Pretubulysin, a potent and chemically accessible tubulysin precursor from Angiococcus disciformis

Angew Chem Int Ed Engl. 2009;48(24):4422-5. doi: 10.1002/anie.200900406.

Abstract

Simplify, simplify, simplify! Pretubulysin (structure without the green substituents), a simplified tubulysin was prepared in the laboratory and also found in a natural myxobacterial source. This biosynthetic precursor of the tubulysins is not as active as tubulysins A and D but is still effective in picomolar concentrations against cancer cell lines.

MeSH terms

  • Amino Acid Sequence
  • Antineoplastic Agents / chemical synthesis*
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology
  • Cell Line, Tumor
  • Drug Screening Assays, Antitumor
  • Humans
  • Myxococcales / chemistry*
  • Oligopeptides / chemical synthesis
  • Oligopeptides / chemistry*
  • Prodrugs / chemical synthesis
  • Prodrugs / chemistry
  • Protein Precursors / chemical synthesis*
  • Protein Precursors / chemistry
  • Protein Precursors / pharmacology

Substances

  • Antineoplastic Agents
  • Oligopeptides
  • Prodrugs
  • Protein Precursors