound that activates the JNK/p38 signaling pathways, specifically through modifications at the C(4) position using aldol or Claisen reactions.
  • - Researchers tested these new C(4) analogues, along with earlier synthetic forms, to evaluate their effectiveness in activating the JNK/SAPK1 and p38/SAPK2 pathways in RAW macrophages by using immunoblot assays.
  • - Results indicate that certain synthetic C(4) analogues are strong activators of the stress kinase pathways, suggesting they could potentially be valuable for further research or therapeutic development.

Article Abstract

The synthesis of C(4)H and C(4)Me analogues of the JNK/p38 pathway activator anisomycin, based upon an aldol or Claisen construction of the C(3)-C(4) bond, has been demonstrated. The relative activation of the JNK/SAPK1 and p38/SAPK2 pathways in RAW macrophages by these analogues, and their synthetic precursors, has been assessed using immunoblot assays against phosphorylated c-Jun and MAPKAP-K2. These studies demonstrate that some of the synthetic C(4) analogues are also potent activators of these stress kinase pathways.

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http://dx.doi.org/10.1039/b311242jDOI Listing

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Synthetic anisomycin analogues activating the JNK/SAPK1 and p38/SAPK2 pathways.

Org Biomol Chem

January 2004

MRC Protein Phosphorylation Unit, Division of Cell Signalling, School of Life Sciences, University of Dundee, Dundee, UKDD1 5EH.

The synthesis of C(4)H and C(4)Me analogues of the JNK/p38 pathway activator anisomycin, based upon an aldol or Claisen construction of the C(3)-C(4) bond, has been demonstrated. The relative activation of the JNK/SAPK1 and p38/SAPK2 pathways in RAW macrophages by these analogues, and their synthetic precursors, has been assessed using immunoblot assays against phosphorylated c-Jun and MAPKAP-K2. These studies demonstrate that some of the synthetic C(4) analogues are also potent activators of these stress kinase pathways.

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