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Your search keyword '"Ross L. Stein"' showing total 4 results
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4 results on '"Ross L. Stein"'

1. ChemInform Abstract: Potent and Selective Inhibitors of the Proteasome: Dipeptidyl Boronic Acids

Author

Mark L. Behnke, Lawrence R. Dick, Ross L. Stein, Yu-Ting Ma, Shaowu Chen, Louis Plamondon, Julian Adams, Janice M. Klunder, Amy A. Cruickshank, and Louis Grenier

Subjects
inorganic chemicals, chemistry.chemical_classification, chemistry.chemical_compound, chemistry, Proteasome, Biochemistry, medicine, Potency, Cancer, General Medicine, medicine.disease, Aldehyde, Boronic acid
Abstract

Potent and selective dipeptidyl boronic acid proteasome inhibitors are described. As compared to peptidyl aldehyde compounds, boronic acids in this series display dramatically enhanced potency. Compounds such as 15 are promising new therapeutics for treatment of cancer and inflammatory diseases.

Published
2010
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2. Structure—Activity Relationship Study of Novel Tissue Transglutaminase Inhibitors

Author

Eric Duval, Gregory D. Cuny, Ross L. Stein, and April Case

Subjects
Stereochemistry, Tissue transglutaminase, Clinical Biochemistry, Pharmaceutical Science, Thiophenes, Sulfides, Biochemistry, Chemical synthesis, Catalysis, Substrate Specificity, Inhibitory Concentration 50, Structure-Activity Relationship, chemistry.chemical_compound, Thioether, Drug Discovery, Thiophene, Structure–activity relationship, Enzyme Inhibitors, Binding site, Molecular Biology, Cells, Cultured, chemistry.chemical_classification, Binding Sites, Transglutaminases, Bicyclic molecule, biology, Chemistry, Organic Chemistry, Caseins, Substrate (chemistry), General Medicine, Fluorescence, Hydrazines, Enzyme, Enzyme inhibitor, biology.protein, Molecular Medicine, Peptides
Abstract

Thieno[2,3-d]pyrimidin-4-one acylhydrazide derivatives were discovered as moderately potent inhibitors of TGase 2 (tissue transglutaminase) utilizing a fluorescence-based assay that measured TGase 2 catalyzed incorporation of the dansylated Lys derivative alpha-N-Boc-Lys-CH(2)-CH(2)-dansyl into the protein substrate N,N-dimethylated-casein. A SAR study revealed that the acylhydrazide thioether side-chain and the thiophene ring were critical to inhibitory activity.

Published
2005
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