Evaluation of the tubulin-bound paclitaxel conformation: synthesis, biology, and SAR studies of C-4 to C-3' bridged paclitaxel analogues.

Evaluation of the tubulin-bound paclitaxel conformation: synthesis, biology, and SAR studies of C-4 to C-3' bridged paclitaxel analogues. Research Abstract Details 

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Evaluation of the tubulin-bound paclitaxel conformation: synthesis, biology, and SAR studies of C-4 to C-3' bridged paclitaxel analogues. Abstract Text:

Thota Ganesh,Chao Yang,Andrew Norris,Tom Glass,Susan Bane,Rudravajhala Ravindra,Abhijit Banerjee,Belhu Metaferia,Shala L Thomas,Paraskevi Giannakakou,Ana A Alcaraz,Ami S Lakdawala,James P Snyder,David G I Kingston,

The important anticancer drug paclitaxel binds to the beta-subunit of the alphabeta-tubulin dimer in the microtubule in a stoichiometric ratio, promoting microtubule polymerization and stability. The conformation of microtubule-bound drug has been the subject of intense study, and various suggestions have been proposed. In previous work we presented experimental and theoretical evidence that paclitaxel adopts a T-shaped conformation when it is bound to tubulin. In this study we report additional experimental data and calculations that delineate the allowable parameters for effective paclitaxel-tubulin interactions.

Evaluation of the tubulin-bound paclitaxel conformation: synthesis, biology, and SAR studies of C-4 to C-3' bridged paclitaxel analogues. Publishing Authors By Initials

T Ganesh,C Yang,A Norris,T Glass,S Bane,R Ravindra,A Banerjee,B Metaferia,SL Thomas,P Giannakakou,AA Alcaraz,AS Lakdawala,JP Snyder,DG Kingston,

For similar macromolecular substances: polymers: biopolymers: microtubule proteins: tubulin research abstracts see: macromolecular substances: polymers: biopolymers: microtubule proteins: tubulin research

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Evaluation of the tubulin-bound paclitaxel conformation: synthesis, biology, and SAR studies of C-4 to C-3' bridged paclitaxel analogues. Journal Published:

PUBLICATION TYPE: Research Support, N.I.H., Extr

Journal: Journal of medicinal chemistry

VOLUME: 50

Page Numbers: 713-25

Journal Abbreviation: J. Med. Chem.

ISSN: 0022-2623

DAY: 31

MONTH: 01

YEAR: 2007

Evaluation of the tubulin-bound paclitaxel conformation: synthesis, biology, and SAR studies of C-4 to C-3' bridged paclitaxel analogues. Information

Number of References:

LANGUAGE: eng

NlmUniqueID: 9716531

Evaluation of the tubulin-bound paclitaxel conformation: synthesis, biology, and SAR studies of C-4 to C-3' bridged paclitaxel analogues. Keywords Mesh Terms:

KEYWORDS: Tubulin

MESH TERMS: chemistry

Chemical & Substance for Abstract: Evaluation of the tubulin-bound paclitaxel conformation: synthesis, biology, and SAR studies of C-4 to C-3' bridged paclitaxel analogues. Information

Substance Name: Paclitaxel

Registry Number: 33069-62-4

Grant and Affiliation Information for Evaluation of the tubulin-bound paclitaxel conformation: synthesis, biology, and SAR studies of C-4 to C-3' bridged paclitaxel analogues.

AFFILIATION: Department of Chemistry, M/C 0212, Virginia Polytechnic Institute and State University, Blacksburg, Virginia 24061, USA.

Country: United States

AGENCY: United States NCI

GRANT: CA-69571

ACRONYM: CA

MEDLINETA: J Med Chem

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