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Activation of Aldehyde Dehydrogenase-2 Reduces Ischemic Damage to the Heart
TLDR
Using an unbiased proteomic search, mitochondrial aldehyde dehydrogenase 2 (ALDH2) is identified as an enzyme whose activation correlates with reduced ischemic heart damage in rodent models and pharmacologic enhancement of ALDH2 activity may be useful for patients with wild-type or mutant AL DH2 who are subjected to cardiac ischemia. Expand
Glycogen and its metabolism: some new developments and old themes.
TLDR
Significant new developments in eukaryotic glycogen metabolism over the last decade or so include: (i) three-dimensional structures of the biosynthetic enzymes glycogenin and glycogen synthase, with associated implications for mechanism and control; (ii) analyses of several genetically engineered mice with altered glycogens metabolism that shed light on the mechanism of control. Expand
Aldehyde Dehydrogenase Inhibitors: a Comprehensive Review of the Pharmacology, Mechanism of Action, Substrate Specificity, and Clinical Application
TLDR
The purpose of this review is to establish the current status of pharmacological inhibition of the ALDHs, provide a rationale for the continued development of ALDH isozyme-selective inhibitors, and identify the challenges and potential therapeutic rewards associated with the creation of such agents. Expand
Structural Basis for Regulation of Protein Phosphatase 1 by Inhibitor-2*
TLDR
The crystal structure of the PP1 regulation by inhibitor-2 complex is solved and provides novel insights into the mechanism of PP1 inhibition and subsequent reactivation, has broad implications for the physiological regulation ofPP1, and highlights common inhibitory interactions among phosphoprotein phosphatase family members. Expand
Structure of mitochondrial aldehyde dehydrogenase: the genetic component of ethanol aversion.
TLDR
The structure of ALDH2 is important for the elucidation of its catalytic mechanism, for a clear understanding of the contribution ofALDH2 to the genetic component of alcoholism and for the development of specific AL DH2 inhibitors as potential drugs for use in the treatment of alcoholism. Expand
The Structural Basis for Phospholamban Inhibition of the Calcium Pump in Sarcoplasmic Reticulum*
TLDR
The long sought crystal structure of the PLB-SERCA complex is presented, showing PLB bound to a previously undescribed conformation of SERCA in which the Ca2+ binding sites are collapsed and devoid of divalent cations (E2-PLB). Expand
Coenzyme isomerization is integral to catalysis in aldehyde dehydrogenase.
TLDR
The data suggest that the presence of magnesium may lead to selection of particular conformations and speed isomerization of the reduced cofactor following hydride transfer and the role of magnesium in activating the human class 2 enzyme is clarified. Expand
Three-dimensional structure of mammalian casein kinase I: molecular basis for phosphate recognition.
TLDR
Comparison of the mammalian and yeast CKI structures suggests that a rotation of the N-terminal domain occurs upon ATP binding, which is similar, but not identical, to that observed in cAMP-dependent protein kinase upon binding ATP. Expand
Lipid Desaturation Is a Metabolic Marker and Therapeutic Target of Ovarian Cancer Stem Cells.
TLDR
It is shown that increased lipid unsaturation is a metabolic marker for ovarian CSCs and a target for CSC-specific therapy and Mechanistically, it is demonstrated that nuclear factor κB (NF-κB) directly regulates the expression levels of lipid desaturases, and inhibition of desaturase blocks NF-κBs signaling. Expand
Hydrolysis of Capecitabine to 5′-Deoxy-5-fluorocytidine by Human Carboxylesterases and Inhibition by Loperamide
TLDR
Northern blot analysis indicates that relative expression in intestinal tissue is CES2 > CES1A1 > CES3, indicating that intestinal activation of capecitabine may contribute to its efficacy in colon cancer and toxic diarrhea associated with the agent. Expand
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