• 1.-.-.- Oxidoreductases: aldo-keto reductase family 1 member B. Last modified on 13/08/2015. (guidetopharmacology.org)
  • 2005) Discovery of 3-[(4,5,7-trifluorobenzothiazol-2-yl)methyl]indole-N-acetic acid (lidorestat) and congeners as highly potent and selective inhibitors of aldose reductase for treatment of chronic diabetic complications. (guidetopharmacology.org)
  • Based on overlapping structural requirements for both efficient aldose reductase inhibitors and PPAR ligands, [5-(benzyloxy)-1H-indol-1-yl] acetic acid (compound 1) was assessed for inhibition of aldose reductase and ability to interfere with PPAR gamma. (metu.edu.tr)
  • The carboxymethylated enzyme was less sensitive than the reduced enzyme to most aldose reductase inhibitors including sorbinil (d-6-fluoro-spiro[chroman-4,4'-im idazolidine]-2',5'-dione), except tolrestat (N-methyl-N-[(5-trifluromethyl-6-methoxy-1-naphthalenyl)-thiomethyl]glyc ine) and quercetin. (utmb.edu)
  • Finally, inhibition analysis was done using non-steroidal anti-inflammatory drugs (NSAIDs) as potential inhibitors. (ox.ac.uk)
  • Part I. The Rational Design, Synthesis and Evaluation of Second Generation Class II HMG-CoA Reductase Inhibitors Part II. (purdue.edu)
  • Over 100 protease inhibitors are currently used in the clinics, and most of them use blockage of the active site for their mode of inhibition. (cipsm.de)
  • The enzymatic requirements for EtOH to inhibit RA biosynthesis were studied using inhibitors of the middle-chain alcohol dehydrogenases (ADH), 4-methylpyrazole (4MP), or the short-chain dehydrogenase/reductases, carbenoxolone (CBX) and chloral hydrate (CH). Late blastula stage embryos were treated with EtOH alone or in combination with 4MP (a,b), CH (c,d) or CBX (e,f). (xenbase.org)
  • The polyol pathway is a glucose metabolic shunt that is defined by two enzymatic reactions catalyzed by aldose reductase (AR, AKR1B1, EC1.1.1.21) and sorbitol dehydrogenase (SDH, EC1.1.1.14), respectively [ 1 , 2 ]. (hindawi.com)
  • Three human PG reductases (PGR), zinc-independent members of the medium-chain dehydrogenase/reductase (MDR) superfamily, perform the first irreversible step of the degradation pathway. (ox.ac.uk)
  • We have focused on the characterization of the recombinant human enzyme prostaglandin reductase 1 (PGR1), also known as leukotriene B4 dehydrogenase. (ox.ac.uk)
  • Disulfiram, an inhibitor of aldehyde dehydrogenase, also blocks the 20‐carboxy‐LXB 4 formation. (elsevierpure.com)
  • These observations suggest that both alcohol dehydrogenase and aldehyde dehydrogenase participate in the oxidation of 20‐hydroxy‐LXB 4 to 20‐carboxy‐LXB 4 . (elsevierpure.com)
  • Pharmacological inhibition of the embryonic alcohol dehydrogenase activity, prevents the oxidation of ethanol to acetaldehyde that in turn functions as a RALDH2 inhibitor. (xenbase.org)
  • In the last step, a NADPH-dependent cinnamyl alcohol dehydrogenase, also called monolignol dehydrogenase (EC 1.1.1.195), catalyzes the reduction of the aldehyde group to an alcohol group, with the formation of the aforementioned monolignols. (tuscany-diet.net)
  • Aldose reductase inhibition by 1 was characterized by IC50 in submicromolar and low micromolar range, for rat and human enzyme, respectively. (metu.edu.tr)
  • Carboxymethylation of Cys-298 was also found to affect NADPH and aldehyde binding to the enzyme. (utmb.edu)
  • Quercetin is a specific quinone reductase 2 (QR2) inhibitor, an enzyme (along with the human QR1 homolog) which catalyzes metabolism of toxic quinolines. (ncats.io)
  • Diacetyl was metabolized in nasal tissues in vitro, likely by is metabolized by diacetyl reductase (also known as diacetyl reductase, an enzyme known to be inhibited by butyric dicarbonyl nicotine adenine dinucleotide phosphate reductase acid. (cdc.gov)
  • Competitive inhibition ELISA reiterates the direct binding results. (scialert.net)
