[Lys3]Didemnins as potential affinity ligands.
The synthesis and biological activity of N(epsilon)-Z-[Lys3]didemnin B are reported. This novel analogue retains antiproliferative, cytotoxic, and protein biosynthesis inhibition activities, but at reduced levels. This result suggests the use of [Lys3]didemnin derivatives as potential affinity probes for studying the molecular target(s) of the didemnin class of natural products.
Vera
M D
MD
Department of Chemistry, University of Pennsylvania, Philadelphia 19104-6323, USA.
Pfizenmayer
A J
AJ
Ding
X
X
Xiao
D
D
Joullié
M M
MM
D000345:Affinity Labels / Q000138:chemical synthesis* / Q000378:metabolism* / Q000494:pharmacology / Q000633:toxicity; D002455:Cell Division / Q000187:drug effects; D047630:Depsipeptides; D006801:Humans; D020128:Inhibitory Concentration 50; D008024:Ligands; D015394:Molecular Structure; D010456:Peptides, Cyclic / Q000138:chemical synthesis* / Q000378:metabolism* / Q000494:pharmacology / Q000633:toxicity; D014176:Protein Biosynthesis; D014407:Tumor Cells, Cultured
D000345:Affinity Labels; D047630:Depsipeptides; D008024:Ligands; D010456:Peptides, Cyclic; C030051:didemnins