Book ChapterDOI
The Behavior and Significance of Slow-Binding Enzyme Inhibitors
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This article is published in Advances in Enzymology and Related Areas of Molecular Biology.The article was published on 1988-01-01. It has received 721 citations till now. The article focuses on the topics: Enzyme inducer & Non-competitive inhibition.read more
Citations
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Journal ArticleDOI
Nongenotropic, sex-nonspecific signaling through the estrogen or androgen receptors: dissociation from transcriptional activity.
Stavroula Kousteni,Teresita Bellido,Lilian I. Plotkin,Charles A. O'Brien,Donald L. Bodenner,Li Han,K. Han,G. B. DiGregorio,John A. Katzenellenbogen,Benita S. Katzenellenbogen,Paula K. Roberson,Robert S. Weinstein,Robert L. Jilka,Stavros C. Manolagas +13 more
TL;DR: A novel paradigm of sex steroid action on osteoblasts, osteocytes, embryonic fibroblasts, and HeLa cells involving activation of a Src/Shc/ERK signaling pathway and attenuating apoptosis is demonstrated, providing proof of principle for the development of function-specific-as opposed to tissue-selective-and gender-neutral pharmacotherapeutics.
Journal ArticleDOI
Copper Active Sites in Biology
Edward I. Solomon,David E. Heppner,Esther M. Johnston,Jake W. Ginsbach,Jordi Cirera,Munzarin F. Qayyum,Matthew T. Kieber-Emmons,Christian H. Kjaergaard,Ryan G. Hadt,Li Tian +9 more
TL;DR: This review presents in depth discussions of all these classes of Cu enzymes and the correlations within and among these classes, as well as the present understanding of the enzymology, kinetics, geometric structures, electronic structures and the reaction mechanisms these have elucidated.
Journal ArticleDOI
A Unique Structure for Epidermal Growth Factor Receptor Bound to GW572016 (Lapatinib): Relationships among Protein Conformation, Inhibitor Off-Rate, and Receptor Activity in Tumor Cells
Edgar R. Wood,Anne T. Truesdale,Octerloney B. McDonald,Derek Yuan,Anne M. Hassell,Scott Howard Dickerson,Byron Ellis,Christopher Pennisi,Earnest Horne,Karen Lackey,Krystal J. Alligood,David W. Rusnak,Tona M. Gilmer,Lisa M. Shewchuk +13 more
TL;DR: The slow off-rate ofGW572016 correlates with a prolonged down-regulation of receptor tyrosine phosphorylation in tumor cells and the differences in the off-rates of these drugs and the ability of GW572016 to inhibit ErbB-2 can be explained by the enzyme-inhibitor structures.
Journal ArticleDOI
Inhibition of Human Caspases by Peptide-based and Macromolecular Inhibitors
Margarita Garcia-Calvo,Erin P. Peterson,Barbara Leiting,Rejean Ruel,Donald W. Nicholson,Nancy A. Thornberry +5 more
TL;DR: The results obtained with peptide-based inhibitors are in accord with those predicted from the substrate specificity studies described earlier, and the cowpox serpin CrmA is a potent and selective inhibitor of Group I and most Group III caspases, suggesting that this virus facilitates infection through inhibition of both apoptosis and the host inflammatory response.
Journal ArticleDOI
Structural Basis for the Inhibition of Caspase-3 by XIAP
Stefan J. Riedl,Martin Renatus,Robert Schwarzenbacher,Qiao Zhou,Chaohong Sun,Stephen W. Fesik,Robert C. Liddington,Guy S. Salvesen +7 more
TL;DR: The crystal structure of the second BIR domain of XIAP (BIR2) in complex with caspase-3, at a resolution of 2.7 A, is reported, revealing the structural basis for inhibition and the mechanism of inhibition is due to a steric blockade prohibitive of substrate binding.
References
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Journal ArticleDOI
Mevinolin: a highly potent competitive inhibitor of hydroxymethylglutaryl-coenzyme A reductase and a cholesterol-lowering agent.
Alfred W. Alberts,Julie S. Chen,G Kuron,V Hunt,Jesse W. Huff,Carl H. Hoffman,John W. Rothrock,Lopez Maria B,Henry Joshua,Elbert E. Harris,Arthur A. Patchett,R L Monaghan,S Currie,E Stapley,George Albers-Schonberg,Otto D. Hensens,J Hirshfield,Karst Hoogsteen,Jerrold M. Liesch,James P. Springer +19 more
TL;DR: It was shown that mevinolin was an orally active cholesterol-lowering agent in the dog and orally administered sodium mevinolinate was an active inhibitor of cholesterol synthesis in an acute assay.
Journal ArticleDOI
Kinetics of the reversible inhibition of enzyme-catalysed reactions by tight-binding inhibitors
TL;DR: A general rate equation has been derived and shown to be quadratic with square and linear terms in v which represents that true initial steady-state velocity of enzymic reactions that are reversibly inhibited by a substrate analogue at concentrations comparable to that of the enzyme.
Journal ArticleDOI
Crystal structures of Escherichia coli and Lactobacillus casei dihydrofolate reductase refined at 1.7 A resolution. I. General features and binding of methotrexate.
TL;DR: Refinement has led to a revised description of the details of methotrexate binding, and a hypothetical model for substrate binding is proposed in which the pteridine ring is turned upside down while all protein and solvent atoms remain fixed.
Journal ArticleDOI
Competitive inhibition of 3-hydroxy-3-methylglutaryl coenzyme a reductase by ML-236A and ML-236B fungal metabolites, having hypocholesterolemic activity
TL;DR: The experiments reported in this paper demonstrate that MG236A and ML-236B inhibit specifically 3-hydroxy-3-methylglutaryl (HMG)CoA reductase (EC 1 .I .1.34), the rate-limiting enzyme in cholesterol synthetic pathway, without affecting the rest of the enzymes involved in this pathway, and that the inhibition is competitive with respect to the substrate HMG-CoA.