• These compounds were very effective inhibitors (low nanomolar) of the human mitochondrial carbonic anhydrase isozymes VA and VB. (edu.au)
  • We report here that the previously described carbonic anhydrase from Aedes aegypti is similar to mammalian CA IV in that it is a GPI-linked peripheral membrane protein. (silverchair.com)
  • Corticosteroid 11-β-dehydrogenase isozyme 2 is an NAD+-dependent enzyme expressed in aldosterone-selective epithelial tissues such as the kidney, colon, salivary and sweat glands. (wikipedia.org)
  • The blood-brain barrier (BBB) and the blood-spinal cord barrier (BSCB) are responsible for controlling the microenvironment within neural tissues in humans. (hindawi.com)
  • Aminopeptidase P isozyme expression in human tissues and peripheral blood mononuclear cell fractions. (nih.gov)
  • Wilson JE, Chandrasekharan NV, Westover KD, Eager KB, Simmons DL: Determination of expression of cyclooxygenase-1 and -2 isozymes in canine tissues and their differential sensitivity to nonsteroidal anti-inflammatory drugs. (hmdb.ca)
  • Apremilast, also known as Otezla, is a phosphodiesterase 4 (PDE4) inhibitor used to treat various types of symptoms resulting from certain inflammatory autoimmune diseases. (drugbank.com)
  • The full mechanism of action of this drug is not fully established, however, it is known that apremilast is an inhibitor of phosphodiesterase 4 (PDE4), which mediates the activity of cyclic adenosine monophosphate (cAMP), a second messenger. (drugbank.com)
  • Characterization of cyclic AMP phosphodiesterase isozymes in rat parotid gland. (shengsci.com)
  • Cyclic AMP phosphodiesterase (PDE) isozymes were isolated and characterized from the soluble fraction of rat parotid gland. (shengsci.com)
  • Two of 15 human livers expressed a second immunoreactive microsomal protein of higher apparent Mr and were more active in midazolam 1'-hydroxylation. (aspetjournals.org)
  • Its metabolism is mediated mainly by cytochrome P450 microsomal isozymes 3A4 (major route) and 2C9 (minor route). (chembase.cn)
  • A specific high performance liquid Chromatographie assay has been developed for the measurement of paracetamol glucuronide formation by the microsomal fraction of human liver. (edu.au)
  • Dive into the research topics of 'Monoclonal anti-human aldolase C antibodies that react to the isozyme group-specific sequences and generally conserved sequences of human aldolase C'. Together they form a unique fingerprint. (elsevierpure.com)
  • Kaihara R, Matsuhashi S , Kusakabe T , Kondo T, Iwanaga A, Hori K. Monoclonal anti-human aldolase C antibodies that react to the isozyme group-specific sequences and generally conserved sequences of human aldolase C . Journal of biochemistry . (elsevierpure.com)
  • Corticosteroid 11-β-dehydrogenase isozyme 2 also known as 11-β-hydroxysteroid dehydrogenase 2 is an enzyme that in humans is encoded by the HSD11B2 gene. (wikipedia.org)
  • These studies have provided fundamental insights into UGT gene structure and regulation, isozyme substrate selectivity, and interindividual variability. (aspetjournals.org)
  • The UGT1 family constitutes a complex gene locus on human chromosome 2q37 and comprises 13 first exons that encode the unique N-terminal domains of the UGT1A proteins and exons 2 to 5 that encode the C-terminal domain, which is identical in all UGT1A family members ( Owens and Ritter, 1992 ). (aspetjournals.org)
  • FHM type 4 is attributed to mutations in the PRRT2 gene, which encodes a proline-rich transmembrane protein of as yet unknown function. (frontiersin.org)
  • We have successfully used a DNA.cDNA molecular hybridization assay to directly determine the presence or absence of human beta globin gene sequences in 20 human-mouse somatic cell hybrids, each of which contained a different subset of human chromosomes. (eurekamag.com)
  • The assay is specific for the individual human globin genes and will detect the presence of a globin gene if the relevant chromosome is present in only 10% of the cells of a hybrid population. (eurekamag.com)
