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Bioactivation of leukotoxins to their toxic diols by epoxide hydrolase
Leukotoxin is a linoleic acic oxide produced by leukocytes and has been associated with the multiple organ failure and adult respiratory distress syndrome seen in some severe burn patients.Expand
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Novel cytotoxic peptides from the tropical marine cyanobacteriumHormothamnion enteromorphoides 1. Discovery, isolation and initial chemical and biological characterization of the hormothamnins from
A Caribbean cyanobacterium,Hormothamnion enteromorphoides, was found to produce a complex mixture of ichthyotoxic peptides, perhaps explaining the apparent absence of predation upon these potentiallyExpand
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CC-223, a Potent and Selective Inhibitor of mTOR Kinase: In Vitro and In Vivo Characterization
mTOR is a serine/threonine kinase that regulates cell growth, metabolism, proliferation, and survival. mTOR complex-1 (mTORC1) and mTOR complex-2 (mTORC2) are critical mediators of the PI3K–AKTExpand
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Efficiency in Drug Discovery: Liver S9 Fraction Assay As a Screen for Metabolic Stability
Background: A rapid and comprehensive metabolic stability screen at the top of a drug discovery flow chart serves as an effective gate in eliminating low value compounds. This imparts a significantExpand
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Proposing advancement criteria for efficient DMPK triage of new chemical entities.
With the goal of refining our discovery DMPK workflow, we conducted a retrospective analysis on internal Celgene compounds by calculating the physicochemical properties and gathering data fromExpand
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Discovery of 12-(S)-hydroxy-5,8,10,14-icosatetraenoic acid [12-(S)-HETE] in the tropical red alga Platysiphonia miniata.
The potent mammalian immunohormone, 12-(S)-hydroxy-5,8,10,14-icosatetraenoic acid (12-(S)-HETE), is a 12-lipoxygenase metabolite of arachidonic acid that is widely distributed in animal tissues. InExpand
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12-Lipoxygenase activity in the red marine alga Gracilariopsis lemaneiformis
Abstract The temperate red alga Gracilariopsis lemaneiformis is a rich source of polyunsaturated fatty acids that are regio-specifically oxidized at C-12. In this in vitro study, we demonstrate theExpand
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Oxylipin metabolism in the red alga Gracilariopsis lemaneiformis: mechanism of formation of vicinal dihydroxy fatty acids.
Conversion of arachidonic acid into the vicinal diol fatty acid 12R,13S-dihydroxy-5Z,8Z,10E,14Z-eicosatetraenoic acid using an acetone powder of the marine red alga, Gracilariopsis lemaneiformis,Expand
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Development of an in situ toxicity assay system using recombinant baculoviruses.
A new method for experimentally analyzing the role of enzymes involved in metabolizing mutagenic, carcinogenic, or cytotoxic chemicals is described. Spodoptera fugiperda (SF-21) cells infected withExpand
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