The structure of epothilone A was determined in 1996 using x-ray crystallography. The principal mechanism of the epothilone ... Epoxidation of cis- and trans-olefins yield epothilone A and its analogs. One of the total syntheses of epothilone B is ... Microtubules are essential to cell division, and epothilones, therefore, stop cells from properly dividing. Epothilone B ... Epothilone B: An Extension of the Suzuki Coupling Method and Insights into Structure-Activity Relationships of the Epothilones ...
Phase II Study: Systemic Treatment With iv ZK219477-Epothilone in Recurrent Glioblastoma Patients. Trial Phase:. Phase 2. ... medication: ZK 219477 epothilone B analog. Study Population: 15 recurrent glioblastoma. patients previously treated by surgery ... Any prior treatment with epothilones, other tubulin-targetting as taxanes (e.g.. paclitaxel, docetaxel) and vinca alkaloids (e. ... Any prior treatment with epothilones, other tubulin-targetting as taxanes (e.g.. paclitaxel, docetaxel) and vinca alkaloids (e. ...
This page or action requires Javascript to work, please enable Javascript in your browser or use a browser where this is supported so that functionality can be served and is provided as requested. For further assistance, please have a look at the noscript help page ...
With results from over 40 synthetic epothilone analogs, the SAR of the epothilones have been determined. The epoxide moiety can ... Development of a common pharmacophore model for taxol and the epothilones. dc.contributor.author. He, Lifeng. ... Recently, three new natural products, the epothilones, eleutherobin and discodermolide, whose chemical structures are highly ... the epothilones and eleutherobin. The meta azido substituted C-2 benzoyl ring of 2-m-azido baccatin III fits into a binding ...
Co-treatment of THP-1 groups with the tubulin depolymerisation inhibitor, Epothilone D (EpoD; 10 nM), was conducted to ...
Dive into the research topics of Stereoselective syntheses of epothilones A and B via nitrile oxide cycloadditions. Together ...
A phase II trial of the epothilone B analog, BMS-247550, in patients with previously treated advanced colorectal cancer. Ann ... A phase II trial of the epothilone B analog, BMS-247550, in patients with previously treated advanced colorectal cancer. ... A phase II trial of the epothilone B analog, BMS-247550, in patients with previously treated advanced colorectal cancer. ...
Paclitaxel, vinblastine, epothilone [224]. F-actin. Formed by the polymerization of G-actin under physiological conditions, ... Taxanes (paclitaxel), epothilones, and Vinca alkaloids. Binds to β-tubulin and disrupts microtubule dynamics by inducing a ...
Epothilones: mechanism of action and biologic activity. Goodin S, Kane MP, Rubin EH. Goodin S, et al. Among authors: kane mp. J ...
The epothilones are a class of microtubule inhibitors that exhibit a strong antitumor activity. UTD2 is a novel epothilone ... Multiple Effects of a Novel Epothilone Analog on Cellular Processes and Signaling Pathways Regulated by Rac1 GTPase in the ... pathways regulated by Rac1 may be evaluated as biomarkers for the response to therapy in clinical trials of epothilones. ... study provided novel insights into the molecular mechanism of the antineoplastic and antimetastatic activities of epothilones. ...
Epothilones. No 2007. Jan. 1, 2008 Dec. 31, 2013 No Longer Used. ...
Epothilones. No 2007. Jan. 1, 2008 Dec. 31, 2013 No Longer Used. ...
The Epothilone Story If one needed proof that natural products remain of crucial importance to drug discovery, the epothilone ... The Epothilone Story This one-day conference held on 1 July 2008, and sponsored by SCI, the RSC, and ICI brought together ... Epothilone, which is isolated from myxobacteria, has taxol-like anticancer activity, but its properties are more attractive ... Schinzer and other groups around the World have carried out detailed studies on the structure of epothilones, their binding to ...
Metabolites secreted by Sorangium cellulosum known as epothilones have been noted to have antineoplastic activity. This has led ...