  • All human chromosomes were present in one or more cell lines devoid of the human beta globin gene except for 6, 8, 9, 11, and 13. (eurekamag.com)
  • Among these latter chromosomes, only chromosome 11 was present in the six hybrid clones that contained the human beta globin gene. (eurekamag.com)
  • In fact, chromosome 11 was the only human chromosome that was present in all of the six hybrid clones found to be positive for the human beta globin gene. (eurekamag.com)
  • 157-BNPT-4 contained the human beta globin gene while 157-BNPT-1 did not. (eurekamag.com)
  • two lines positive for human beta globin gene sequences also contained human gamma globin gene sequences while one line was negative for both beta and gamma gene sequences. (eurekamag.com)
  • The metabolism of midazolam and triazolam to their 1'-hydroxy and 4-hydroxy metabolites was studied in microsomes of 15 human livers. (aspetjournals.org)
  • We conclude that the metabolism of midazolam and triazolam in human liver is predominantly mediated by cytochrome P450IIIA4. (aspetjournals.org)
  • The regio- and stereoselective metabolism of phenanthrene (PA) by seven cDNA-expressed human and five rodent and rabbit cytochromes P-450 has been examined using reverse-phase and chiral stationary phase high-pressure liquid chromatography (HPLC). (nih.gov)
  • Regioselectivities for PA metabolism were found to be both isozyme and species-dependent. (nih.gov)
  • The Effect of 4-Hydroxyindoles on the Metabolism of 5-Hydroxytryptamin. (erowid.org)
  • Comparison of the metabolism of 3,4-dimethoxyphenylethylamine and mesc. (erowid.org)
  • Confocal studies showed differential cellular and compartmental distribution of isozymes involved in glucose, glutamate, glutamine, lactate, and creatine metabolism. (molvis.org)
  • in an inhalation study and only equivocal evidence of metabolism to SO is below the limit of detection in nearly all samples, and the most active sample of lung lung tumors in two of four chronic toxicity/oncogenicity was approximately 100-fold less active than mouse studies by gavage in mice (reviewed in Cruzan et al . (cdc.gov)
  • Each inhibitor has its personal specificity towards one of extra of these isozymes, causing differential effects Research in wholesome volunteers offered p38/p38 inhibitors found reductions in pro-inflammatory cytokine secretion from ex-vivo LPS-stimulated peripheralblood mononuclear cells (PBMCs) (Parasrampuria et al 2003), and decreased LPS-induced pro-inflammatory cytokine production, neutrophil and endothelial-cell activation in vivo. (deubiquitinaseinhibitor.com)
  • The procedure has been used to characterize paracetamol glucuronidation kinetics in human liver microsomes and to assess the substrate specificity of the paracetamol UDP-glucuronosyltransferase (UDPGT) activity. (edu.au)
  • The nature of the enzyme(s) catalyzing the major metabolic pathway of diclofenac, 4'-hydroxylation, was investigated in human liver microsomes. (nih.gov)
  • This contrasts to the approximately three-fold activation of 4-methylumbelliferone, morphine and 4-nitrophenol glucuronidation observed following Brij 58 treatment of human liver microsomes. (edu.au)
  • Diclofenac 4'-hydroxylation displayed single enzyme Michaelis-Menten kinetics and was similar in microsomes from one poor and five extensive metabolizers of debrisoquin (CYP2D6), with a Km of 5.6 +/- 1.5 microM (mean +/- sd) and a Vmax of 60.6 +/- 23.5 nmol/mgP/h. (nih.gov)
  • Moreover, midazolam hydroxylase activity was immunoprecipitated from solubilized human microsomes with polyclonal antibodies against rat P450PCN1 and the closely related human isozyme P450NF. (aspetjournals.org)
  • So far it is not clear, to which extent such cancer-related or experimentally induced epigenetic alterations correspond to the natural epigenetic variability in human livers. (biomedcentral.com)
