Anti-angiogenic effects of the tubulysin precursor pretubulysin and of simplified pretubulysin derivatives.

ABSTRACT:

Background and purpose

The use of tubulin-binding compounds, which act in part by inhibiting tumour angiogenesis, has become an integral strategy of tumour therapy. Recently, tubulysins were identified as a novel class of natural compounds of myxobacterial origin, which inhibit tubulin polymerization. As these compounds are structurally highly complex, the search for simplified precursors [e.g. pretubulysin (Prt)] and their derivatives is mandatory to overcome supply problems hampering clinical development. We tested the anti-angiogenic efficacy of Prt and seven of its derivatives in comparison to tubulysin A (TubA).

Experimental approach

The compounds were tested in cellular angiogenesis assays (proliferation, cytotoxicity, cell cycle, migration, chemotaxis, tube formation)

SUBMITTER: Rath S 

PROVIDER: S-EPMC3492986 | biostudies-literature | 2012 Nov

REPOSITORIES: biostudies-literature