PMID-sentid Pub_year Sent_text compound_name comp_offset prot_official_name organism prot_offset 14830-11 1977 The carbodiimide-reactive groups were not identical with the two carboxylate groups recently found to react with conduritol-B-epoxide, an active-site-directed inhibitor of sucrase-isomaltase (Quaroni, A. and Semenza, G., 1976, J. Biol. conduritol epoxide 113-133 sucrase-isomaltase, intestinal Oryctolagus cuniculus 172-190 33720-2 1979 Injection of a single dose of conduritol B epoxide into mice produced almost complete destruction of glucocerebrosidase (D-glucosyl-N-acylsphingosine glucohydrolase, EC 3.2.1.45) in liver, spleen, brain, and kidney within 5 h. Restoration of activity became noticeable within 1 day (2 days in the case of brain) and was about 80% of normal within 16 days. conduritol epoxide 30-50 glucosidase, beta, acid Mus musculus 101-119 560212-0 1977 Stereospecific ring opening of conduritol-B-epoxide by an active site asparatate residue of sucrase-isomaltase. conduritol epoxide 31-51 sucrase-isomaltase Homo sapiens 92-110 560212-1 1977 Conduritol-B-epoxide inactivates sucrase-isomaltase (sucrose alpha-glucohydrolase, EC 3.2.1.48-dextrin 6-alpha-glucohydrolase, EC 3.2.1.10) irreversibly with incorporation of 1 mol inhibitor/mol subunit, the affinity label being bound in both subunits to a beta-carboxyl group of an aspartic acid (Quaroni, A. and Semnza; G. (1976) J. Biol. conduritol epoxide 0-20 sucrase-isomaltase Homo sapiens 33-51 27655403-4 2016 A nGD cell model (CBE-N2a) was created by inhibiting acid beta-glucosidase (GCase) in N2a cells with conduritol B epoxide (CBE). conduritol epoxide 101-121 glucosidase, beta, acid Mus musculus 76-81 32743826-4 2021 We now induce nGD in mice by injection with conduritol B-epoxide (CBE), an irreversible inhibitor of acid beta-glucosidase (GCase), the enzyme defective in nGD, with or without co-injection with Genz-667161, a prototype for SRT which crosses the BBB. conduritol epoxide 44-64 glucosidase, beta, acid Mus musculus 124-129 32743826-4 2021 We now induce nGD in mice by injection with conduritol B-epoxide (CBE), an irreversible inhibitor of acid beta-glucosidase (GCase), the enzyme defective in nGD, with or without co-injection with Genz-667161, a prototype for SRT which crosses the BBB. conduritol epoxide 66-69 glucosidase, beta, acid Mus musculus 124-129 28166796-5 2017 Chemically-induced Gaucher macrophages were developed by differentiateing THP-1 monocytes to macrophages by treatment with phorbol 12-myristate 13-acetate (PMA) and then inhibiting intracellular GCase with conduritol B-epoxide (CBE), a specific irreversible inhibitor of GCase activity, and supplementing the medium with exogenous GlcCer. conduritol epoxide 206-226 glucosylceramidase beta Homo sapiens 195-200 28242245-4 2017 Using SH-SY5Y cells, complex I deficiency was modelled by using rotenone whilst GBA1 deficiency was modelled by the use of conduritol B epoxide (CBE). conduritol epoxide 123-143 glucosylceramidase beta Homo sapiens 80-84 27234572-3 2016 Chemical induction of GD by inhibition of acid beta-glucosidase (GCase) using the irreversible inhibitor conduritol B-epoxide (CBE) is particularly attractive, although few systematic studies examining the effect of CBE on the development of symptoms associated with neurological forms of GD have been performed. conduritol epoxide 105-125 glucosidase, beta, acid Mus musculus 47-63 27234572-3 2016 Chemical induction of GD by inhibition of acid beta-glucosidase (GCase) using the irreversible inhibitor conduritol B-epoxide (CBE) is particularly attractive, although few systematic studies examining the effect of CBE on the development of symptoms associated with neurological forms of GD have been performed. conduritol epoxide 105-125 glucosidase, beta, acid Mus musculus 65-70 27126635-5 2016 Partial inhibition of glucocerebrosidase activity in PrP-A53T-SNCA mice using the covalent inhibitor conduritol-B-epoxide induced a profound increase in soluble alpha-synuclein in the CNS and exacerbated cognitive and motor deficits. conduritol epoxide 101-121 glucosidase, beta, acid Mus musculus 22-40 27126635-5 2016 Partial inhibition of