  • Although at least 14 unique GSDs are discussed in the literature, the 4 that cause clinically significant muscle weakness are Pompe disease ( GSD type II , acid maltase deficiency ), Cori disease ( GSD type III , debranching enzyme deficiency), McArdle disease ( GSD type V , myophosphorylase deficiency), and Tarui disease (GSD type VII, phosphofructokinase deficiency). (medscape.com)
  • This particular isozyme therefore appears to be responsible for the oxidation of polar acidic substances such as non-steroidal anti-inflammatory drugs from different chemical classes. (nih.gov)
  • A subset of workers in swine confinement facilities develop chronic inflammatory lung disease, and an aqueous hog-barn dust extract (HDE) induces diverse inflammation-related responses in cultured BEAS-2B human airway epithelial cells, including release of inflammatory cytokines. (cdc.gov)
  • These observations have attracted interest in p38 as a molecular target in the therapy of inflammatory human ailments. (deubiquitinaseinhibitor.com)
  • It plays an important role as a glucose-manipulating system that maintains appropriate glucose levels in the human body. (medscape.com)
  • The cause of 5-alpha-reductase type 2 deficiency is the deficiency of the type 2 isozyme of 5-alpha-reductase. (medscape.com)
  • Sulfaphenazole competitively inhibited diclofenac 4'-hydroxylation (Ki = 0.11 +/- 0.08 microM, n = 3). (nih.gov)
  • Diclofenac 4'-hydroxylation is predominantly catalyzed by a cytochrome P450 isozyme of the CYP2C subfamily, most likely CYP2C9. (nih.gov)
  • Monkey COS cells transfected with human P450PCN1 cDNA were able to catalyze both the 1'- and the 4-hydroxylation of midazolam. (aspetjournals.org)
  • Hydroxylation is catalysed by prolyl-4-hydroxylases (PHD isozymes in humans) which are iron(II) and 2-oxoglutarate dependent oxygenases. (ox.ac.uk)
  • Along with the results of previous studies of the kinetics and inhibitor profile of human liver glucuronidation reactions (Miners et al. (edu.au)
  • These responses require the calcium (Ca)-dependent protein kinase C-alpha isozyme, and we showed previously that HDE stimulates Ca elevation in these cells. (cdc.gov)
  • Mechanisms of intracellular calcium elevation in human airway epithelial cells by an airway disease-relevant extract of hog-barn dust. (cdc.gov)
  • Oxidation of midazolam and triazolam by human liver cytochrome P450IIIA4. (aspetjournals.org)
  • icologic and metabolic data that explain the nasal and major differences are 4- to 10-fold more ring-oxidation lung differences and their relevance for human risk and phenylacetaldehyde pathways in mice compared assessment. (cdc.gov)
  • Accumulating evidence demonstrates that many of the 17 human UGTs characterized to date exhibit tissue-specific patterns of expression. (aspetjournals.org)
  • The glucuronidation and elimination of endogenous compounds ( e.g. , bilirubin) and xenobiotics, including HPPH, the major, para -hydroxylated metabolite of the anticonvulsant drug phenytoin (diphenylhydantoin) ( Butler, 1957 ), are catalyzed by a superfamily of membrane-bound isozymes known collectively as UGTs ( Dutton, 1980 ). (aspetjournals.org)
  • Zika Virus Surveillance at the Human-Animal Interface in West-Central Brazil, 2017-2018. (cdc.gov)
  • iii) Ubiquitous mAbs, which react with vertebrate aldolases irrespective of type of isozyme and species (A4 and B7). (elsevierpure.com)
  • Similarly, the ubiquitous mAb B7 should serve as a probe for general use to detect vertebrate aldolases irrespective of isozyme groups and species. (elsevierpure.com)
  • iv) Sub-ubiquitous mAbs, which are closely similar to the ubiquitous mAbs but differ slightly in terms of antigenic specificity (A8 and C1). (elsevierpure.com)
  • The glucuronidated xenobiotics chloramphenicol, digitoxigenin monodigitoxoside, 4-hydroxybiphenyl, 4-methylumbelliferone, morphine, 1-naphthol and 4-nitrophenol were screened for inhibitory effects on paracetamol glucuronidation. (edu.au)
