ライフサイエンスコーパス: radicicol

1 open chain amide chimera of geldanamycin and radicicol.

2 alogues showed binding properties similar to radicicol.

3 lowing HSP90 inhibition with geldanamycin or radicicol.

4 to hsp90 is inhibited by the hsp90 inhibitor radicicol.

5 th over 75% inhibition achieved at 20 microm radicicol.

6 ame conformational change as does binding of radicicol.

7 that was inhibited by both geldanamycin and radicicol.

8 te for the Hsp90 inhibitors geldanamycin and radicicol.

9 was efficiently blocked by geldanamycin and radicicol.

10 sualize cellular proteins that interact with radicicol.

11 the results of a synthetic program targeting radicicol (1) and monocillin I (2), highlighted by the a

12 Radicicol (1) exhibits potent anticancer properties in v

13 nd the transformation-suppressing effects of radicicol, a biotinylated derivative of radicicol was ch

14 Recently, it was found that radicicol, a drug known to block Hsp90 function, also in

15 Peptide binding is inhibited by radicicol, a known inhibitor of the chaperone activities

16 Radicicol, a macrocyclic anti-fungal antibiotic, has the

17 medium, and this activation is inhibited by radicicol, a specific inhibitor of hsp90.

18 ed less efficiently, and the Hsp90 inhibitor radicicol abolished curing, implying that Sti1 acts in c

19 The antibiotics geldanamycin and radicicol act as highly selective inhibitors of in vivo

20 Geldanamycin, ADP, ATP, and radicicol-all known to bind to the ATP domain of Hsp90-c

21 17-AAG and radicicol also induced splicing of XBP1, with the induct

22 ng crystallographic approaches, we show that radicicol (an Hsp90 inhibitor) binds and interacts speci

23 of GRP94 function was efficiently blocked by radicicol, an established inhibitory ligand for the aden

24 ion of the K632A/K633A mutant are blocked by radicicol, an Hsp90 inhibitor.

25 Radicicol, an inhibitor of Hsp90 ATPase activity, revers

26 finity of the chaperone for geldanamycin and radicicol and causing in vitro and in vivo depletion of

27 A series of macrocylic chimeras of radicicol and geldanamycin and the corresponding seco-ag

28 Radicicol and geldanamycin could both maintain chaperone

29 superimposition of these ligands, hybrids of radicicol and geldanamycin have been designed.

30 have demonstrated that the natural products, radicicol and geldanamycin, are potent inhibitors of the

31 Using the hsp90-specific inhibitors radicicol and geldanamycin, we show that hsp90 is requir

32 ab3a off membranes, and by Hsp90 inhibitors, radicicol and geldanamycin, which are known to inhibit R

33 verexpression of p23 buffered the effects of radicicol and herbimycin A, but not novobiocin, on AhR s

34 concentrations of the N-terminal inhibitors radicicol and herbimycin A.

35 The interaction between radicicol and PhoQcat demonstrates significant similarit

36 erone Cdc37 and two Hsp90 ATPase inhibitors: Radicicol and the first-generation anticancer drug DMAG.

37 prostate cancer cells, both pharmacological (radicicol) and genetic (small interfering RNA) approache

38 in complex with N-ethylcarboxamidoadenosine, radicicol, and 2-chlorodideoxyadenosine reveals a struct

39 of the three Hsp90 inhibitors geldanamycin, radicicol, and herbimycin A resulted in a dose-dependent

40 llylamino-17-demethoxygeldanamycin (17-AAG), radicicol, and PU-H71.

41 Geldanamycin and radicicol are structurally different macrocycles determi

42 the basis of structural homology, we tested radicicol as a potential inhibitor of Sln1 and branched-

43 mily proteins and various drugs, and reveals radicicol as a versatile scaffold for targeting distantl

44 In contrast, GRP94 bound radicicol at a stoichiometry of 2 mol of radicicol/mol o

45 Geldanamycin and radicicol, ATP-competitive inhibitors of the chaperone H

46 n our laboratory envisions natural macrolide radicicol-based inhibitors targeting the molecular chape

47 activities, with the potent Hsp90 inhibitor radicicol being an important representative member.

48 The anti-tumor agents geldanamycin and radicicol bind specifically at this site and induce dest

49 he peptide-binding site is distinct from the radicicol-binding pocket, because both can bind to the N

50 te face of the beta sheet from the pan-HSP90 radicicol-binding pocket, in close proximity to a deep h

51 The peptide and radicicol-binding sites are distinct, as shown by the ab

52 oximately 10-12%) between topo VI and Hsp90, radicicol binds to the ATPase sites of these two enzymes

53 resorcylic acid lactone intermediate of the radicicol biosynthetic pathway, (R)-monocillin II.

