ライフサイエンスコーパス: CYP24A1

1 CYP24A1 (hereafter referred to as CYP24) enzymatic activ

2 CYP24A1 expression is up-regulated by 1,25-dihydroxyvita

3 CYP24A1 may be a predictive marker of vitamin D3 clinica

4 CYP24A1 mRNA was elevated in malignant human prostate ti

5 CYP24A1 promoter DNA methylation was measured by means o

6 CYP24A1, the primary inactivating enzyme for vitamin D,

7 Variants at an additional locus (20q13, CYP24A1) were genome-wide significant in the pooled samp

8 bitor 5-aza-2'-deoxycytidine (DAC) activates CYP24A1 expression in prostate cancer cells.

9 ing affinity and inhibitory activity against CYP24A1 identified the imidazole styrylbenzamides as pot

10 p, CaR expression increased 27% (P=0.03) and CYP24A1 expression decreased 21% (P=0.79).

11 tudy the association between the CYP27B1 and CYP24A1 gene polymorphisms and type 1 diabetes.

12 lorectal carcinoma cells express CYP27B1 and CYP24A1 that locally regulate 1,25D with potential impli

13 D-binding protein gene (Gc) and CYP27B1 and CYP24A1, which code for enzymes that, respectively, synt

14 (VDR), and the P450 cytochromes, CYP27B1 and CYP24A1; however, they have yet to be investigated in hu

15 rectal neoplasms, and CaR, VDR, CYP27B1, and CYP24A1 as modifiable, preneoplastic risk biomarkers for

16 CaR, VDR, CYP27B1, and CYP24A1 expression and distribution in biopsies of norma

17 n D metabolism genes (GC, DHCR7, CYP2R1, and CYP24A1) with 25(OH)D in control subjects.

18 fferentiation between SLC34A1 (NaPi-IIa) and CYP24A1 (24-hydroxylase) defects appears critical for ta

19 Four SNPs (in FCER1A, IL13, and CYP24A1) and three SNPs (in IL4 and CYP24A1) were associ

20 L13, and CYP24A1) and three SNPs (in IL4 and CYP24A1) were associated with total IgE and specific IgE

21 ion), DBP (also known as GC; transport), and CYP24A1 (catabolism).

22 ckets, more work will need to be done before CYP24A1 inhibition can be integrated into the management

23 25(OH)2D3, on the other hand, increased both CYP24A1 and CYP27B1 protein expression in WT and VDR KO

24 1,25D is then deactivated by CYP24A1 and ultimately catabolized.

25 vitamin D [25(OH)D-24-hydroxylase encoded by CYP24A1] to neonatal 25(OH)D concentrations.

26 with 1,25(OH)2D3 increased levels of Cyp24a1/CYP24A1 and Cyp7a1/CYP7A1 mRNA in mouse and human hepato

27 hway genes (VDR, GC, DHCR7, CYP2R1, CYP27B1, CYP24A1, and CASR) modify the effects of vitamin D3 or c

28 xpression of vitamin D-24-hydroxylase (i.e., CYP24A1).

29 In addition, TBBz downregulates endogenous CYP24A1 mRNA level in TBBz-treated PC3 cells.

30 roduces 1,25(OH)2D3) and inactivating enzyme CYP24A1 (produces 24R,25(OH)2D3).

31 ed the effect of its major catabolic enzyme, CYP24A1, in prostate cancer.

32 s work supports an important role for excess CYP24A1 activity in the pathogenesis of FGF23-mediated h

33 ly more 1,25-dihydroxyvitamin D(3) and fewer CYP24A1 transcripts, encoding the 1,25-dihydroxyvitamin

34 For CYP24A1, all tested SNPs reduced enzyme activity.

35 ingle-nucleotide polymorphisms (SNP) or four CYP24A1 SNPs.