glucocerebrosidase activity in PrP-A53T-SNCA mice using the covalent inhibitor conduritol-B-epoxide induced a profound increase in soluble alpha-synuclein in the CNS and exacerbated cognitive and motor deficits. conduritol epoxide 101-121 prion protein Mus musculus 53-56 27126635-5 2016 Partial inhibition of glucocerebrosidase activity in PrP-A53T-SNCA mice using the covalent inhibitor conduritol-B-epoxide induced a profound increase in soluble alpha-synuclein in the CNS and exacerbated cognitive and motor deficits. conduritol epoxide 101-121 synuclein, alpha Mus musculus 62-66 27126635-5 2016 Partial inhibition of glucocerebrosidase activity in PrP-A53T-SNCA mice using the covalent inhibitor conduritol-B-epoxide induced a profound increase in soluble alpha-synuclein in the CNS and exacerbated cognitive and motor deficits. conduritol epoxide 101-121 synuclein, alpha Mus musculus 161-176 26909767-6 2016 We established that zebrafish has endogenous beta-glucosidase activity toward lipid- and water-soluble GBA2 substrates, which can be inhibited by miglustat, N-butyldeoxygalactonojirimycin, and conduritol B epoxide. conduritol epoxide 193-213 glucosidase, beta (bile acid) 2 Danio rerio 103-107 26995090-4 2016 Additionally, three dimensional cultured skin was incubated with SM-L and the beta-GCase inhibitor conduritol B epoxide (CBE) and the ceramide content determined by high performance thin layer chromatography. conduritol epoxide 99-119 glucosylceramidase beta Homo sapiens 78-88 26104567-5 2015 Conversely, we could show that inhibition of GCase activity with conduritol-B-epoxide (CBE) enhances both alpha-Syn and MPP(+) induced toxicity in vitro. conduritol epoxide 65-85 glucosidase, beta, acid Mus musculus 45-50 26104567-5 2015 Conversely, we could show that inhibition of GCase activity with conduritol-B-epoxide (CBE) enhances both alpha-Syn and MPP(+) induced toxicity in vitro. conduritol epoxide 65-85 synuclein, alpha Mus musculus 106-115 26104567-5 2015 Conversely, we could show that inhibition of GCase activity with conduritol-B-epoxide (CBE) enhances both alpha-Syn and MPP(+) induced toxicity in vitro. conduritol epoxide 87-90 glucosidase, beta, acid Mus musculus 45-50 26104567-5 2015 Conversely, we could show that inhibition of GCase activity with conduritol-B-epoxide (CBE) enhances both alpha-Syn and MPP(+) induced toxicity in vitro. conduritol epoxide 87-90 synuclein, alpha Mus musculus 106-115 24599400-9 2014 In cultured wild-type brain cortical neural cells, the GCase-irreversible inhibitor, conduritol B epoxide (CBE), reproduced the APP/alpha-synuclein aggregation and the accumulation of GC/GS. conduritol epoxide 85-105 synuclein, alpha Mus musculus 132-147 23880767-4 2013 We have addressed the ambiguity surrounding one of the defining characteristics of GBA2, which is its sensitivity to inhibition by conduritol B epoxide (CBE). conduritol epoxide 131-151 glucosidase beta 2 Mus musculus 83-87 24211208-8 2013 In addition, purified recombinant GBA1 exhibits conduritol B-epoxide-sensitive cholesterol glucosylation activity. conduritol epoxide 48-68 glucosylceramidase beta Homo sapiens 34-38 23880767-4 2013 We have addressed the ambiguity surrounding one of the defining characteristics of GBA2, which is its sensitivity to inhibition by conduritol B epoxide (CBE). conduritol epoxide 153-156 glucosidase beta 2 Mus musculus 83-87 22451348-4 2012 Similarly, conduritol B epoxide, an inhibitor of beta-glucocerebrosidase, significantly down-regulated SC ceramide levels and significantly increased glucosylceramide levels. conduritol epoxide 11-31 glucosylceramidase beta Homo sapiens 49-72 19587377-5 2009 Transcriptome analysis on normal MSCs treated with the glucocerebrosidase inhibitor conduritol B epoxide showed an up-regulation of an array of inflammatory mediators, including CCL2, and other differentially regulated pathways. conduritol epoxide 84-104 C-C motif chemokine ligand 2 Homo sapiens 178-182 19651460-0 2010 Uncoupling between CD1d upregulation induced by retinoic acid and conduritol-B-epoxide and iNKT cell responsiveness. conduritol epoxide 66-86 CD1d molecule Homo sapiens 19-23 19651460-4 2010 We also show that