  • 4. Induces epigenetic alterations usual y arises as the cell attempts to repair the DNA damage. (who.int)
  • 3. HEALTH EFFECTS the effects vary with dose and/or duration, and place into perspective the possible significance of these effects to human health. (cdc.gov)
  • Public health officials and others concerned with appropriate actions to take at hazardous waste sites may want information on levels of exposure associated with more subtle effects in humans or animals (LOAELs) or exposure levels below which no adverse effects (NOAELs) have been observed. (cdc.gov)
  • Symptoms had to have been present for at least four weeks and preceded by a pain-free period of four weeks or longer (de Vet et al 2002). (aktinhibitor.com)
  • On the basis of these results, the human beta and gamma globin genes have been assigned to human chromosome 11. (eurekamag.com)
  • Biochem Pharmacol 37: 665-671, 1988 and 37: 2839-2845, 1988), these data indicate that the model glucuronidated substrates paracetamol, morphine and 4-methyllumbelliferone may be used to differentiate at least four human liver UDPGT isozyme activities. (edu.au)
  • A library of 10 novel benzenesulfonamides containing triazole-tethered phenyl 'tail' moieties were synthesized by a Cu(I) catalyzed 1,3-dipolar cycloaddition reaction (DCR) (i.e., click chemistry) between 4-azido benzenesulfonamide and a panel of variously substituted phenyl acetylenes. (edu.au)
  • Because meth use releases a surge of dopamine nearly four times the level that cocaine use does, prolonged meth use over time ultimately destroys dopamine receptors and makes it impossible to feel pleasure. (motorextremeblog.es)
  • Effect of 3,4-dimethoxyphenylethylamine injections upon dopamine metab. (erowid.org)
  • [ 6 ] Both of the pertinent genes, SRD5A1 and SRD5A2 , contain five exons separated by four introns. (medscape.com)
  • Mutations in four genes have been identified in familial hemiplegic migraine (FHM), from which CACNA1A (FHM type 1) and SCN1A (FHM type 3) code for neuronal voltage-gated calcium or sodium channels, respectively, while ATP1A2 (FHM type 2) encodes the α 2 isoform of the Na + ,K + -ATPase's catalytic subunit, thus classifying FHM primarily as an ion channel/ion transporter pathology. (frontiersin.org)
  • This difference in permeability has attracted motor neuron disease (MND) research, with findings suggesting that the BSCB is damaged in human and rodent ALS sufferers. (hindawi.com)
  • A predominance of mutations have been observed in exons 1 and 4. (medscape.com)
  • Finally, perspectives for future research on the implications of Na + ,K + -ATPase mutations in human pathologies are presented. (frontiersin.org)
  • There is a QSPR to estimate the blood:air partition coefficient for human subjects as published by Meulenberg and Vijverberg (2000). (europa.eu)
  • To obtain basic data on the occurrence and distribution of IGF components in human permanent teeth we immunohistochemically investigated 25 extracted, decalcified and paraffin-embedded teeth using mono and polyclonal antibodies against the ligands IGF-I and -II, the IGF1 receptor (IGF1R) and all six IGF binding proteins (IGFBP-1 to -6). (shengsci.com)
  • For the cementum, in the acellular cementum only IGF-II could be detected, while outer cementum layers with inserting Sharpey's fibers reacted with all antibodies applied except for IGFBP-4 and -6. (shengsci.com)
  • BEAS-2B cells were loaded with Fluo-4 and treated with agents to alter various Ca signaling pathways, and the effects of these agents on HDE modulation of intracellular Ca were then assessed by Flex Station assays. (cdc.gov)
  • Aldolase C-specific mAbs B8, H1, B4, and E10, but not D9, have their epitopes on a region within amino acid positions 79-193 of antigens, where the type-C isozyme group-specific sequence-3 (IGS-3) is situated. (elsevierpure.com)