36 sed expression of the 1,25(OH)2D target gene CYP24A1 involved immunoprecipitation of hnRNPC1/C2 with

37 Especially VDR target genes CYP24A1, IGFBP-3, and TRPV6 were negatively regulated by

38 enografts of prostate cancer cells harboring CYP24A1 shRNA resulted in a drastic reduction in tumor v

39 High CYP24A1 protein levels were seen in poorly differentiate

40 Of note, high CYP24A1 expression significantly correlated with poor pa

41 duction and secretion of 25(OH)D3 and higher CYP24A1 gene transcript abundance in response to choleca

42 nic regions 50-69 kb downstream of the human CYP24A1 gene and 35-45 kb downstream of the mouse Cyp24a

43 co-expression with vitamin D 24-hydroxylase (CYP24A1) caused inactivation.

44 cription of the vitamin D(3) 24-hydroxylase (CYP24A1) gene.

45 enzyme 25-hydroxyvitamin D3-24-hydroxylase (CYP24A1) were described that lead to increased sensitivi

46 CYP2R1) with 3-epi-25(OH)D3; 24-hydroxylase (CYP24A1) with 25(OH)D3, 3-epi-25(OH)D3, and 1,25-dihydro

47 and symptomatic hypercalcemia, mutations in CYP24A1 were excluded.

48 tivation (CYP2R1, CYP27B1) and inactivation (CYP24A1, CYP3A4) and the newest physiological roles of v

49 ified several new UV target genes, including CYP24A1, GJA5, SLAMF7 and ETV1, which were frequently dy

50 In HCEC, 24,25(OH)2D3 increased CYP24A1 and CYP27B1 mRNA and protein expression, and sti

51 epithelial cells (KO), 1,25(OH)2D3 increased CYP24A1 and CYP27B1 protein expression.

52 lial cell line (HCEC), 1,25(OH)2D3 increased CYP24A1 mRNA and protein expression.

53 epithelial cells (WT), 1,25(OH)2D3 increased CYP24A1 protein expression and decreased CYP27B1 express

54 iated CK2 knockdown reduces 1,25D(3)-induced CYP24A1 mRNA expression in PC3 cells.

55 molecular library for compounds that inhibit CYP24A1 promoter activity.

56 ypothesize that an ovarian hormone inhibited CYP24A1 gene expression in the spinal cord, so the local

57 We show that TBBz inhibits CYP24A1 promoter activity induced by 1,25D(3) in prostat

58 Local CYP24A1 expression levels and the effect of selective mo

59 and potential VDREs located within mediated CYP24A1 induction, we constructed recombinant wild-type

60 YP3A4-dependent 4beta,25(OH)(2)D(3), but not CYP24A1-dependent 24R,25-dihydroxyvitamin D(3) formation

61 ith phenytoin) revealed a general absence of CYP24A1 mRNA.

62 Analysis of CYP24A1's proximal surface identifies the determinants o

63 se CK2 selective inhibitor as a disruptor of CYP24A1 promoter activity.

64 chostatin A (TSA) enhances the expression of CYP24A1 in prostate cancer cells.

65 Expression of CYP24A1 is up-regulated to attenuate vitamin D signaling

66 kdown of hnRNPC1/C2 suppressed expression of CYP24A1, but also increased expression of an exon 10-ski

67 roxyvitamin D(3) binding in the open form of CYP24A1 that clarifies the structural determinants of se

68 Inhibition of CYP24A1 enhances 1,25D(3) antitumor activity.

69 s demonstrate that deletion or inhibition of CYP24A1, which initiates degradation of the active form

70 ole styrylbenzamides as potent inhibitors of CYP24A1, having selectivity with respect to CYP27B1 comp

71 eatly facilitated by structural knowledge of CYP24A1.

72 dictive power of existing homology models of CYP24A1 is proposed.