retinoic acid (RA) and the beta-glucocerebrosidase inhibitor conduritol-B-epoxide (CBE) lead to upregulation of CD1d expression by THP-1 cells, which correlated with an increase in mRNA expression. conduritol epoxide 79-99 glucosylceramidase beta Homo sapiens 45-68 19651460-4 2010 We also show that retinoic acid (RA) and the beta-glucocerebrosidase inhibitor conduritol-B-epoxide (CBE) lead to upregulation of CD1d expression by THP-1 cells, which correlated with an increase in mRNA expression. conduritol epoxide 79-99 CD1d molecule Homo sapiens 130-134 19576930-3 2009 We inhibited glucocerebrosidase (GCase) with conduritol B epoxide (CBE) in neuroblastoma cells and mice to test whether a biological link exists between GCase activity and alpha-syn. conduritol epoxide 45-65 glucosidase, beta, acid Mus musculus 13-31 19576930-3 2009 We inhibited glucocerebrosidase (GCase) with conduritol B epoxide (CBE) in neuroblastoma cells and mice to test whether a biological link exists between GCase activity and alpha-syn. conduritol epoxide 45-65 glucosidase, beta, acid Mus musculus 33-38 15890646-4 2005 Here, we show that apoA-I-mediated cholesterol efflux was inhibited (by up to 53% over 8 h) when fibroblasts were treated with lactosylceramide or the glucocerebrosidase inhibitor conduritol B epoxide. conduritol epoxide 180-200 apolipoprotein A1 Homo sapiens 19-25 18346921-4 2008 Conduritol B epoxide (CBE, a covalent inhibitor of GCase) treatment (for 8-12 days) of wild type, D409H, D409V or V394L homozygotes recapitulated the CNS phenotype of the kn-9H mice with seizures, tail arching, shaking, tremor, quadriparesis, extensive neuronal degeneration loss and apoptosis, and death by the age of 14 days. conduritol epoxide 0-20 glucosidase, beta, acid Mus musculus 51-56 17482853-2 2007 We now demonstrate that treatment of macrophages with conduritol-B-epoxide (CBE), a glucocerebrosidase inhibitor, results in elevated activity of CTP:phosphocholine cytidylyltransferase (CCT), the rate-limiting enzyme in the pathway of PC biosynthesis. conduritol epoxide 54-74 phosphate cytidylyltransferase 1, choline, alpha isoform Mus musculus 146-185 17482853-2 2007 We now demonstrate that treatment of macrophages with conduritol-B-epoxide (CBE), a glucocerebrosidase inhibitor, results in elevated activity of CTP:phosphocholine cytidylyltransferase (CCT), the rate-limiting enzyme in the pathway of PC biosynthesis. conduritol epoxide 54-74 phosphate cytidylyltransferase 1, choline, alpha isoform Mus musculus 187-190 15817452-0 2005 X-ray structure of human acid-beta-glucosidase covalently bound to conduritol-B-epoxide. conduritol epoxide 67-87 glucosylceramidase beta Homo sapiens 25-46 15916690-3 2005 We now show that GluCerase-deficient monocytes from GD patients or monocytes from healthy subjects treated with conduritol-B-epoxide (CBE), an irreversible inhibitor of GluCerase activity, display high levels of surface expression of the lipid-binding molecule CD1d. conduritol epoxide 112-132 CD1d molecule Homo sapiens 261-265 10037475-2 1999 Incubation of NG108-15 cells with conduritol-B-epoxide, a covalent inhibitor of glucosylceramidase, raised the intracellular concentration of glucosylceramide (GC) by more than fourfold, indicating a glycolipid composition equivalent to that of Gaucher"s cells. conduritol epoxide 34-54 glucosidase, beta, acid Mus musculus 80-98 12401882-5 2002 Treatment of fibroblasts or RAW macrophages with conduritol B epoxide, an inhibitor of lysosomal glucocerebrosidase, resulted in a change in the endocytic targeting of lactosylceramide from the Golgi to the lysosomes. conduritol epoxide 49-69 glucosylceramidase beta Homo sapiens 87-115 1386724-8 1992 Conduritol B epoxide is also known to inhibit glucocerebrosidase and induce Gaucher"s like-disease in mice by repetitive injection. conduritol epoxide 0-20 glucosidase, beta, acid Mus musculus 46-64 7769132-5 1995 Topical applications of conduritol B epoxide, a specific irreversible inhibitor of beta-glucocerebrosidase, increased epidermal GlcCer levels twofold, an alteration localized largely to the basal, proliferative cell layer (fourfold increase); and stimulated epidermal