title: Chemistry and biology of tubulysins: antimitotic tetrapeptides with activity against drug resistant cancers.
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.
authors: University of Minnesota, Medicinal Chemistry, 8-101 Weaver Densford Hall, 308 Harvard Street S.E, Minneapolis, Minnesota 55455, USA.
authors: Bryan C
authors: BC
authors: Murray
authors: Michael T
authors: MT
authors: Peterson
authors: Robert A
authors: RA
authors: Fecik
mesh_terms: D050256:Antimitotic Agents / Q000737:chemistry* / Q000494:pharmacology*; D006801:Humans; D015394:Molecular Structure; D009842:Oligopeptides / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D050256:Antimitotic Agents; D009842:Oligopeptides; C510756:tubulysin A