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A unique mode of microtubule stabilization induced by peloruside A.
TLDR
It is suggested that taxoid-site ligands epothilone A and docetaxel stabilize microtubules primarily through improved longitudinal interactions centered on the interdimer interface, with no observable contributions from lateral interactions between protofilaments. Expand
CONFORMATIONAL PROPERTIES OF EPOTHILONE
The epothilones are macrolide natural products, produced by myxobacterium Sorangium cellulosum (So ce 90), which mimic the biological activity of the anticancer agent Taxol. These interestingExpand
Mutations in the β-tubulin binding site for peloruside A confer resistance by targeting a cleft significant in side chain binding
TLDR
Four resistant lines of the human ovarian carcinoma cell line A2780(1A9) are described with single-base mutations in class I β-tubulin that result in the following substitutions: R306H, Y340S, N337D, and A296S in various combinations. Expand
Elucidation of gephyronic acid biosynthetic pathway revealed unexpected SAM-dependent methylations.
TLDR
The identification of the gene cluster sets the stage for the generation of a heterologous expression system, which will allow further investigation of selective eukaryotic protein synthesis inhibitors through thegeneration of gephyronic acid analogues. Expand
Draft Genome Sequence of Gephyronic Acid Producer Cystobacter violaceus Strain Cb vi76
ABSTRACT A draft genome sequence of Cystobacter violaceus strain Cb vi76, which produces the eukaryotic protein synthesis inhibitor gephyronic acid, has been obtained. The genome contains numerousExpand
Conformation-activity relationships in polyketide natural products: a new perspective on the rational design of epothilone analogues.
TLDR
Conformational analysis using computational methods, X-ray crystallography, and NMR studies showed that the stereochemistry at C14 has a pronounced effect on the conformation of the epoxide region of epothilone. Expand
Total synthesis of (+)-peloruside A.
TLDR
A total synthesis of (+)-peloruside A has been successfully achieved by a late stage aldol coupling of two complex fragments followed by an intramolecular hemi-ketal cyclization, a MOM group participated epoxide ring fragmentation reaction, and a highly selective methylation. Expand
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