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Zebrafish chemical screening reveals an inhibitor of Dusp6 that expands cardiac cell lineages
TLDR
A temporal role for Dusp6 in restricting cardiac progenitors and controlling heart organ size was uncovered with BCI treatment at varying developmental stages, highlighting the power of in vivo zebrafish chemical screens to identify novel compounds targeting D Susp6, a component of the FGF signaling pathway that has eluded traditional high-throughput in vitro screens. Expand
APC is essential for targeting phosphorylated beta-catenin to the SCFbeta-TrCP ubiquitin ligase.
TLDR
It is shown that the SCF(beta-TrCP) binding site created by phosphorylation of beta-catenin is highly vulnerable to protein phosphatase 2A (PP2A) and must be protected by the adenomatous polyposis coli (APC) tumor suppressor protein. Expand
Regulation of the autophagy protein LC3 by phosphorylation
TLDR
PKA puts the brakes on autophagy by inhibiting LC3 recruitment to autophagosomes in mice and spares the cell from apoptosis. Expand
A common pharmacophore for a diverse set of colchicine site inhibitors using a structure-based approach.
TLDR
Using the recently determined X-ray structure of the tubulin:colchicinoid complex as the template, docking studies were employed to determine the binding modes of a set of structurally diverse colchicine site inhibitors and this work constructed a comprehensive, structure-based pharmacophore that in combination with molecular dynamics simulations confirms and extends the understanding of binding interactions at the colchichine site. Expand
Small Molecule Modulators of Endogenous and Co-chaperone-stimulated Hsp70 ATPase Activity*
TLDR
Small molecules with structural similarity to 15-deoxyspergualin and NSC 630668-R/1 are identified and screened for their effects on endogenous and Hsp40-stimulated Hsp70 ATPase activity, indicating the potential for continued screening of small molecule HSp70 effectors and that specific modulators of Hsp 70-Hsp40 interaction can be obtained, potentially for future therapeutic use. Expand
Discodermolide, a cytotoxic marine agent that stabilizes microtubules more potently than taxol.
TLDR
Discodermolide arrests Burkitt lymphoma cells in mitosis and shows spectacular rearrangement of the microtubule cytoskeleton, including extensive microtubules bundling in breast carcinoma cells. Expand
The microtubule-stabilizing agent discodermolide competitively inhibits the binding of paclitaxel (Taxol) to tubulin polymers, enhances tubulin nucleation reactions more potently than paclitaxel, and
TLDR
It is demonstrated that discodermolide is a competitive inhibitor with [3H]paclitaxel in binding to tubulin polymer, with an apparent Ki value of 0.4 microM, and that these properties represent hypernucleation phenomena. Expand
Histone deacetylase inhibitor enhances recovery after AKI.
TLDR
The data suggest that accelerating recovery may be a viable approach to treating AKI and provide proof of concept that a screen in zebrafish embryos can identify therapeutic candidates for kidney injury. Expand
Identification of an Inhibitor of hsc70-mediated Protein Translocation and ATP Hydrolysis*
TLDR
A novel compound, R/1, inhibits the endogenous and DnaJ-stimulated ATPase activity of hsc70 by 48 and 51%, respectively, and blocks the h scsc70-mediated translocation of a preprotein into yeast endoplasmic reticulum-derived microsomal vesicles. Expand
Theory and Applications of Surface Plasmon Resonance, Resonant Mirror, Resonant Waveguide Grating, and Dual Polarization Interferometry Biosensors
TLDR
This review discusses the basic theory and operational arrangements of four commercially available types of optical biosensors: surface plasmon resonance, resonant mirror, resonance waveguide grating, and dual polarization interferometry. Expand
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