ライフサイエンスコーパス: bivalent ligand

1 ain in which dimerization was regulated by a bivalent ligand.

2 s with five flexible arms each ending with a bivalent ligand.

3 roviding evidence of the discrete effects of bivalent ligands.

4 nding properties of nanometer-scale flexible bivalent ligands.

5 tween mu and delta opioid receptors by using bivalent ligands.

6 possibility, we have synthesized a series of bivalent ligands 1-5 that contain both mu agonist and CB

7 However, the analogous bivalent ligand 15 comprised of two (-)-trans-piperidine

8 In this series, the bivalent ligand 16, comprised of two (+)-trans-piperidin

9 In the dual receptor-bearing cells, bivalent ligands 3a-c capable of simultaneously binding

10 A functional switch is observed for the bivalent ligands 3b,c inhibiting cAMP formation in cells

11 Bivalent ligand 4 with spacer too short to occupy both r

12 is selectivity has led to the synthesis of a bivalent ligand (5) whose linker constrains the N17' bas

13 Finally, selected bivalent ligands (5d and 7b) were able to attenuate the

14 odel, which mimicked the interaction between bivalent ligands and their target molecules, to investig

15 ties compared to their parent compounds, the bivalent ligand approach led to significantly higher aff

16 The bivalent ligands are H(2)R partial or full agonists, up

17 The assembled bivalent ligands are significantly more potent inhibitor

18 sis for our continuing investigation of such bivalent ligands as probes of the opioid receptor oligom

19 The affinities of these bivalent ligands at CB1 and CB2 receptors were determine

20 Our investigation of bivalent ligands at mu, delta, and kappa opioid receptor

21 e unexpected observation that intermolecular bivalent ligand binding is enhanced for bivalent ligands

22 blocking required to prevent intermolecular bivalent ligand binding.

23 Bivalent ligands bridged in the 2-position were also syn

24 ide in complex with human FcRn shows how the bivalent ligand can bridge two FcRn molecules, which may

25 Receptor tethering with appropriate bivalent ligands can down-regulate signaling by moving a

26 to create nearly instantaneous high-affinity bivalent ligands capable of sequestering cellular target

27 A library of bivalent ligands composed of two identical CB1 antagonis

28 In addition to binding the bivalent ligands, concanavalin A discriminated between C

29 We report here bivalent ligands consisting of two identical oxytocin-mi

30 ive BRET signal, on exposure of the cells to bivalent ligands containing mu-opioid agonist and CCK2 r

31 All of these bivalent ligands effectively bind and cross-link anti-DN

32 Enforced dimerization of FKBP-BAX by the bivalent ligand FK1012 resulted in its translocation to

33 l synthesis and biological investigations of bivalent ligands for dopamine D2 receptor/neurotensin NT

34 exible linkers, we constructed aptamer-based bivalent ligands for human alpha-thrombin.

35 ptide-linked, spatially segregated mono- and bivalent ligands for the legume lectin concanavalin A.

36 ity of ErbB receptors to dimerize to signal, bivalent ligands, formed by the synthetic linkage of two

37 In acute i.c.v. studies, the bivalent ligands functioned as agonists with potencies r

38 The development of bivalent ligands has attracted interest as a way to pote

39 attempt to enhance this effect, we prepared bivalent ligands incorporating CCK(2) receptor antagonis

40 We also show that, for bivalent ligands, inhibitory capacity is correlated with

41 he first time that an appropriately designed bivalent ligand is capable of inducing association of G-

42 delta- and kappa-opioid receptor phenotypes, bivalent ligands (KDAN series) containing delta-antagoni

43 valuated (intrathecally in mice) a series of bivalent ligands (KDN series) containing kappa and delta

44 nditions defining the total concentration of bivalent ligand [L2]0, the total concentration of protei

45 lved in such cross-talk, we have synthesized bivalent ligands (MCC series) that contain mu opioid ago

46 e by the delta antagonist naltrindole (NTI), bivalent ligands [mu-delta agonist-antagonist (MDAN) ser

47 nce to examine the dissociation of a soluble bivalent ligand, N, N'-bis[[epsilon-[(2,4-dinitrophenyl)

48 laboratory established that the symmetrical bivalent ligand, N,N'-bis-[[epsilon-(2,4-dinitrophenyl)a

49 Bivalent ligands of G protein-coupled receptors have bee

50 t a new chemical genetic method for creating bivalent ligands of protein kinases.

51 ential formation of intra-IgE cross-links by bivalent ligands of sufficient length, (ii) self-associa

52 present in a complex of two proteins and one bivalent ligand (P x L2 x P) is maximized at [L2]0 = Kd/

53 comparison of the experimental data with the bivalent ligand properties predicted by a wormlike chain

54 The development of this bivalent ligand provides a tool for further probing the

55 ular bivalent ligand binding is enhanced for bivalent ligands relative to monovalent ligands allowed

56 The newly discovered oxytocin bivalent ligands represent a powerful tool for targeting

57 , this is the first report of a melanocortin bivalent ligand's in vivo physiological effects.

58 Moreover, the newly synthesized bivalent ligands show a strong, predominantly NTS1R-medi

59 The bivalent ligands show binding affinity in the picomolar

60 affinity compared to O-methyl glycoside, two bivalent ligands show significant enhancements in affini

61 Unexpectedly, different bivalent ligands showed preferences for particular melan

62 ons involving Fc epsilon RI, Lyn, Syk, and a bivalent ligand that aggregates Fc(epsilon)RI.

63 KDN21 is a bivalent ligand that contains delta and kappa opioid ant

64 keeping the site available for high-affinity bivalent ligands that can bind multiple sites in Nck.

65 d by the design and synthesis of a series of bivalent ligands that contain mu opioid agonist and mGlu

66 valent complexes with a stoichiometry of one bivalent ligand to one dimer.

67 ffold on the binding of these monovalent and bivalent ligands to anti-DNP IgE in solution.

68 The stoichiometry of binding of the bivalent ligands to both di- and tetrameric lectin was t

69 ent behavior follows from the binding of the bivalent ligands to dimeric receptors based on a TMH1-TM

70 study focused on the design and synthesis of bivalent ligands to target melanocortin receptor homodim

71 84, the prototype of our previously reported bivalent ligand TTR 'superstabiliser' family, is notably

72 Novel piperidine-based bivalent ligands were prepared in enantiomerically pure

73 and the anticlotting activities of thrombin bivalent ligands were significantly improved compared to

74 The 16 and 18 atom spacer bivalent ligands were the highlight compounds, displayin

75 cope of the method, the assembly of a set of bivalent ligands, which integrate members of the epiderm

76 nked with a long flexible linker to create a bivalent ligand with significantly improved binding affi

77 of cell surface receptors by a collection of bivalent ligands with different affinities for the recep

78 a nanometer-scale flexible linker to produce bivalent ligands with improved binding affinity and spec

79 This dimer binds the series of bivalent ligands with low picomolar avidities (K(d)(avid

80 To verify the practicality of bivalent ligands with nanometer-scale flexible linkers,

81 The resulting bivalent ligands with optimized spacer length and struct