ライフサイエンスコーパス: glucosylceramide synthase

1 to oral eliglustat, a selective inhibitor of glucosylceramide synthase.

2 argeted disruption of the Ugcg gene encoding glucosylceramide synthase.

3 yldeoxynojirimycin (NB-DNJ), an inhibitor of glucosylceramide synthase, a pivotal enzyme in the early

4 ceptor), and TNF-stimulated Gb3 synthase and glucosylceramide synthase activities but did not affect

5 0.01); both serine palmitoyltransferase and glucosylceramide synthase activities remained unaltered.

6 Because both sphingomyelin synthase and glucosylceramide synthase activities were significantly

7 4'-Hydroxy-P4 and ethylenedioxy-P4 blocked glucosylceramide synthase activity at concentrations tha

8 d by fumonisin B(1) and by overexpression of glucosylceramide synthase; again implicating endogenous

9 ed by PDMP cannot be caused by inhibition of glucosylceramide synthase alone.

10 mal developmental increases in activities of glucosylceramide synthase and cholesterol sulfotransfera

11 lamino-3-morpholino-1-propanol.HCI (PDMP), a glucosylceramide synthase and LacCer synthase (galactosy

12 lamino-3-morpholino-1-propanol.HCl (PDMP), a glucosylceramide synthase and LacCer synthase (GalT-2) i

13 pholino-1-propanol (D-PDMP), an inhibitor of glucosylceramide synthase and lactosylceramide synthase

14 ol (PDMP), which inhibits acid ceramidase or glucosylceramide synthase and then increases endogenous

15 D-PDMP is a potent inhibitor of glucosylceramide synthase and thereby the synthesis of c

16 s compound, D-threo-4'-hydroxy-P4, inhibited glucosylceramide synthase at an IC50 of 90 nM.

17 d-t-EtDO-P4 has the advantage of blocking glucosylceramide synthase at low nanomolar concentration

18 Our results suggest that (a) inhibition of glucosylceramide synthase does not reverse multidrug res

19 Conversely, silencing glucosylceramide synthase expression disrupts Gb3 synthe

20 holesterol and glycosphingolipids, including glucosylceramide synthase (GCS) (gene Ugcg)-derived gang

21 n mammalian sphingomyelin synthase (SMS) and glucosylceramide synthase (GCS) and yeast inositol phosp

22 Glucosylceramide synthase (GCS) catalyzes the transfer o

23 c:ceramide glucosyltransferase (EC 2.4.1.80; glucosylceramide synthase (GCS) from a rat liver and pre

24 Here, we investigated the merits of glucosylceramide synthase (GCS) inhibition as a potentia

25 Glucosylceramide synthase (GCS) inhibitors, including th

26 32 (EXEL-0346) represents a new class of glucosylceramide synthase (GCS) inhibitors.

27 In this study, we have introduced glucosylceramide synthase (GCS) into wild type MCF-7 bre

28 Glucosylceramide synthase (GCS) is a rate-limiting enzym

29 Glucosylceramide synthase (GCS) transfers glucose from U

30 Overexpression of glucosylceramide synthase (GCS), a pivotal enzyme in gly

31 Ceramide glycosylation, through glucosylceramide synthase (GCS), allows cellular escape

32 native approach that involves suppression of glucosylceramide synthase (GCS), an enzyme that glycosyl

33 other glucosylceramide metabolizing enzymes, glucosylceramide synthase (GCS), lysosomal glucosylceram

34 The enzyme glucosylceramide synthase (GCS), responsible for bioacti

35 Glucosylceramide synthase (GCS), the enzyme responsible

36 s was achieved by cellular transfection with glucosylceramide synthase (GCS), the enzyme that convert

37 through up-regulating the gene expression of glucosylceramide synthase (GCS).

38 Since clearance is mediated by glucosylceramide synthase (GCS, EC 2.4.1.80) levels of t

39 Microarray data demonstrated that glucosylceramide synthase (GCS; glucosylceramide transfe

40 olipid C9-methyltransferases (SmtA/SmtB) and glucosylceramide synthase (GcsA) to fungal phenotypes, s

41 n CD4(+) T cells using a potent inhibitor of glucosylceramide synthase (Genz-122346) led to a moderat

42 hibiting glycolipid biosynthesis by blocking glucosylceramide synthase has been proposed to reverse d

43 hance insulin signaling, but those targeting glucosylceramide synthase have no effect.

