ライフサイエンスコーパス: echistatin

1 ed with microbubbles bearing the disintegrin echistatin.

2 ds smaller conformational perturbations than echistatin.

3 ceptor-binding assay in the presence of 125I-echistatin.

4 ure-targeting ligands, cyclic RGD (cRGD) and echistatin.

5 d to alpha(v)beta3 by surface conjugation of echistatin.

6 ,Leu(28)]-, [Bpa(23),Leu(28)]-, and [Bpa(28)]echistatin.

7 at encompasses the contact site for [Bpa(28)]echistatin.

8 -aspartic acid sequences and the disintegrin echistatin.

9 group in position 45, near the C-terminus of echistatin.

10 alphaIIbbeta3, 3 kcal/mol lower than that of echistatin.

11 nd an auxiliary epitope at the C-terminus of echistatin.

12 resting) integrin binding to the disintegrin echistatin.

13 ompletely abolished by echicetin, but not by echistatin.

14 ggregins A and B, echicetin, botrocetin, and echistatin.

15 The ability of echistatin 1-41 to compete with binding of vitronectin t

16 istatin and its three analogues (R24A, D27W, echistatin 1-41).

17 antial increase in phosphorylated IRS-1, and echistatin (10(-7) M) blocked the IGF-I-induced IRS-1 ph

18 Echistatin (10(-7) M) inhibited IGF-I-stimulated DNA syn

19 Echistatin (10(-7) M) significantly reduced IGF-I-stimul

20 Echistatin (50-100 nM) competitively antagonizes and aba

21 the synthesis of a photoreactive analogue of echistatin (a 49-amino acid peptide), a potent RGD-conta

22 h affinity (K(D) = 60 fM) binding of [(125)I]echistatin (a competitive integrin receptor antagonist)

23 integrin-dependent mechanisms, the effect of echistatin (a disintegrin) on proliferation in response

24 We have employed echistatin, a 5.4 kDa snake venom disintegrin, as a mode

25 th specific integrin-blocking antibodies and echistatin, a disintegrin peptide.

26 sidues of the RGD loops and the C termini of echistatin, a potent antagonist of alpha(IIb)beta(3), al

27 Echistatin also attenuated downstream signaling because

28 (2) Both echicetin and echistatin, an alphavbeta3 antagonist, inhibited the adh

29 ind efficiently, tightly, and selectively to echistatin, an RGD disintegrin.

30 In this study, we have used echistatin, an RGD-containing short monomeric disintegri

31 beta(3)[209-220] as the contact site for an echistatin analogue with a photoreactive group in positi

32 While echistatin analogues containing Bpa in either position 2

33 orms exhibited high affinity binding to 125I-echistatin and cyclic and linear RGD peptides.

34 ttern of cysteines to the short disintegrins echistatin and eristostatin but contains the sequence KT

35 d the inhibitory effect of the disintegrins, echistatin and eristostatin, and the alphaIIbbeta3 antag

36 hibition of integrin and Cox-2 activation by echistatin and indomethacin, respectively, each blocked

37 We investigated the activities of echistatin and its three analogues (R24A, D27W, echistat

38 further increase of the binding affinity of echistatin and of the inhibitory effect.

39 In vitro experiments showed that the echistatin and RGD peptide were released from ELVAX in a

40 ELVAX loaded with either RGD peptide or echistatin and surgically implanted next to the maxillar

41 t smooth muscle cells (SMCs) were exposed to echistatin and their ability to respond to IGF-I was det

42 Using disintegrins, echistatin, and VLO4, peptide inhibitors to alphavbeta3

43 Competitive cell binding assay, using (125)I-echistatin as the radioligand, and live cell staining we

44 is the dominant factor stabilizing integrin:echistatin binding, while transition-state thermodynamic

45 6 were determined by displacement of (125)I-echistatin bound to U87MG glioma cells.

46 analogues of the 49-amino acid disintegrin, echistatin: [Bpa(21),Leu(28)]-, [Bpa(23),Leu(28)]-, and

47 nt and was blocked by RGDS, HHLGGAKQAGDV, or echistatin, but not by RGES.

48 Echistatin, but not echicetin, inhibited the adhesion to

49 [Bpa(23),Leu(28)]echistatin cross-links 10-30 times more effectively than

50 subunit of alpha(V)beta(3), [Bpa(21),Leu(28)]echistatin cross-links to both the alpha(V) and the beta

51 located within an auxiliary binding site in echistatin, cross-links to a site distinct from the two

52 Deletion of nine C-terminal amino acids of echistatin decreased its ability to bind alphaIIb beta3

53 lphav and alpha1 integrins or treatment with echistatin did not cause cell death.

