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Formaldehyde fixation.
TLDR
The use of formaldehyde as a biological reagent occurred rather late in the history of histological methodology, and the possibility that formaldehyde solutions might provide a "nontoxic sublimate" was a desirable goal that was not lost on Meister, Lucius and Brunig. Expand
Development and optimization of a binding assay for the XIAP BIR3 domain using fluorescence polarization.
TLDR
The development of a homogeneous high-throughput assay based on fluorescence polarization for measuring the binding affinities of small-molecule inhibitors to the BIR3 domain of XIAP and results obtained indicated that the FP-based competitive binding assay performs correctly as designed. Expand
Discovery of embelin as a cell-permeable, small-molecular weight inhibitor of XIAP through structure-based computational screening of a traditional herbal medicine three-dimensional structure
The X-linked inhibitor of apoptosis (XIAP) is a promising new molecular target for the design of novel anticancer drugs aiming at overcoming apoptosis-resistance of cancer cells to chemotherapeuticExpand
Structure-based design of potent small-molecule inhibitors of anti-apoptotic Bcl-2 proteins.
TLDR
A structure-based approach was employed to design a new class of small-molecule inhibitors of Bcl-2 that Potently inhibits cell growth in PC-3 prostate cancer cells with an IC(50) value of 200 nM and effectively induces apoptosis in a dose-dependent manner. Expand
Discovery of embelin as a cell-permeable, small-molecular weight inhibitor of XIAP through structure-based computational screening of a traditional herbal medicine three-dimensional structure
TLDR
Embelin is a fairly potent, nonpeptidic, cell-permeable, small-molecule inhibitor of XIAP and represents a promising lead compound for designing an entirely new class of anticancer agents that target the BIR3 domain of XI AP. Expand
Molecular mechanism of gossypol-induced cell growth inhibition and cell death of HT-29 human colon carcinoma cells.
TLDR
Treatment of HT-29 cells with gossypol not only induces cell cycle arrest on the G0/G1 phase, but also induces apoptosis, which initiates extensive alterations of cell cycle and apoptosis proteins. Expand
Conformational transitions, dissociation, and unfolding of scrapie amyloid (prion) protein.
TLDR
Experimental evidence is provided for the beta-sheet type assembly of scrapie amyloid PrP27-30 in the solid state and the importance of amino-terminal cleavage in the stability and alignment of the amyloids-forming monomers is demonstrated. Expand
Structure-based design of spiro-oxindoles as potent, specific small-molecule inhibitors of the MDM2-p53 interaction.
TLDR
Potent, specific, non-peptide small-molecule inhibitors of the MDM2-p53 interaction were successfully designed and the most potent inhibitor (MI-63) has excellent specificity over cancer cells with deleted p53 and shows a minimal toxicity to normal cells. Expand
Discovery of small-molecule inhibitors of Bcl-2 through structure-based computer screening.
TLDR
It was found that compound 6 can be used as a valuable pharmacological tool to elucidate the function of Bcl-2 and also serves as a novel lead compound for further design and optimization of small-molecule inhibitors targeted at the BH3 binding pocket in B cl-2. Expand
Identification of Novel Non-phosphorylated Ligands, Which Bind Selectively to the SH2 Domain of Grb7*
TLDR
The synthetic Grb 7-binding peptide G7-18 in cell lysates was able to specifically inhibit the association of Grb7 with the ErbB family of RTKs, in particular Erb B3, in a dose-dependent manner. Expand
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