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Combretastatin A-4, an agent that displays potent and selective toxicity toward tumor vasculature.
Selective induction of vascular damage within tumors represents an emerging approach to cancer treatment. Histological studies have shown that several tubulin-binding agents can induce vascularExpand
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Inhibition of cyclin-dependent kinases, GSK-3beta and CK1 by hymenialdisine, a marine sponge constituent.
BACKGROUND Over 2000 protein kinases regulate cellular functions. Screening for inhibitors of some of these kinases has already yielded some potent and selective compounds with promising potentialExpand
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Microplate Alamar Blue Assay for Staphylococcus epidermidis Biofilm Susceptibility Testing
ABSTRACT Biofilms are at the root of many infections largely because they are much more antibiotic resistant than their planktonic counterparts. Antibiotics that target the biofilm phenotype areExpand
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The guanine nucleotide exchange factor RasGRP is a high -affinity target for diacylglycerol and phorbol esters.
RasGRP is a recently described guanine nucleotide exchange factor (GEF) that possesses a single C1 domain homologous to that of protein kinase C (PKC). The phorbol ester [(3)H]phorbol 12,Expand
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Anti-vascular approaches to solid tumour therapy: evaluation of combretastatin A4 phosphate.
Combretastatin A4 phosphate has recently been identified by us as an agent which can selectively damage tumour neovasculature. In the current study we establish that combretastatin induces extensiveExpand
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Isolation, structure, and synthesis of combretastatins A-1 and B-1, potent new inhibitors of microtubule assembly, derived from Combretum caffrum.
The principal antineoplastic constituent of the South African tree Combretum caffrum has been isolated and designated combretastatin A-1. The structure of this new cis-stilbene was unequivocallyExpand
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Interactions of tubulin with potent natural and synthetic analogs of the antimitotic agent combretastatin: a structure-activity study.
Combretastatin, an antineoplastic and antimitotic agent, was isolated from the bark of Combretum caffrum [Can. J. Chem. 60: 1374-1376 (1982); Biochem. Pharmacol. 32:3864-3867 (1983)]. Structurally,Expand
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In vivo and in vitro evaluation of combretastatin A-4 and its sodium phosphate prodrug
SummaryThe anti-tumour effects and mechanism of action of combretastatin A-4 and its prodrug, combretastatin A-4 disodium phosphate, were examined in subcutaneous and orthotopically transplantedExpand
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Comparative Preclinical Pharmacokinetic and Metabolic Studies of the Combretastatin Prodrugs Combretastatin A4 Phosphate and A1 Phosphate
Purpose: Combretastatin A4 phosphate (CA4P) and its structural analog, combretastatin A1 phosphate (CA1P), are soluble prodrugs capable of interacting with tubulin and causing rapid vascular shutdownExpand
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