T-Taxol and the electron crystallographic density in beta-tubulin.
[chemical structure: see text]. T-Taxol has been proposed as the bioactive conformation on beta-tubulin and subsequently utilized in the design of a series of highly active bridged taxane analogues. A modified T-form with a reversed C-13 side chain orientation has recently been proposed as an equally plausible bioactive shape. A comparison of the two spatial alternatives within the tubulin binding site electron crystallographic density suggests strongly that T-Taxol is the bioactive conformation.
Johnson
Scott A
SA
Department of Chemistry, Emory University, Atlanta, Georgia 30322, USA.
Alcaraz
Ana A
AA
Snyder
James P
JP
D001665:Binding Sites; D008958:Models, Molecular; D008968:Molecular Conformation; D015394:Molecular Structure; D017239:Paclitaxel / Q000031:analogs & derivatives* / Q000737:chemistry*; D014404:Tubulin / Q000737:chemistry*
D014404:Tubulin; D017239:Paclitaxel