proliferation (2.3-fold elevation in [3H]thymidine incorporation; P < or = 0.001), localized autoradiographically again to the basal layer, and resulting in epidermal hyperplasia. conduritol epoxide 24-44 glucosidase, beta, acid Mus musculus 83-106 7766184-1 1995 The modification of amino acid residues in sugar beet alpha-glucosidase with conduritol B epoxide (CBE), an affinity labeling reagent, inactivated the enzyme. conduritol epoxide 77-97 alpha-glucosidase Beta vulgaris subsp. vulgaris 54-71 1386724-9 1992 Cyclophellitol was shown to be more potent than conduritol B epoxide in inhibition of glucocerebrosidase and in induction of the neural abnormality. conduritol epoxide 48-68 glucosidase, beta, acid Mus musculus 86-104 3087971-3 1986 Conduritol B epoxide (CBE) and its brominated derivative are mechanism-based inhibitors which bind covalently to the catalytic site of acid beta-glucosidase. conduritol epoxide 0-20 glucosylceramidase beta Homo sapiens 135-156 1731615-2 1992 The role of glucosylceramide metabolism was explored further by exposing Madin-Darby canine kidney (MDCK) cells to the beta-glucosidase inhibitor conduritol B epoxide, which produced time-dependent and concentration-dependent increases in glucosylceramide levels and decreased bradykinin-stimulated inositol trisphosphate formation from isolated MDCK cell membranes. conduritol epoxide 146-166 kininogen 1 Canis lupus familiaris 277-287 34459538-5 2021 Here we show that the xylopyranose preference also holds up for covalent inhibitors: xylose-configured cyclophellitol and cyclophellitol aziridines selectively react with GBA over GBA2 and GBA3 in vitro and in vivo , and that the xylose-configured cyclophellitol is more potent and more selective for GBA than the classical GBA inhibitor, conduritol B-epoxide (CBE). conduritol epoxide 339-359 glucosylceramidase beta Homo sapiens 171-174 34459538-5 2021 Here we show that the xylopyranose preference also holds up for covalent inhibitors: xylose-configured cyclophellitol and cyclophellitol aziridines selectively react with GBA over GBA2 and GBA3 in vitro and in vivo , and that the xylose-configured cyclophellitol is more potent and more selective for GBA than the classical GBA inhibitor, conduritol B-epoxide (CBE). conduritol epoxide 339-359 glucosylceramidase beta Homo sapiens 324-327 34459538-5 2021 Here we show that the xylopyranose preference also holds up for covalent inhibitors: xylose-configured cyclophellitol and cyclophellitol aziridines selectively react with GBA over GBA2 and GBA3 in vitro and in vivo , and that the xylose-configured cyclophellitol is more potent and more selective for GBA than the classical GBA inhibitor, conduritol B-epoxide (CBE). conduritol epoxide 361-364 glucosylceramidase beta Homo sapiens 171-174 34459538-5 2021 Here we show that the xylopyranose preference also holds up for covalent inhibitors: xylose-configured cyclophellitol and cyclophellitol aziridines selectively react with GBA over GBA2 and GBA3 in vitro and in vivo , and that the xylose-configured cyclophellitol is more potent and more selective for GBA than the classical GBA inhibitor, conduritol B-epoxide (CBE). conduritol epoxide 361-364 glucosylceramidase beta Homo sapiens 324-327 1856189-2 1991 The substrate analogue conduritol B epoxide (CBE) is demonstrated to be an active site-directed inhibitor of human lysosomal alpha-glucosidase. conduritol epoxide 23-43 alpha glucosidase Homo sapiens 115-142 3943537-1 1986 The kinetics of glucocerebrosidase synthesis and degradation in rat peritoneal macrophages and in human fibroblasts have been studied using conduritol B epoxide (CBE), an irreversible and specific inhibitor of mammalian glucocerebrosidase. conduritol epoxide 140-160 glucosylceramidase beta Rattus norvegicus 220-238 6693432-5 1984 These effectors also increased the reactivity of glucocerebrosidase to the inhibitor conduritol B epoxide; HSF alone had no effect (t1/2 = 19 +/- 0.5 min) whereas the maximum rate of inactivation (t1/2 = 4.0 min) by conduritol B epoxide was achieved in the presence of a mixture of PS (1 microgram) and HSF (3 micrograms). conduritol epoxide 85-105 interleukin 6 Homo sapiens 107-110