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Celastrols as Inducers of the Heat Shock Response and Cytoprotection*[boxs]
Alterations in protein folding and the regulation of conformational states have become increasingly important to the functionality of key molecules in signaling, cell growth, and cell death.Expand
Mechanism-based enzyme inactivators.
TLDR
This approach to the studies of enzyme mechanisms is well suited for those who are geared more to the organic chemistry of enzymecatalyzed reactions and who have insights into the chemical machinery of active sites of enzymes. Expand
The Organic Chemistry of Drug Design and Drug Action
The Organic Chemistry of Drug Design and Drug Action, Third Edition, represents a unique approach to medicinal chemistry based on physical organic chemical principles and reaction mechanisms thatExpand
The Organic Chemistry of Enzyme Catalyzed Reactions
Preface About the Author Enzymes as Catalysts What Are Enzymes, and How Do They Work? Historical Specificity of Enzyme-Catalyzed Reactions Rate Acceleration Mechanisms of Enzyme CatalysisExpand
Activation of heat shock and antioxidant responses by the natural product celastrol: transcriptional signatures of a thiol-targeted molecule.
TLDR
It is reported that celastrol's biological effects, including inhibition of glucocorticoid receptor activity, can be blocked by the addition of excess free thiol, suggesting a chemical mechanism for biological activity based on modification of key reactive thiols by this natural product. Expand
The sirtuin 2 inhibitor AK-7 is neuroprotective in Huntington's disease mouse models.
TLDR
In vivo efficacy of a brain-permeable SIRT2 inhibitor in two genetic mouse models of HD resulted in improved motor function, extended survival, and reduced brain atrophy and is associated with marked reduction of aggregated mutant huntingtin, a hallmark of HD pathology. Expand
Structures of γ-Aminobutyric Acid (GABA) Aminotransferase, a Pyridoxal 5′-Phosphate, and [2Fe-2S] Cluster-containing Enzyme, Complexed with γ-Ethynyl-GABA and with the Antiepilepsy Drug Vigabatrin*
TLDR
The crystal structures of pig liver GABA-AT provide direct support for specific inactivation mechanisms proposed earlier on the basis of radio-labeling experiments. Expand
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