Chemistry and biology of tubulysins: antimitotic tetrapeptides with activity against drug resistant cancers

  • Nat Prod Rep. 2015 May;32(5):654-62. doi: 10.1039/c4np00036f.
Bryan C Murray  1 ,  Michael T Peterson ,  Robert A Fecik
Affiliations
  • 1. University of Minnesota, Medicinal Chemistry, 8-101 Weaver Densford Hall, 308 Harvard Street S.E, Minneapolis, Minnesota 55455, USA.
PMID: 25677951 DOI: 10.1039/c4np00036f
Abstract

Since their first report in 2000, tubulysins have sparked great interest for development as anti-cancer agents due to their exceptionally potent antiproliferative activity. Progress in the discovery and development of tubulysins, especially tubulysin conjugates, has quickly advanced despite limitations in their availability from Nature. In this Highlight, the key research on the isolation and structure determination, biosynthesis, bioactivity, structure-activity relationships (SAR), synthesis, and conjugates of tubulysins is presented.

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