S. Rath, J. Liebl, R. Fürst
Nov 1, 2012
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Journal
British Journal of Pharmacology
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).