ライフサイエンスコーパス: ansamycin

1 synthesis of a triene-containing C17-benzene ansamycin.

2 of structural derivatives (6-9) of phenolic ansamycins.

3 e the preparation of potent non-benzoquinone ansamycins.

4 compared with the corresponding benzoquinone ansamycins.

5 synthetic precursor of rifamycin and related ansamycins, a series of target-directed mutations and he

6 have suggested that the in vitro potency of ansamycins against Hsp90 may be enhanced in the presence

7 hydroxybenzoic acid (AHBA), precursor of the ansamycin and mitomycin antibiotics, proceeds by the ami

8 ibition of Akt activation is achievable with ansamycins and may be useful for the treatment of HER2 d

9 e quinone chromophores of the naphthoquinone ansamycins and related natural products.

10 cins are metabolized by NQO1 to hydroquinone ansamycins and that Hsp90-mediated trans-cis isomerizati

11 s- and cis-amide isomers of the benzoquinone ansamycins and their mechanism of Hsp90 inhibition.

12 The ansamycin antibiotic geldanamycin (GA) induces the intra

13 sent studies demonstrate that treatment with ansamycin antibiotic geldanamycin (GA), or its less toxi

14 The ansamycin antibiotic geldanamycin has frequently been us

15 ibited hypersensitivity to the Hsp90-binding ansamycin antibiotic geldanamycin.

16 ino)-17-demethoxygeldanamycin (17-AAG) is an ansamycin antibiotic that binds to a conserved pocket in

17 Geldanamycin (GA) is a benzoquinone ansamycin antibiotic that disrupts Hsp90-protein interac

18 eatment of MCF-7 cells with geldanamycin, an ansamycin antibiotic that inhibits Hsp90 function, MLK3

19 methoxygeldanamycin (17-AAG), a benzoquinoid ansamycin antibiotic, which binds to heat shock protein

20 h two additional AHBA synthases from related ansamycin antibiotic-producing microorganisms.

21 maturation of Hsp90 target proteins and that ansamycin antibiotics abrogate the activity of such prot

22 The recent discovery that a class of ansamycin antibiotics bind specifically to Hsp90 allowed

23 -dependent processes to ansamycin treatment, ansamycin antibiotics disrupt signaling through some mec

24 complexes in cell lysates, and Hsp90-binding ansamycin antibiotics disrupt the activity of Hsp90-depe

25 In this study, I demonstrate that ansamycin antibiotics disrupt the function of Hsp90 targ

26 Targeting HSP90 with ansamycin antibiotics disrupts the normal processing of

27 Ansamycin antibiotics inhibit function of the heat shock

28 ological intercession of Hsp90 activity with ansamycin antibiotics or depletion of BAG3 by small inte

29 Hsp90 inhibitory ansamycin antibiotics such as geldanamycin (GA) induce r

30 amino)-17-demethoxygeldanamycin (17-AAG) are ansamycin antibiotics that bind to a highly conserved po

31 cking Sba1 displays increased sensitivity to ansamycin antibiotics, and this phenotype is rescued by

32 The polyketide chains of the two ansamycin antibiotics, ansatrienin (mycotrienin) and nap

33 E (1), member of a novel class of cytotoxic ansamycin antibiotics, has been achieved.

34 The ansamycin antibiotics, herbimycin A (HA) and geldanamyci

35 The biosynthesis of ansamycin antibiotics, like rifamycin B, involves format

36 Ansamycin antibiotics, such as 17-allylaminogeldanamycin

37 Ansamycin antibiotics, such as geldanamycin, potently in

38 tiosum, the producer of the highly cytotoxic ansamycin antibiotics, the ansamitocins.

39 that some of the effects of 17-AAG and other ansamycins are due to their effects on VDAC and that thi

40 rather than cis-amide forms of benzoquinone ansamycins are metabolized by NQO1 to hydroquinone ansam

41 These benzoquinone ansamycins are potent inhibitors of Hsp90 function, whic

42 uch attention is focused on the benzoquinone ansamycins as anticancer agents, with several derivative

43 Benzoquinonoid ansamycins (BAs) have recently been shown to specificall

44 Geldanamycin is an ansamycin benzoquinone, and we show here that it causes

45 Cross-resistance was found with other ansamycin benzoquinones but not with the structurally un

46 sent evidence that the approximately 100-kDa ansamycin-binding protein is GRP94.

47 DDP-induced signaling pathways revealed that ansamycins block the activation of mitogen-activated pro

48 neurodegenerative diseases, and benzoquinone ansamycin (BQA) Hsp90 inhibitors such as geldanamycin (G

49 The benzoquinone ansamycins (BQAs) are a valuable class of antitumor agen

50 the reduction of this series of benzoquinone ansamycins by NQO1 generates the corresponding hydroquin

51 The reduction of these benzoquinone ansamycins by recombinant human NQO1 to the correspondin

52 Ansamycins cause RB-dependent G1 arrest that is associat

53 Ansamycins caused rapid degradation of HER2 and a concom

54 bition after treatment with the benzoquinone ansamycins compared with the MDA468 cells; this increase

55 We found that while the ansamycin compounds have the commonly observed negative

56 investigation of binding of nucleotides and ansamycin compounds to this domain.

