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Zebrafish chemical screening reveals an inhibitor of Dusp6 that expands cardiac cell lineages
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.
APC is essential for targeting phosphorylated beta-catenin to the SCFbeta-TrCP ubiquitin ligase.
Regulation of the autophagy protein LC3 by phosphorylation
PKA puts the brakes on autophagy by inhibiting LC3 recruitment to autophagosomes in mice and spares the cell from apoptosis.
Small Molecule Modulators of Endogenous and Co-chaperone-stimulated Hsp70 ATPase Activity*
- S. W. Fewell, Christine Smith, J. Brodsky
- Biology, ChemistryJournal of Biological Chemistry
- 3 December 2004
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.
A common pharmacophore for a diverse set of colchicine site inhibitors using a structure-based approach.
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.
Discodermolide, a cytotoxic marine agent that stabilizes microtubules more potently than taxol.
Discodermolide arrests Burkitt lymphoma cells in mitosis and shows spectacular rearrangement of the microtubule cytoskeleton, including extensive microtubules bundling in breast carcinoma cells.
The microtubule-stabilizing agent discodermolide competitively inhibits the binding of paclitaxel (Taxol) to tubulin polymers, enhances tubulin nucleation reactions more potently than paclitaxel, and…
- R. Kowalski, P. Giannakakou, S. Gunasekera, R. Longley, B. Day, E. Hamel
- Biology, ChemistryMolecular Pharmacology
- 1 October 1997
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.
Histone deacetylase inhibitor enhances recovery after AKI.
- Chiara Cianciolo Cosentino, N. Skrypnyk, N. Hukriede
- BiologyJournal of the American Society of Nephrology
- 1 June 2013
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.
Identification of an Inhibitor of hsc70-mediated Protein Translocation and ATP Hydrolysis*
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.
Theory and Applications of Surface Plasmon Resonance, Resonant Mirror, Resonant Waveguide Grating, and Dual Polarization Interferometry Biosensors
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.