54 R24A echistatin did not react with alphaIIb beta3 and alpha(v

55 ould tolerate insertion of the 49-amino acid echistatin domain.

56 )beta(1) integrins, we expressed recombinant echistatin, eristostatin, and 15 hybrid molecules.

57 Eight disintegrins (bitistatin, albolabrin, echistatin, eristostatin, kistrin, mambin, halysin and b

58 Truncated echistatin failed to induce LIBS epitopes on cells trans

59 creasing concentrations of either kistrin or echistatin inhibited IGF-I-induced migration, whereas de

60 Echicetin, but not echistatin, inhibited the adhesion of cells transfected

61 ypothesis is proposed that the C terminus of echistatin interacts with separate sites on beta(1) and

62 Echistatin is a disintegrin that blocks alphavbeta3.

63 Echistatin is a viper venom disintegrin containing RGD l

64 mentation equilibrium demonstrated that both echistatin ligands induced substantial alphaIIbbeta3 dim

65 Taken together, position 45 in echistatin, located within an auxiliary binding site in

66 which was higher than platelets, fibrinogen, echistatin, mambin or halysin (p < 0.05).

67 We propose that echistatin may serve as a paradigm for understanding mul

68 ha(v)-integrins were prepared by conjugating echistatin (MB(E)) or monoclonal antibody against murine

69 In order to identify echistatin motifs required for selective recognition of

70 ntration-dependent effect of the disintegrin echistatin on cell adhesion.

71 MV-ERV correctly displayed echistatin on the outer surface of its envelope and prod

72 could be blocked by local administration of echistatin or an arginine-glycine-aspartic acid (RGD) pe

73 Application of echistatin or beta(1) integrin function blocking antibod

74 poration is virtually abolished by 50-100 nM echistatin or by 5-10 nM rapamycin, a blocker of the mam

75 nd pit resorption in vitro and is reduced by echistatin or calcitonin and cytochalasin D.

76 nstrated that both full length and truncated echistatin perturbed alphaIIbbeta3's solution structure,

77 (125)I-[Arg(35),Lys(45)(N(epsilon)-pBz(2))]-echistatin photo-cross-links effectively to a site withi

78 tween micellar alphaIIbbeta3 and recombinant echistatin (rEch) mutants, immobilized on the surface of

79 Echistatin reduced basal proliferation by approximately

80 Finally, treatment of HCFs with echistatin reduced virus-induced expression of the neutr

81 he placement of the benzophenone in [Bpa(28)]echistatin relative to the RGD triad.

82 integrin alpha(V), as blockage by antagonist echistatin (RGD peptide) or alpha(V)-specific siRNA resu

83 nt of Met(28) with Leu selectively decreased echistatin's ability to recognize alpha(5)beta(1) only.

84 ent of Met(28) with Asn completely abolished echistatin's ability to recognize each of the integrins,

85 We propose a hypothesis in which echistatin's RGD loop determines selective recognition o

86 D27W echistatin showed increased binding to alphaIIb beta3 an

87 , a focal adhesion associated protein, while echistatin significantly decreased phosphorylation level

88 maintained on laminin/type IV collagen, and echistatin significantly inhibited the DNA synthesis res

89 The related disintegrin echistatin specifically inhibited 125I-labeled kistrin b

90 We displayed a disintegrin, M28L echistatin that binds with a high affinity to integrin a

91 hesis that the very high binding affinity of echistatin to alpha(V)beta(3) results from two distinct

92 pounds, SCH 221153, inhibited the binding of echistatin to alpha(v)beta3 (IC50 = 3.2 nM) and alpha(v)

93 assays, SCH 221153 inhibited the binding of echistatin to alpha(v)beta3- and alpha(v)beta5-expressin

94 This substitution impaired the ability of echistatin to induce LIBS in alpha(v) beta3 integrin.

95 The addition of an RGD peptide and echistatin to pSMC cultures that had been plated on fibr

96 Application of echistatin to Xenopus retinal-derived XR1 glial cells in

97 fied human alphaIIbbeta3 and two recombinant echistatin variants: rEch (1-49) M28L, chosen for its se

98 e new targeted virus was named measles virus echistatin vector (MV-ERV).

99 In vitro studies demonstrated that the VSV-echistatin viruses specifically bound to targeted integr

100 ning peptides and by the snake venom protein echistatin, whereas an RGE-containing peptide and four n

101 Parallel experiments included echistatin, which is a snake venom disintegrin and a par