54 (MAP) kinase family, while geldanamycin and radicicol blocked the phosphorylation of ERK1 and -2 in

55 ydrolyzable ATP analog) bound to PhoQcat and radicicol bound to Hsp90.

56 red with the N-ethylcarboxamidoadenosine and radicicol-bound forms, these structures reveal a large c

57 by the inhibition of binding of biotinylated radicicol by the native drug.

58 and disparate binding affinities for the Gdm-radicicol chimera radamide when bound to the two paralog

59 ne kinases prompted our inquiry into whether radicicol could be a potential inhibitor of histidine ki

60 tment of human B cells with geldanamycin and radicicol did not alter cellular MHC class II expression

61 resulted in a highly convergent synthesis of radicicol dimethyl ether but failed in the removal of th

62 rminal ATP/ADP-binding domain of Hsp90, with radicicol displaying nanomolar affinity, and both inhibi

63 this useful property, the mechanism by which radicicol exerts its anti-transformation effects is curr

64 ynamic and requires higher concentrations of radicicol for its inhibition, whereas GR steroid binding

65 The known HSP90 inhibitors geldanamycin and radicicol gave IC(50) values of 4.8 and 0.9 microM respe

66 ost prominent cellular protein that bound to radicicol had a molecular weight of approximately 90 kDa

67 Geldanamycin and radicicol had nanomolar potency in vitro against bloodst

68 NOS, whereas the non-quinone hsp90 inhibitor radicicol had no effect.

69 17-allylamino-17-demethoxygeldanamycin, and radicicol have been described.

70 minal domain complexes with geldanamycin and radicicol identify key aspects of their nucleotide mimic

71 the bioactive conformers of geldanamycin and radicicol in CDCl3 solution with populations of 4% and 2

72 g IPKS, are required for the biosynthesis of radicicol in Pochonia chlamydosporia.

73 analogue and an alternative HSP90 inhibitor radicicol indicated that increased expression of HSP72,

74 tion of HSP90 function using geldanamycin or radicicol inhibited MHC class II presentation of exogeno

75 We further demonstrate that radicicol inhibits both the dimerization of the topo VI

76 In contrast, the HSP90 inhibitor radicicol, lacking a bezoquinone moiety, has no measurab

77 products (e.g., 17-allylaminogeldanamycin or radicicol) leads to the ubiquitination of oncogenic clie

78 f protein-protein interaction; ATP, ADP, and radicicol markedly suppress this conformational change.

79 gest that the anti-transformation effects of radicicol may be mediated, at least in part, by the asso

80 und radicicol at a stoichiometry of 2 mol of radicicol/mol of GRP94 dimer.

81 The antifungal antibiotic radicicol (Monorden) has been shown to bind to the Berge

82 is markedly decreased by geldanamycin and by radicicol (monorden).

83 namycin and the resorcylic acid macrolactone radicicol not only in driving forward drug discovery pro

84 The hsp90 inhibitor radicicol or coexpression of an ATPase-defective hsp90 b

85 have discovered that inhibition of hsp90 by radicicol or geldanamycin nearly prevents the heme-media

86 the Hsp90-specific inhibitor geldanamycin or radicicol potently suppressed the production of infectio

87 We also examined the effect of Radicicol (RA), a drug with higher affinity than GA for

88 thoxygeldanamycin (17-AAG, 210+/-50 nM), and radicicol (RAD, 20+/-9 nM) were consistent with previous

89 The natural products geldanamycin (GM) and radicicol (RD) are known inhibitors of Hsp90, and their

90 s are distinct, as shown by the ability of a radicicol-refractive mutant to bind peptide.

91 y expressing CYP2E1 with the hsp90 inhibitor radicicol results in CYP2E1 degradation that is inhibite

92 the structurally unrelated HSP90 inhibitors, radicicol, the purine BIIB021, and the resorcinylic pyra

93 as confirmed by demonstrating the ability of radicicol to specifically bind purified human HSP90.

94 ty of the immunopurified GR are inhibited by radicicol treatment of Sf9 cells prior to cytosol prepar

95 Both geldanamycin and radicicol, two structurally different Hsp90 inhibitors,

96 s of radicicol, a biotinylated derivative of radicicol was chemically synthesized and used as a probe

97 ecific inhibitors of Hsp90, geldanamycin and radicicol, we found that functional Hsp90 is essential f

98 ted, at least in part, by the association of radicicol with HSP90 and the consequent dissociation of