Search Results - "Horwitz, Susan B"
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Structural Basis of Microtubule Stabilization by Discodermolide
Published in Chembiochem : a European journal of chemical biology (18-05-2017)“…Microtubule‐stabilizing agents (MSAs) are widely used in chemotherapy. Using X‐ray crystallography we elucidated the detailed binding modes of two potent MSAs,…”
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Activation of the Steroid and Xenobiotic Receptor (Human Pregnane X Receptor) by Nontaxane Microtubule-Stabilizing Agents
Published in Clinical cancer research (01-09-2005)“…Purpose: Because induction of drug efflux transporters is one of the major underlying mechanisms of drug resistance in cancer chemotherapy, and human pregnane…”
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Highly Concise Routes to Epothilones: The Total Synthesis and Evaluation of Epothilone 490
Published in Journal of the American Chemical Society (21-08-2002)“…A concise modular laboratory construction of the epothilone class of promising antitumor agents has been accomplished. For the first time in the epothilone…”
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The Effect of Ketoconazole on the Pharmacokinetics and Pharmacodynamics of Ixabepilone: A First in Class Epothilone B Analogue in Late-Phase Clinical Development
Published in Clinical cancer research (01-05-2008)“…Purpose: To determine if ixabepilone is a substrate for cytochrome P450 3A4 (CYP3A4) and if its metabolism by this cytochrome is clinically important, we did a…”
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Design, Synthesis, and Biological Evaluation of New-Generation Taxoids
Published in Journal of medicinal chemistry (12-06-2008)“…Novel second-generation taxoids with systematic modifications at the C2, C10, and C3′N positions were synthesized and their structure−activity relationships…”
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Synthesis and biological evaluation of novel 3′-difluorovinyl taxoids
Published in Journal of fluorine chemistry (01-11-2012)“…Novel 3′-difluorovinyl taxoids were synthesized and evaluated for their in vitro cytotoxicities against human breast, ovarian, colon and pancreatic cancer cell…”
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Multiple microtubule alterations are associated with Vinca alkaloid resistance in human leukemia cells
Published in Cancer research (Chicago, Ill.) (01-08-2001)“…Vinca alkaloids are used extensively in the treatment of childhood acute lymphoblastic leukemia (ALL) and despite their usefulness, drug resistance remains a…”
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Design, Synthesis, and Biological Evaluation of Novel C14−C3′BzN-Linked Macrocyclic Taxoids
Published in Journal of organic chemistry (19-12-2008)“…Novel macrocyclic paclitaxel congeners were designed to mimic the bioactive conformation of paclitaxel. Computational analysis of the “REDOR-Taxol” structure…”
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Promotion of microtubule assembly in vitro by taxol
Published in Nature (London) (22-02-1979)Get full text
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Design, Synthesis, and Biological Evaluation of Novel C14-C3'BzN-Linked Macrocyclic Taxoids
Published in Journal of organic chemistry (19-12-2008)“…Novel macrocyclic paclitaxel congeners were designed to mimic the bioactive conformation of paclitaxel. Computational analysis of the "REDOR-Taxol" structure…”
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Use of the Tubulin Bound Paclitaxel Conformation for Structure-Based Rational Drug Design
Published in Chemistry & biology (01-03-2005)“…A new computational docking protocol has been developed and used in combination with conformational information inferred from REDOR-NMR experiments on…”
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Properties and products of the degradation of DNA by bleomycin and iron(II)
Published in Biochemistry (Easton) (11-07-1978)Get full text
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Effect of VP-16-213 on the intracellular degradation of DNA in HeLa cells
Published in Biochemistry (Easton) (01-12-1976)“…The effect of VP-16-213 on cellular DNA was studied by following the sedimentation profiles of radioactive DNA in HeLa cells on alkaline sucrose gradients. In…”
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Effects of podophyllotoxin and VP-16-213 on microtubule assembly in vitro and nucleoside transport in HeLa cells
Published in Biochemistry (Easton) (01-12-1976)“…VP-16-213, a semisynthetic derivative of podophyllotoxin, is an active antitumor agent. In this paper, the effects of VP-16-213 and podophyllotoxin on…”
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Biologically active taxol analogs with deleted A-ring side chain substituents and variable C-2' configurations
Published in Journal of medicinal chemistry (01-03-1991)“…Taxol, a potent inhibitor of cell replication, enhances the assembly of tubulin into stable microtubules and promotes the formation of microtubule bundles in…”
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Bleomycin-DNA interactions: fluorescence and proton magnetic resonance studies
Published in Biochemistry (Easton) (09-08-1977)“…The interaction of bleomycin A2 with DNA has been examined by fluorescence spectroscopy and proton magnetic resonance techniques. Fluorescence bands observed…”
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On the Total Synthesis and Preliminary Biological Evaluations of 15(R) and 15(S) Aza-dEpoB: A Mitsunobu Inversion at C15 in Pre-Epothilone Fragments
Published in Organic letters (01-06-2000)“…The syntheses of two epothilone analogues, 15(S)-aza-12,13-desoxyepothilone B and the epimeric 15(R)-aza-12,13-desoxyepothilone B, are described. A Mitsunobu…”
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Taxol in ovarian cancer
Published in Cancer (15-02-1993)“…Taxol is a structurally complex natural plant product with a novel mechanism of action. The supply of this drug is limited by its low abundance in the bark of…”
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