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Article

Mutations in the β-tubulin binding site for peloruside A confer resistance by targeting a cleft significant in side chain binding.

Cell cycle (Georgetown, Tex.) - 1 Oct 2011

Begaye Adrian, Trostel Shana, Zhao Zhiming, Taylor Richard E, Schriemer David C, Sackett Dan L

Abstract excerpt

Peloruside A is a microtubule-stabilizing macrolide that binds to beta tubulin at a site distinct from the taxol site. The site was previously identified by H-D exchange mapping and molecular docking as a region close to the outer surface of the microtubule and confined in a cavity surrounded by a continuous loop of protein folded so as to center on Y340. We have isolated a series of peloruside A-resistant lines...

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Share to Amino Acid Substitution
Share to Bridged Bicyclo Compounds, Heterocyclic

Methodology Data sources Editorial policy Privacy About Contact Helena Bioinformatics

Share to Deuterium Exchange Measurement

Share to Drug Resistance, Neoplasm

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Identifiers

PMID: 21926482
DOI: 10.4161/cc.10.19.17706
PMCID: PMC3233629

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