44 3) Overexpression of glucosylceramide synthase in myotubes induces glucosylce

45 In the Zucker diabetic fatty rat, the glucosylceramide synthase inhibitor (1R,2R)-nonanoic aci

46 e induction of T-cell apoptosis, because the glucosylceramide synthase inhibitor (PPPP) significantly

47 ceramide synthase inhibitor fumonisin B1 or glucosylceramide synthase inhibitor 1-phenyl-2-decanoyla

48 D4 and various chemokine receptors, with the glucosylceramide synthase inhibitor 1-phenyl-2-hexadecan

49 yristoylphosphatidylcholine liposome and the glucosylceramide synthase inhibitor D-PDMP induced cell

50 The glucosylceramide synthase inhibitor ethylenedioxyphenyl-

51 earlier studies utilized a first generation glucosylceramide synthase inhibitor to deplete cells of

52 ssion was reduced approximately 40% with the glucosylceramide synthase inhibitor, d-threo-1-phenyl-2-

53 Complications observed with another glucosylceramide synthase inhibitor, N-butyldeoxynojirim

54 lioside synthesis in SK-RC-45 cells with the glucosylceramide synthase inhibitor, PPPP, protected T c

55 lene, antagonists of Ryrs and by Genz-161, a glucosylceramide synthase inhibitor, suggesting substrat

56 ), proteases (trypsin and chymotrypsin), and glucosylceramide synthase inhibitors (dl-threo-1-phenyl-

57 A new series of glucosylceramide synthase inhibitors based on substituti

58 both multidrug-resistant cell lines with the glucosylceramide synthase inhibitors PDMP (d-threo-1-phe

59 rs C9DGJ and C4DGJ, which are more selective glucosylceramide synthase inhibitors than PDMP, failed t

60 Recently, more active and specific glucosylceramide synthase inhibitors, including d-threo-

61 ition, R28 retinal neurons were treated with glucosylceramide synthase inhibitors.

62 3-morpholino-1-propanol HCl, an inhibitor of glucosylceramide synthase, markedly abrogated gangliosid

63 irimycin derivatives on their merits as dual glucosylceramide synthase/neutral glucosylceramidase inh

64 xample, either ganglioside addition or human glucosylceramide synthase overexpression suppresses insu

65 iprocally modulated by chronic palmitate and glucosylceramide synthase overexpression.

66 Thus, overexpression of glucosylceramide synthase, previously shown to protect a

67 hreo-ethylenedioxyphenyl-P4, an inhibitor of glucosylceramide synthase, restored cholesterol in cultu

68 dentified sites of action: the inhibition of glucosylceramide synthase, resulting in the depletion of

69 A null mutation of the FgGCS1 gene encoding glucosylceramide synthase results in a mutant lacking gl

70 of knockout mice with a potent inhibitor of glucosylceramide synthase reversed accumulation of globo

71 Inhibitors of glucosylceramide synthase, sphingomyelin synthase, and c

72 In cell-free assays for glucosylceramide synthase, tamoxifen (1:10 molar ratio w

73 s are considerably more potent inhibitors of glucosylceramide synthase than their aliphatic counterpa

74 s led to the identification of inhibitors of glucosylceramide synthase, the enzyme catalyzing the fir

75 ted for 7 weeks with a specific inhibitor of glucosylceramide synthase, the initial enzyme involved i

76 We used a potent inhibitor of glucosylceramide synthase to test whether substrate depr

77 D-threo-3', 4'-Ethylenedioxy-P4-inhibited glucosylceramide synthase was comparably active to the p

78 the potency of these inhibitors in blocking glucosylceramide synthase was primarily dependent upon t

79 Sphingomyelin synthase, as well as glucosylceramide synthase, was inactivated by PDT in bot

80 pholino-1-propanol (D-PDMP) (an inhibitor of glucosylceramide synthase) were reduced by >90%.

81 ecanoylamino-3 -pyrrolidino-1-propanol-HC l (glucosylceramide synthase), which depletes cellular gang

82 Finally, stable overexpression of human glucosylceramide synthase, which attenuates ceramide lev

83 tat, a small iminosugar, reversibly inhibits glucosylceramide synthase, which catalyses the first com

84 ort that ceramide glycosylation catalyzed by glucosylceramide synthase, which is enhanced in breast c