مورد إلكتروني
Sustainable Syntheses of (-)-Jerantinines A & E and Structural Characterisation of the Jerantinine-Tubulin Complex at the Colchicine Binding Site
| العنوان: | Sustainable Syntheses of (-)-Jerantinines A & E and Structural Characterisation of the Jerantinine-Tubulin Complex at the Colchicine Binding Site |
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| المؤلفون: | Smedley, CJ, Stanley, PA, Qazzaz, ME, Prota, AE, Olieric, N, Collins, H, Eastman, H, Barrow, AS, Lim, K-H, Kam, T-S, Smith, BJ, Duivenvoorden, HM, Parker, BS, Bradshaw, TD, Steinmetz, MO, Moses, JE |
| بيانات النشر: | NATURE PORTFOLIO 2018-07-13 |
| نوع الوثيقة: | Electronic Resource |
| مستخلص: | The jerantinine family of Aspidosperma indole alkaloids from Tabernaemontana corymbosa are potent microtubule-targeting agents with broad spectrum anticancer activity. The natural supply of these precious metabolites has been significantly disrupted due to the inclusion of T. corymbosa on the endangered list of threatened species by the International Union for Conservation of Nature. This report describes the asymmetric syntheses of (-)-jerantinines A and E from sustainably sourced (-)-tabersonine, using a straight-forward and robust biomimetic approach. Biological investigations of synthetic (-)-jerantinine A, along with molecular modelling and X-ray crystallography studies of the tubulin-(-)-jerantinine B acetate complex, advocate an anticancer mode of action of the jerantinines operating via microtubule disruption resulting from binding at the colchicine site. This work lays the foundation for accessing useful quantities of enantiomerically pure jerantinine alkaloids for future development. |
| مصطلحات الفهرس: | Journal Article |
| URL: | NHMRC/1127754 |
| الإتاحة: | Open access content. Open access content CC BY https://creativecommons.org/licenses/by/4.0 |
| أرقام أخرى: | UMV oai:jupiter.its.unimelb.edu.au:11343/306645 Smedley, C. J., Stanley, P. A., Qazzaz, M. E., Prota, A. E., Olieric, N., Collins, H., Eastman, H., Barrow, A. S., Lim, K. -H., Kam, T. -S., Smith, B. J., Duivenvoorden, H. M., Parker, B. S., Bradshaw, T. D., Steinmetz, M. O. & Moses, J. E. (2018). Sustainable Syntheses of (-)-Jerantinines A & E and Structural Characterisation of the Jerantinine-Tubulin Complex at the Colchicine Binding Site. SCIENTIFIC REPORTS, 8 (1), https://doi.org/10.1038/s41598-018-28880-2. 10.1038/s41598-018-28880-2 2045-2322 2045-2322 1340015187 |
| المصدر المساهم: | UNIV OF MELBOURNE From OAIster®, provided by the OCLC Cooperative. |
| رقم الأكسشن: | edsoai.on1340015187 |
| قاعدة البيانات: | OAIster |
| الوصف غير متاح. |