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In vitro and in vivo anticancer activities of synthetic macrocyclic ketone analogues of halichondrin B.
It is shown that two macrocyclic ketone analogues of halichondrir B, ER-076349 and ER-086526, have sub-nM growth inhibitory activities in vitro against numerous human cancer cell lines as well as marked in vivo activities against four human xenografts. Expand
Induction of Morphological and Biochemical Apoptosis following Prolonged Mitotic Blockage by Halichondrin B Macrocyclic Ketone Analog E7389
Results show that prolonged mitotic blockage by E7 389 can lead to apoptotic cell death of human cancer cells in vitro and can provide a mechanistic basis for the significant in vivo anticancer efficacy of E7389. Expand
Semi-synthetic aequorins with improved sensitivity to Ca2+ ions.
Thirty-seven coelenterazine analogues were synthesized and incorporated into apo-aequorin, yielding 30 semi-synthetic aequorins that have the capacity to emit a significant amount of light in theExpand
Light-emitting properties of recombinant semi-synthetic aequorins and recombinant fluorescein-conjugated aequorin for measuring cellular calcium.
The fluorescein-conjugated aEquorin exhibited fluorescence in addition to the Ca(2+)-triggered luminescence, thus it can be used to visualize the diffusion and distribution of aequorin in cells. Expand
Recombinant aequorin and recombinant semi-synthetic aequorins. Cellular Ca2+ ion indicators.
The recombinant aEquorin and recombinant semi-synthetic aequorins are highly suited for monitoring cellular Ca2+. Expand
E5531, a synthetic non‐toxic lipid A derivative blocks the immunobiological activities of lipopolysaccharide
Results support the contention that E5531 is a potent antagonist of lipopolysaccharide‐induced release of tumour necrosis factor‐α and other cellular mediators and may be an effective therapeutic agent for human septic shock due to Gram‐negative bacteria. Expand
The relative rate of aequorin regeneration from apoaequorin and coelenterazine analogues.
The recovery of an active semi-synthetic aequorin from apoaequorin produced in cells and a coelenterazine analogue is a key step in measuring Ca2+ in the cells, and the results indicated that the rate is strongly influenced by the analogues used. Expand
Chlorophyll Catabolism Leading to the Skeleton of Dinoflagellate and Krill Luciferins: Hypothesis and Model Studies.
Remarkable selectivity is exhibited in the photooxidation of 20-methoxychlorin methyl ester (1) to exclusively yield the C1-C20 bond cleaved product 2. This selectivity lends strong support to theExpand
Eribulin induces irreversible mitotic blockade: implications of cell-based pharmacodynamics for in vivo efficacy under intermittent dosing conditions.
The results suggest that compound-specific reversibility characteristics of antimitotic agents contribute to interactions between cell-based pharmacodynamics and in vivo pharmacokinetics that define antitumor efficacy under intermittent dosing conditions. Expand