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Literature DB >> 15226503

The bioactive Taxol conformation on beta-tubulin: experimental evidence from highly active constrained analogs.

Thota Ganesh¹, Rebecca C Guza, Susan Bane, Rudravajhala Ravindra, Natasha Shanker, Ami S Lakdawala, James P Snyder, David G I Kingston.

Abstract

The important anticancer drug Taxol (paclitaxel) binds to tubulin in a stoichiometric ratio and promotes its assembly into microtubules. The conformation of microtubule-bound drug has been the subject of intense study, and various suggestions have been made. In this work we present experimental and theoretical evidence that Taxol adopts a T-shaped conformation when it is bound to tubulin.

Entities: Chemical

Mesh：

Substances：
Tubulin
Paclitaxel

Year: 2004 PMID： 15226503 PMCID： PMC454156 DOI： 10.1073/pnas.0403459101

Source DB: PubMed Journal: Proc Natl Acad Sci U S A ISSN： 0027-8424 Impact factor: 11.205

39 in total

1. Conformationally restricted paclitaxel analogues: macrocyclic mimics of the "hydrophobic collapse" conformation.

Authors: T C Boge; Z J Wu; R H Himes; D G Vander Velde; G I Georg
Journal: Bioorg Med Chem Lett Date: 1999-10-18 Impact factor: 2.823

2. The binding conformation of Taxol in beta-tubulin: a model based on electron crystallographic density.

Authors: J P Snyder; J H Nettles; B Cornett; K H Downing; E Nogales
Journal: Proc Natl Acad Sci U S A Date: 2001-04-17 Impact factor: 11.205

3. Conformation of microtubule-bound paclitaxel determined by fluorescence spectroscopy and REDOR NMR.

Authors: Y Li; B Poliks; L Cegelski; M Poliks; Z Gryczynski; G Piszczek; P G Jagtap; D R Studelska; D G Kingston; J Schaefer; S Bane
Journal: Biochemistry Date: 2000-01-18 Impact factor: 3.162

4. A unified and quantitative receptor model for the microtubule binding of paclitaxel and epothilone.

Authors: M Wang; X Xia; Y Kim; D Hwang; J M Jansen; M Botta; D C Liotta; J P Snyder
Journal: Org Lett Date: 1999-07-15 Impact factor: 6.005

Review 5. Chemotherapy of breast cancer: are the taxanes going to change the natural history of breast cancer?

Authors: J M Nabholtz; K Tonkin; M Smylie; H J Au; M A Lindsay; J Mackey
Journal: Expert Opin Pharmacother Date: 2000-01 Impact factor: 3.889

6. A common pharmacophore for epothilone and taxanes: molecular basis for drug resistance conferred by tubulin mutations in human cancer cells.

Authors: P Giannakakou; R Gussio; E Nogales; K H Downing; D Zaharevitz; B Bollbuck; G Poy; D Sackett; K C Nicolaou; T Fojo
Journal: Proc Natl Acad Sci U S A Date: 2000-03-14 Impact factor: 11.205

7. A common pharmacophore for Taxol and the epothilones based on the biological activity of a taxane molecule lacking a C-13 side chain.

Authors: L He; P G Jagtap; D G Kingston; H J Shen; G A Orr; S B Horwitz
Journal: Biochemistry Date: 2000-04-11 Impact factor: 3.162

Review 8. The taxanes: an update.

Authors: J Crown; M O'Leary
Journal: Lancet Date: 2000-04-01 Impact factor: 79.321

9. Molecular recognition of taxol by microtubules. Kinetics and thermodynamics of binding of fluorescent taxol derivatives to an exposed site.

Authors: J F Díaz; R Strobe; Y Engelborghs; A A Souto; J M Andreu
Journal: J Biol Chem Date: 2000-08-25 Impact factor: 5.157

10. Novel d-seco paclitaxel analogues: synthesis, biological evaluation, and model testing.

Authors: L Barboni; A Datta; D Dutta; G I Georg; D G Vander Velde; R H Himes; M Wang; J P Snyder
Journal: J Org Chem Date: 2001-05-18 Impact factor: 4.354

31 in total

1. Design and synthesis of simplified taxol analogs based on the T-Taxol bioactive conformation.

Authors: Jielu Zhao; Susan Bane; James P Snyder; Haipeng Hu; Kamalika Mukherjee; Carla Slebodnick; David G I Kingston
Journal: Bioorg Med Chem Date: 2011-10-13 Impact factor: 3.641

2. Taxol biosynthesis and molecular genetics.

Authors: Rodney Croteau; Raymond E B Ketchum; Robert M Long; Rüdiger Kaspera; Mark R Wildung
Journal: Phytochem Rev Date: 2006-02 Impact factor: 5.374

Review 3. Drug discovery targeting cell division proteins, microtubules and FtsZ.

Authors: Iwao Ojima; Kunal Kumar; Divya Awasthi; Jacob G Vineberg
Journal: Bioorg Med Chem Date: 2014-03-05 Impact factor: 3.641

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

Authors: 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
Journal: J Med Chem Date: 2007-01-31 Impact factor: 7.446

5. Rotational-echo double-resonance NMR distance measurements for the tubulin-bound Paclitaxel conformation.

Authors: Younkee Paik; Chao Yang; Belhu Metaferia; Shoubin Tang; Susan Bane; Rudravajhala Ravindra; Natasha Shanker; Ana A Alcaraz; Scott A Johnson; Jacob Schaefer; Robert D O'Connor; Lynette Cegelski; James P Snyder; David G I Kingston
Journal: J Am Chem Soc Date: 2007-01-17 Impact factor: 15.419