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Combretastatin A-4, an agent that displays potent and selective toxicity toward tumor vasculature.
Vascular shutdown, within experimental and human breast cancer models in vivo following systemic drug administration, was demonstrated with a reduction in functional vascular volume of 93% at 6 h following drug administration and persisted over the next 12 h, with corresponding histology consistent with hemorrhagic necrosis resulting from vascular damage. Expand
Microplate Alamar Blue Assay for Staphylococcus epidermidis Biofilm Susceptibility Testing
The described method of microplate Alamar blue biofilm susceptibility testing, which is simple, reproducible, cost-effective, nontoxic, and amenable to high throughput, is applicable to other important biofilm forming species, and should greatly facilitate the discovery of biofilm specific agents. Expand
Inhibition of cyclin-dependent kinases, GSK-3beta and CK1 by hymenialdisine, a marine sponge constituent.
The natural product hymenialdisine is a new kinase inhibitor with promising potential applications for treating neurodegenerative disorders. Expand
The guanine nucleotide exchange factor RasGRP is a high -affinity target for diacylglycerol and phorbol esters.
RasGRP thus provides a direct link between diacylglycerol generation or phorbol ester/bryostatin treatment and Ras activation and is concluded that RasGRP is a high affinity receptor for phorbobol esters and diacyLglycersol. Expand
Isolation, structure, and synthesis of combretastatins A-1 and B-1, potent new inhibitors of microtubule assembly, derived from Combretum caffrum.
The structural simplicity and ready synthesis of combretastatin A-1 and combretastsatin B-1 suggest that these new biosynthetic products will become useful in a variety of biological endeavors. Expand
Comparative Preclinical Pharmacokinetic and Metabolic Studies of the Combretastatin Prodrugs Combretastatin A4 Phosphate and A1 Phosphate
Although in vitro studies suggest that variable rates of tumor-specific prodrug dephosphorylation may explain differences in pharmacokinetics profiles, the improved antitumor activity and altered pharmacokinetic profile of CA1 may be due to the formation of a more reactive metabolite. Expand
In vivo and in vitro evaluation of combretastatin A-4 and its sodium phosphate prodrug
It is concluded that combretastatin A-4 and its prodrug caused extensive necrosis in MAC 15A s.c. and orthotopic colon cancer and metastases, resulting in anti-tumour effects. Expand
Phorbol ester-stimulated phosphorylation of PU.1: association with leukemic cell growth inhibition.
The data suggest that TPA-induced growth inhibition is associated with phosphorylation of PU.1 and generation of a unique PU.2 DNA binding activity, which is believed to be the first of its kind in the world. Expand
Amino Acids and Derivatives
This chapter discusses the chemistry of amino acids and derivatives. Methods for selective protection and deprotection of amino acid units comprise an expanding series of reactions of fundamentalExpand