  • 2. Oka M, Matsumoto Y, Sugiyama S, Tsuruta N, Matsushima M. (2000) A potent aldose reductase inhibitor, (2S,4S)-6-fluoro-2', 5'-dioxospiro[chroman-4,4'-imidazolidine]-2-carboxamide (Fidarestat): its absolute configuration and interactions with the aldose reductase by X-ray crystallography. (guidetopharmacology.org)
  • Moreover, chamomile extract showed potent inhibition against aldose reductase (ALR2), with an IC50 value of 16.9 microg/mL, and its components, umbelliferone (1), esculetin (3), luteolin (6), and quercetin (7), could significantly inhibit the accumulation of sorbitol in human erythrocytes. (nih.gov)
  • We have performed an extensive kinetic characterization of PGR1, which catalyzes the NADPH-dependent reduction of the α,β-double bond of aliphatic and aromatic aldehydes and ketones, and 15-keto-PGs. (ox.ac.uk)
  • These enzymes catalyze the conversion of aldehydes and ketones to their corresponding alcohols by utilizing NADH and/or NADPH as cofactors. (cancerindex.org)
  • The review is summarized and systematized the published data on the multicomponent reactions of ethyl trifluoroacetoacetate, carbonyl compounds (aldehydes and ketones), and nucleophilic reagents. (researchgate.net)
  • In the inactivating pathway of PGs, the first metabolic intermediates are 15-keto-PGs, which are further converted into 13,14-dihydro-15-keto-PGs by different enzymes having 15-keto-PG reductase activity. (ox.ac.uk)
  • This gene encodes a member of the aldo/keto reductase superfamily, which consists of more than 40 known enzymes and proteins. (cancerindex.org)
  • Glutathione, a powerful antioxidant, which also plays a key role in detoxifying reactive aldehydes, protects certain bacteria from oxidative stress, and could also be implicated in resistance to reuterin. (biomedcentral.com)
  • Inhibition of QR2 in plasmodium may potentially cause lethal oxidative stress. (ncats.io)
  • Nature has evolved a number of enzymatic reactions to produce aldehydes, and this review provides an overview of aldehyde-forming reactions in biological systems and beyond. (tuwien.ac.at)
  • 1975. Effect of chloroquine on cultured fibroblasts: release of lysosomal hydrolases and inhibition of their uptake. . (umass.edu)
  • However, insufficient supply of NAD(P)H for XR and inhibition of xylose uptake by glucose are identified as major constraints for achieving high xylitol productivity. (illinois.edu)
  • We previously demonstrated in streptozotocin-induced diabetic mice that deficiency or inhibition of aldose reductase (AR) caused significant dephosphorylation of hepatic transcriptional factor PPAR α , leading to its activation and significant reductions in serum lipid levels. (hindawi.com)
  • Herein, we report that inhibition of AR by zopolrestat or by a short-hairpin RNA (shRNA) against AR caused a significant reduction in serum and hepatic triglycerides levels in 10-week old diabetic db/db mice. (hindawi.com)
  • Recently, we demonstrated that deficiency or inhibition of AR caused significant dephosphorylation of hepatic PPAR α , leading to the activation of this transcriptional factor as well significant reduction in serum TG levels in streptozotocin-(STZ-) diabetic mice, an experimental model for type I diabetes mellitus (T1DM) [ 17 ]. (hindawi.com)
  • Diabetic-like retinopathy in rats prevented with an aldose reductase inhibitor. (koreamed.org)
  • Together, these data indicate that inhibition of AR might lead to significant amelioration in hyperglycemia-induced dyslipidemia and nonalcoholic fatty liver disease. (hindawi.com)
  • Our data suggest that inhibition of AR in the T2DM db/db mice led to significant activation in hepatic PPAR α and significant reductions in serum triglycerides (TG) and hepatic TG, suggesting that under hyperglycemia, AR/the polyol pathway might be greatly upregulated to contribute significantly to the hepatic regulation of TG metabolism and the development of nonalcoholic steatohepatitis (NASH) or nonalcoholic fatty liver disease (NAFLD). (hindawi.com)
