Enzyme Inhibitors - Metabolism
Research News and Information

Sunday, November 22, 2009

Role of E166 in the imine to enamine tautomerization of the clinical beta-lactamase inhibitor sulbactam.

Nov 2009 Mechanism-based inhibitors of class A beta-lactamases, such as sulbactam, undergo a complex series of chemical reactions in the enzyme active site. Formation of a trans-enamine acyl-enzyme via a hydrolysis-prone imine is responsible for transient ... Read more...

MAC inhibitors suppress mitochondrial apoptosis.

10 Oct 2009 MAC (mitochondrial apoptosis-induced channel) forms in the mitochondrial outer membrane and unleashes cytochrome c to orchestrate the execution of the cell. MAC opening is the commitment step of intrinsic apoptosis. Hence closure of MAC may prevent ... Read more...

Biosynthesis and role in virulence of the histone deacetylase inhibitor depudecin from Alternaria brassicicola.

29 Sep 2009 Depudecin, an eleven-carbon linear polyketide made by the pathogenic fungus Alternaria brassicicola, is an inhibitor of histone deacetylase (HDAC). A chemically unrelated HDAC inhibitor, HC toxin, was earlier shown to be a major virulence factor in ... Read more...

Latest indexed articles for 'Enzyme Inhibitors - Metabolism'

These are the very latest articles for this heading:

• Role of E166 in the imine to enamine tautomerization of the clinical beta-lactamase inhibitor sulbactam. Nov 2009
• MAC inhibitors suppress mitochondrial apoptosis. 10 Oct 2009
• Biosynthesis and role in virulence of the histone deacetylase inhibitor depudecin from Alternaria brassicicola. 29 Sep 2009
• Developing dual and specific inhibitors of dimethylarginine dimethylaminohydrolase-1 and nitric oxide synthase: toward a targeted polypharmacology to control nitric oxide. 13 Sep 2009
• Crystal structure of the catalytic domain of the tumor-associated human carbonic anhydrase IX. 12 Sep 2009
• Benzothiopyranoindole-based antiproliferative agents: synthesis, cytotoxicity, nucleic acids interaction, and topoisomerases inhibition properties. 8 Sep 2009
• Snapshots of the fluorosalinosporamide/20S complex offer mechanistic insights for fine tuning proteasome inhibition. 8 Sep 2009
• Structural basis for the inhibition of human 5,10-methenyltetrahydrofolate synthetase by N10-substituted folate analogues. 6 Sep 2009
• Oxidant-induced apoptosis is mediated by oxidation of the actin-regulatory protein cofilin. 4 Sep 2009
• Ceramide mediates inhibition of the AKT/eNOS signaling pathway by palmitate in human vascular endothelial cells. 30 Aug 2009
• Asymmetric dimethylarginine endogenous inhibition of nitric oxide synthase causes differential vasculature effects. 30 Aug 2009
• Stearoyl-CoA desaturase inhibitors: update on patented compounds. 30 Aug 2009
• Interaction of ionizing radiation and ZRBA1, a mixed EGFR/DNA-targeting molecule. 30 Aug 2009
• Insights into the two-domain architecture of the metallocarboxypeptidase inhibitor from the Ascaris parasite inferred from the mechanism of its oxidative folding. 30 Aug 2009
• Radical triplets and suicide inhibition in reactions of 4-thia-D- and 4-thia-L-lysine with lysine 5,6-aminomutase. 30 Aug 2009
• Quaternary benzyltriethylammonium ion binding to the Na,K-ATPase: a tool to investigate extracellular K(+) binding reactions. 30 Aug 2009
• Study on the inhibitory mechanism and binding mode of the hydroxycoumarin compound NSC158393 to HIV-1 integrase by molecular modeling. 30 Aug 2009
• Single molecule measurements of F1-ATPase reveal an interdependence between the power stroke and the dwell duration. 23 Aug 2009
• Inhibition of the soluble epoxide hydrolase by tyrosine nitration. 22 Aug 2009
• AURKB-mediated effects on chromatin regulate binding versus release of XIST RNA to the inactive chromosome. 22 Aug 2009

See a longer list of these articles.

Technical information about 'Enzyme Inhibitors'

Definition: Compounds or agents that combine with an enzyme in such a manner as to prevent the normal substrate-enzyme combination and the catalytic reaction.

Registry Number: 0

Descriptor UI: D004791

Alternative terms: Enzyme Inhibitors; Inhibitors, Enzyme;

Allowable Qualifiers: administration & dosage; adverse effects; analysis; blood; cerebrospinal fluid; chemical synthesis; classification; diagnostic use; economics; history; immunology; isolation & purification; metabolism; pharmacokinetics; pharmacology; poisoning; radiation effects; standards; supply & distribution; therapeutic use; toxicity; urine; chemistry; contraindications; agonists;

Tree Number: D27.505.519.389;

Online Note: search ENZYMES /AI 1968-74 & ENZYMES 1966-67

History Note: 75,64-67

Technical Notes: GEN only; prefer specifics