EpoK catalyzes the epoxidation of C12-C13 double bond in epothilone D to form epothilone B36 (Supplementary Fig. 13a). Among ... Isolation and characterization of the epothilone biosynthetic gene cluster from Sorangium cellulosum. Gene 249, 153-160 (2000). ... Heterologous redox partners supporting the efficient catalysis of epothilone B biosynthesis by EpoK in Schlegelella brevitalea ...
A Phase II Study of Epothilone B Analog (BMS-247550) in Advanced Soft Tissue Sarcomas. Trial Phase:. Phase 2. Minimum Age:. 18 ... composition to Epothilone B analog, BMS-247550 or polyoxyethylated castor oil. (Cremophor[R] EL). - Motor or sensory neuropathy ... Any of the following as the effects of Epothilone B analog, BMS-247550, on the. developing fetus or nursing child, at the ... interactions with Epothilone B analog, BMS-247550; appropriate studies will be. undertaken in patients receiving combination ...
Description: Tubulin-Peloruside A-Epothilone A complex. Class: cell cycle/inhibitor. Keywords: ALPHA-TUBULIN, BETA-TUBULIN, ... LIGASE, GTPASE, MICROTUBULE, STATHMIN, PELORUSIDE A, EPOTHILONE A, TUBULIN FOLD, CYTOSKELETON, CELL CYCLE-INHIBITOR complex. ...
The binding mode of epothilone A on a,b-tubulin by electron crystallography. ...
El-Sayed, A. S. A. et al. Production and bioprocess optimization of antitumor Epothilone B analogue from Aspergillus fumigatus ... produces epothilone (21.5 μg/g biomass), which has potent antiproliferative activity against tumour cells HepG-2, MCF-7 and ...
Validation of the pharmacodynamics of BMS-247550, an analogue of epothilone B, during a phase I clinical study -- 2002 Clin. ...
Experiments have shown epothilone works on several levels. Epothilone reduces the growth of scar tissue by inhibiting the ... In higher doses, epothilone inhibits the growth of cancer cells, while low doses have been shown to stimulate axonal growth in ... The substance epothilone can stabilize microtubules and is already licensed on the American market - as a cancer treatment. „It ... Systemic administration of epothilone B promotes axon regeneration after spinal cord injury", Jörg Ruschel, Farida Hellal, ...
Aktuelle API Auditberichte • GMP-Audits der Herstelung pharmazeutischer Ausgangs- und Wirkstoffe nach ICH Q7 / EU GMP Guide Part II • Diapharm
In that time the company reacquired its epothilone program by ending a development and commercialization pact with Swiss drug ... Kosans epothilone compounds and related intellectual property and data and will assign to Bristol-Myers Squibb its epothilone ... inhibitors and epothilones.. The deal represents a premium of nearly 230 percent to the $1.65 per share trading price of Kosan ... and in HER2+ metastatic breast cancer and for its epothilone candidate for the treatment of solid tumors KOS-1584 which just ...
Flavopiridol down-regulates antiapoptotic proteins and sensitizes human breast cancer cells to epothilone B-induced apoptosis. ...
... serous carcinomas is a marker for poor overall survival after platinum/taxane chemotherapy and sensitivity to epothilonesRoque ... serous carcinomas is a marker for poor overall survival after platinum/taxane chemotherapy and sensitivity to epothilones. ...
BMS 247550 belongs to a class of drugs called epothilones that interfere with the ability of cancer cells to divide. In the way ... Other characteristics of the epothilones, however, enable them to work in cells that are resistant to Taxol. Patients 18 years ...
Injured spinal cord: Regeneration possible with epothilone?. .td-block-title-wrap .td-wrapper-pulldown-filter{font-family: ...
Taxol and epothilone have been subjected to immense SAR and analog preparation by some of the hard hitters in the synthetic ... And Paterson has now used this technique for disco and epothilone.. I am sure the technique has to be done carefully and that ... One of the better known cases concerns the search for a common pharmacophore for Taxol, Epothilone, and other ligands which ... First came Taxol, then the epothilones, then discodermolide, and the list continues with peluroside, eleutherobin, and ...
Newer cytotoxic chemotherapeutic agents that have been developed are epothilones and ixabepilone (121). Both these agents ...