  • Hot water extract, esculetin (3) and quercetin (7) have been found to show moderate inhibition of sucrase with IC50 values of 0.9 mg/mL and 72 and 71 microM, respectively. (nih.gov)
  • Thus, e.g., inhibition of metabolic changes including air trapping, bronchial wall thickening, and clearance pathways leads to a diminished scrubbing capacity constrictive bronchiolitis (Akpinar-Elci et al. (cdc.gov)
  • Alcohol consumption during pregnancy induces Fetal Alcohol Spectrum Disorder (FASD), which has been proposed to arise from competitive inhibition of retinoic acid (RA) biosynthesis. (xenbase.org)
  • Ethanol-dependent retinoic acid inhibition requires middle-chain alcohol dehydrogenases. (xenbase.org)
  • In the second step, a NADPH-dependent cinnamoyl-CoA: oxidoreductase, also called cinnamoyl-CoA reductase (EC1.2.1.44) catalyzes the formation of the corresponding aldehydes, and the release of coenzyme A. (tuscany-diet.net)
  • Prostaglandins (PGs) are lipid compounds derived from arachidonic acid by the action of cyclooxygenases, acting locally as messenger molecules in a wide variety of physiological processes, such as inflammation, cell survival, apoptosis, smooth muscle contraction, adipocyte differentiation, vasodilation and platelet aggregation inhibition. (ox.ac.uk)
  • Of the second generation analogue set, two compounds were found to possess improved enzymatic inhibition compared to that of the most biologically active first generation analogue. (purdue.edu)
  • Many aldehydes are volatile compounds with distinct and characteristic olfactory properties. (tuwien.ac.at)
  • 3. Singh SB, Malamas MS, Hohman TC, Nilakantan R, Carper DA, Kitchen D. (2000) Molecular modeling of the aldose reductase-inhibitor complex based on the X-ray crystal structure and studies with single-site-directed mutants. (guidetopharmacology.org)
  • We provide biochemical and developmental evidence identifying acetaldehyde as responsible for this inhibition. (xenbase.org)
  • RESULTS- Activation of nrf2 by sulforaphane induced nuclear translocation of nrf2 and increased ARE-linked gene expression, for example, three- to fivefold increased expression of transketolase and glutathione reductase. (diabetesjournals.org)
  • Evidence for the formation of the cytotoxic aldehyde acrolein from enzymatically oxidized spermine or spermidine. (cdc.gov)
  • Each red arrow is a long-range allosteric influence, either activation (arrow) or inhibition (bar). (biomedcentral.com)
  • We here identify and characterize some of the specific bacterial targets and show a unique inhibition of the azoreductase family. (cipsm.de)
  • Specific inhibition of GhFAD2-3 using the RNA interference approach resulted in male sterility due to impaired anther development at the stages from meiosis to maturation. (researchsquare.com)
  • In the present work, we have developed a new HPLC-based method for the determination of the 15-keto-PG reductase activity. (ox.ac.uk)
  • The inhibition of antioxidant activity in plasmodium may contribute to killing the malaria causing parasites. (ncats.io)
  • 1963. Spectrophotometric analysis of aldehydes in the Los Angeles atmosphere. (cdc.gov)
  • As Saccharomyces cerevisiae cannot utilize xylose as a carbon source, expression of XYL1 coding for xylose reductase (XR) from Scheffersomyces (Pichia) stipitis enabled production of xylitol from xylose with a high yield. (illinois.edu)
  • Antioxidative and aldose reductase (AR)-inhibitory effects of a fermentation filtrate of Rubus coreanus (FRC) were investigated using corneal/retinal homogenate and lens cytosol, respectively. (koreamed.org)
  • 4. Steuber H, Zentgraf M, Gerlach C, Sotriffer CA, Heine A, Klebe G. (2006) Expect the unexpected or caveat for drug designers: multiple structure determinations using aldose reductase crystals treated under varying soaking and co-crystallisation conditions. (guidetopharmacology.org)