57 ot the cis-amide isomers of the benzoquinone ansamycins could be accommodated by the NQO1 active site

58 spite structural studies on the complexes of ansamycin derivatives with the ATPase domain of Hsp90, c

59 Thus, benzoquinone ansamycin drugs and their derivatives, such as 17-allyl-

60 s- and cis-amide isomers of the hydroquinone ansamycins exhibited increased binding affinity for Hsp9

61 The increased duration of benzoquinone ansamycin exposure showed increased potency and -fold in

62 cer cells and is inhibited by members of the ansamycin family of antibiotics.

63 The ansamycin family of natural products and their derivativ

64 The benzoquinone ansamycin geldanamycin (GA) binds to HSP90 and disrupts

65 One of them, the benzoquinone ansamycin geldanamycin (GA) Mr-90,000 heat-shock protein

66 Therefore, we hypothesized that the ansamycin geldanamycin and its 17-allylamino-17-demethox

67 The benzoquinone ansamycin geldanamycin and its derivatives are inhibitor

68 bes the influential role of the benzoquinone ansamycin geldanamycin and the resorcylic acid macrolact

69 Cotreatment with the benzoquinone ansamycin Geldanamycin depleted Raf-1 but did not decrea

70 r PC-3 and LNCaP cells with the benzoquinone ansamycin geldanamycin, an Hsp90-specific inhibitor, ind

71 The benzoquinoid ansamycins geldanamycin (GA), herbimycin, and their deri

72 t extracts was inhibited by the benzoquinoid ansamycins geldanamycin and macbecin.

73 ADP and the benzoquinone ansamycin, geldanamycin, are potent inhibitors of comple

74 eatment of tumor cells with the benzoquinone ansamycin, geldanamycin, leading to a marked reduction i

75 breast carcinoma cells with the benzoquinoid ansamycin, geldanamycin, rapidly depletes p185c-erbB-2 p

76 The ansamycins, geldanamycin (GA) and its derivative, 17-all

77 0 ATPase activity including the benzoquinone ansamycins, geldanamycin and 17-allylamino-17-demethoxyg

78 trans-cis isomerization of the benzoquinone ansamycins in Hsp90 inhibition has been disputed in rece

79 mulation of the high-affinity dihydroquinone ansamycins in tumor cells contributes to the antitumor a

80 tive effects of geldanamycin, a benzoquinone ansamycin, in HT22 cells were associated with a down-reg

81 This mechanism also explains the ansamycin-induced proteolysis of several protooncogenic

82 The ansamycins inhibit refolding, both in vivo and in a cell

83 The benzoquinone ansamycins inhibit the ATPase activity of the 90-kDa hea

84 The ansamycins inhibited DDP-induced activation of caspases

85 Ansamycin inhibition of chaperone-dependent activity inc

86 s- and cis-amide isomers of the benzoquinone ansamycins into the open Hsp90 structure.

87 Ansamycin natural products and selected structural analo

88 Four cyclopentenone-containing ansamycin polyketides (mccrearamycins A-D), and six new

89 Ansamycins reduced to their dihydroquinones in the prese

90 ating increased efficacy of the hydroquinone ansamycin relative to its parent quinone.

91 ks chemical and structural similarity to the ansamycin rifampicin (Rif), an RNAP inhibitor widely use

92 tions with the C-12 methoxy group of the GdA ansamycin ring.

93 7-allylamino portion of 17AAG and not on its ansamycin ring.

94 The ansamycins shift the mode of Hsp90 from refolding to deg

95 Ansamycins such as rifamycin, ansamitocin, and geldanamy

96 Treatment of SKBr3 cells with benzoquinone ansamycins, such as geldanamycin (GA), depletes p185erbB

97 Geldanamycin, a benzoquinone ansamycin that binds to animal hsp90s and prevents their

98 Sf9 cells with geldanamycin, a benzoquinone ansamycin that binds to hsp90 and disrupts its function,

99 of L cells with geldanamycin, a benzoquinone ansamycin that binds to hsp90 and disrupts its function,

100 Geldanamycin (GD) is a benzoquinone ansamycin that inhibits the function of Hsp90.

101 when this function is interfered with by an ansamycin, there is a further shift to proteolytic degra

102 sensitivity of Hsp90-dependent processes to ansamycin treatment, ansamycin antibiotics disrupt signa

103 The triene-containing C17-benzene ansamycins trienomycins A and F were prepared in 16 step

104 g a fundamentally new route to shikimate and ansamycin-type compounds, this result enables further ge

105 fied human Hsp90 by a series of benzoquinone ansamycins was examined in the presence and absence of N

106 human NQO1 to the corresponding hydroquinone ansamycins was monitored by high-performance liquid chro

107 , and HPLC analysis showed that hydroquinone ansamycins were formed by the MDA468/NQ16 cells, which c

108 bitor of NQO1, showing that the hydroquinone ansamycins were more potent Hsp90 inhibitors than their

109 C inhibitor, or geldanamycin, a benzoquinone ansamycin, which destabilizes and depletes Raf-1, marked

110 QO1 generates the corresponding hydroquinone ansamycins, which exhibit enhanced Hsp90 inhibition.

111 xtensive study with a series of benzoquinone ansamycins, which includes gel-danamycin, 17-(amino)-17-

112 cts between yeast Hsp90 and the hydroquinone ansamycins, which translated to greater interaction ener

113 teraction of rifabutin (RFB), a naphthalenic ansamycin, with membrane models.