73 kinase CK2 is involved in the regulation of CYP24A1 expression by 1,25D(3) and CK2 inhibitor enhance

74 To isolate regulators of CYP24A1 expression in prostate cancer cells, we establis

75 Our findings indicate that repression of CYP24A1 gene expression in human prostate cancer cells i

76 In this study, we investigated the role of CYP24A1 on malignant progression of a murine model of Br

77 on of vitamin D signaling via suppression of CYP24A1, a rate-limiting enzyme in the 1alpha,25-dihydro

78 reochemical preference compared with that of CYP24A1, a known 1,25(OH)(2)D(3) hydroxylase.

79 ic clearance of CYP3A4 was less than that of CYP24A1, comparison of metabolite profiles and experimen

80 ngest association with rs6127099 upstream of CYP24A1 (P=4.2 x 10(-53)), a gene that encodes the prima

81 The use of CYP24A1 RNAi enhanced the cytostatic effects of vitamin

82 Placental CYP24A1 methylation did not show an association with mat

83 Here, we report the crystal structure of rat CYP24A1 at 2.5 A resolution.

84 For those with up-regulated CYP24A1, combination therapy with RNAi targeting CYP24A1

85 o increased expression of an exon 10-skipped CYP24A1 splice variant; in a minigene model the latter w

86 ex mechanism is responsible for the striking CYP24A1 up-regulation induced by the vitamin D hormone i

87 4A1, combination therapy with RNAi targeting CYP24A1 could be considered to improve clinical responsi

88 We found that CYP24A1 expression is inversely correlated with promoter

89 paired human prostate samples revealed that CYP24A1 expression is downregulated in prostate malignan

90 Bisulfite pyrosequencing shows that CYP24A1 gene is hypermethylated in malignant lesions com

91 e absence of vitamin D(3), PXR activates the CYP24A1 gene by directly binding to and transactivating

92 Vitamin D(3) activates the CYP24A1 promoter by dissociating the corepressor silenci

93 and simultaneously decreases H3K9me2 at the CYP24A1 promoter.

94 24-Hydroxylase, encoded by the CYP24A1 gene, is the key enzyme for degrading many forms

95 inactivated by 24-hydroxylase encoded by the CYP24A1 gene.

96 For the CYP24A1 gene, we found no evidence of association with t

97 und to prevent dissociation of SMRT from the CYP24A1 promoter.

98 D(3)-dependent dissociation of SMRT from the CYP24A1 promoter.

99 Docking experiments on the inhibitors in the CYP24A1 enzyme active site suggest the compounds reach t

100 (rs4646536) and 16 tag polymorphisms in the CYP24A1 gene.

101 r was attenuated by a functional VDRE in the CYP24A1 promoter.

102 gly represses vitamin D(3) activation of the CYP24A1 gene, in which PXR indirectly binds to and preve

103 roperties, is degraded by the product of the CYP24A1 gene, which is downregulated in human prostate c

104 The placental methylation of the CYP24A1 promoter appears subject to a genetic influence,

105 In vitro methylation of the CYP24A1 promoter represses its promoter activity.

106 Overall, the CYP24A1 structure provides the first template for unders

107 teractions with vitamin D(3) to regulate the CYP24A1 gene.

108 the recruitment of vitamin D receptor to the CYP24A1 promoter.

109 istone modifications are associated with the CYP24A1 promoter region.

110 putative downstream elements contributed to CYP24A1 up-regulation by 1,25(OH)(2)D(3).

111 ctivity, regulate VDR downstream genes (VDR, CYP24A1, TRPV6 and CYP27B1), and inhibit the production

112 Sequencing analysis of the VDR, CYP24A1, CYP27B1 and CYP2R1 detected twelve nucleotide c

113 However, it is unclear whether CYP24A1 expression serves as a functional contributor ve

114 olved immunoprecipitation of hnRNPC1/C2 with CYP24A1 chromatin and RNA.

115 a stable prostate cancer cell line PC3 with CYP24A1 promoter driving luciferase expression to screen