Synthetic anisomycin analogues activating the JNK/SAPK1 and p38/SAPK2 pathways.
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.
Rosser
Edward M
EM
MRC Protein Phosphorylation Unit, Division of Cell Signalling, School of Life Sciences, University of Dundee, Dundee, UKDD1 5EH.
Morton
Simon
S
Ashton
Kate S
KS
Cohen
Philip
P
Hulme
Alison N
AN
D000818:Animals; D000841:Anisomycin / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry; D002460:Cell Line; D004789:Enzyme Activation; D020935:MAP Kinase Signaling System; D008264:Macrophages / Q000187:drug effects / Q000201:enzymology; D051379:Mice; D048055:Mitogen-Activated Protein Kinase 8; D020928:Mitogen-Activated Protein Kinases / Q000378:metabolism*; D048051:p38 Mitogen-Activated Protein Kinases
D000841:Anisomycin; D048055:Mitogen-Activated Protein Kinase 8; D020928:Mitogen-Activated Protein Kinases; D048051:p38 Mitogen-Activated Protein Kinases