  • Estimates of exposure levels posing minimal risk to humans (Minimal Risk Levels or MRLs) have been made for methyl parathion. (cdc.gov)
  • An MRL is defined as an estimate of daily human exposure to a substance that is likely to be without an appreciable risk of adverse effects (noncarcinogenic) over a specified duration of exposure. (cdc.gov)
  • As these kinds of health effects data become available and methods to assess levels of significant human exposure improve, these MRLs will be revised. (cdc.gov)
  • For the purposes of environmental fate and exposure assessment, a 'block' approach is used, whereby constituents with similar physicochemical and environmental properties are grouped together (Section 4). (europa.eu)
  • However, for exposure of humans via the environment, separate DNELs are calculated for individual blocks using the best available data for each. (europa.eu)
  • GalNAc-T catalyzes the transfer of GalNAc into G(M3) and G(D3) by a beta-1,4 linkage, resulting in the synthesis of G(M2) and G(D2), respectively. (nih.gov)
  • 1,4-DMAA is a chemical with stimulant effects. (motorextremeblog.es)
  • respiratory tract effects in rodents are not relevant for human risk assessment. (cdc.gov)
  • In contrast, ubiquitous mAbs A4 and B7 and sub-ubiquitous mAb A8 may have their epitopes on the commonly conserved regions of the three isozyme groups. (elsevierpure.com)
  • The agents documented and list- ed that carcinogens commonly show tween tumour sites in humans and ed as carcinogenic to humans one or more of 10 key characteristics experimental animals. (who.int)
  • Phenytoin-initiated micronucleus formation was increased about 4-fold in both +/ j (P = .006) and j/j (P = .009) UGT-deficient cells vs. +/+ UGT-normal cells, providing the first evidence that the bioactivation and oxidative toxicity of phenytoin itself may be avoided by direct N -glucuronidation, which was confirmed by tandem mass spectrometry. (aspetjournals.org)
  • The BBB separates the blood from the extracellular cerebrospinal fluid and protects the brain from bloodborne pathogens and toxins while allowing the diffusion of oxygen, carbon dioxide, and small lipophilic molecules/ethanol [ 4 ]. (hindawi.com)
  • The PBPK model predicts that humans do not gener- toxicity, and nasal olfactory lesions. (cdc.gov)
  • More than 60% of patients are diagnosed at late stage of CRC (III-IV) and approximately 25% of them display metastatic disease [ 3 , 4 ]. (biomedcentral.com)
  • L'étude portait sur 20 patients atteints d'un carcinome gastrique, 20 patients souffrant d'une gastrite à H. pylori et 20 personnes en tant que groupe témoin. (who.int)
  • SARS-CoV-2 spike and nucleocapsid proteins fail to activate human dendritic cells or "" T cells. (tcd.ie)
  • To fight MDR, efflux pump inhibitors (EPIs) are an appealing option, and many EPIs that action against the AcrAB-TolC efflux pump have been completely defined in the books (4,C16), among which arylpiperazine and arylmorpholine derivatives constitute a number of the largest systematically analyzed compound classes. (technumber.com)
  • Of the human P-450s, 1A2 and 2B6 have the highest activity and 2C9 has moderate activity. (nih.gov)
  • Using cytochrome P-450s expressed in a lymphoblastoid cell line in presence of epoxide hydrolase (EH), human 1A1 had approximately twice the activity of human 1A2. (nih.gov)
  • Structure of the human aminopeptidase XPNPEP3 and comparison of its in vitro activity with Icp55 orthologs: Insights into diverse cellular processes. (nih.gov)
  • Four main peaks containing PDE activity were obtained by Q-Sepharose Fast Flow column chromatography. (shengsci.com)
  • Micronuclei were not initiated by 10 μM HPPH in +/+ UGT-normal cells but were increased by 4- and 3.8-fold in +/ j and j/j UGT-deficient cells (P = .0001), respectively, and were increased 2.7- and 3.0-fold in +/ j (P = .007) and j/j (P = .0002) UGT-deficient cells, respectively, vs. +/+ UGT-normal cells. (aspetjournals.org)