Christopher Tsu

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(A) The concentration-dependent effects of compound 1 and bortezomib on the proliferation of MDA-MB-231-4xUb-Luc reporter cell line were determined by the ATPlite assay at 72 h. (B) Accumulation of the 4xUb-Luc reporter in the stable MDA-MB-231 cell line was determined by incubation with the indicated concentrations of compounds for 8 h followed by(More)
The proteasome was validated as an oncology target following the clinical success of VELCADE (bortezomib) for injection for the treatment of multiple myeloma and recurring mantle cell lymphoma. Consequently, several groups are pursuing the development of additional small-molecule proteasome inhibitors for both hematologic and solid tumor indications. Here,(More)
We have identified short N,C-capped peptides that selectively inhibit the proteasome of the malaria-causing pathogen Plasmodium falciparum. These compounds are highly potent in culture with no toxicity in host cells. One cyclic biphenyl ether compound inhibited intraerythrocytic growth of P. falciparum with an IC50 of 35 nM, and we show that even a pulse(More)
The proteasome is responsible for the generation of most epitopes presented on MHC class I molecules. Treatment of cells with IFN-γ leads to the replacement of the constitutive catalytic subunits β1, β2, and β5 by the inducible subunits low molecular mass polypeptide (LMP) 2 (β1i), multicatalytic endopeptidase complex-like-1 (β2i), and LMP7 (β5i),(More)
PURPOSE To investigate whether clinically relevant levels of epigallocatechin gallate (EGCG, a component of green tea) or vitamin C (ascorbic acid) could antagonize bortezomib antitumor activity in CWR22 human prostate xenograft tumors. METHODS The pharmacokinetics (PK) of EGCG and ascorbic acid were determined in immunocompromised mice and compared with(More)
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