ライフサイエンスコーパス: tethered ligand

1 re for a PAR2 antagonist competing against a tethered ligand.

2 tivation of a chemokine receptor by a pseudo-tethered ligand.

3 s at a conserved target arginine to reveal a tethered ligand.

4 by proteolysis of the N terminus to reveal a tethered ligand.

5 red testisin specifically releases the PAR-2 tethered ligand.

6 MrgprC11 did not involve the generation of a tethered ligand.

7 proteolytic cleavage and the unmasking of a tethered ligand.

8 ytic cleavage, PAR(2) is activated through a tethered ligand.

9 by proteolytic cleavage and generation of a tethered ligand.

10 or 2 (PAR-2), via cleavage and exposure of a tethered ligand.

11 y cleavage of the amino terminus to unmask a tethered ligand.

12 tivated by proteolytic exposure of an occult tethered ligand.

13 ond both to exogenous SFLLRN and to a second tethered ligand.

14 placement of diffusible Netrin-B by membrane-tethered ligands.

15 ated by proteolytic shedding of its membrane-tethered ligands.

16 functionalized Au surfaces with three thiol-tethered ligands: 2-mercaptopropionic acid, 4-pyridinyle

17 These experiments suggest that tethered ligand activity is conferred in large part by t

18 SFLLRN-NH2, a thrombin receptor-tethered ligand analogue, and [3H]haTRAP exhibited compe

19 force-distance interaction between a polymer-tethered ligand and its receptor.

20 ward arrowT(57), which removed the canonical tethered ligand and prevented trypsin activation.

21 tially involved in interaction with both the tethered ligand and the soluble peptide agonist.

22 ins whose activity is controlled by flexibly tethered ligands and receptors.

23 the hexapeptide SFFLRN (that functions as a tethered ligand) and was blocked by the thrombin inhibit

24 the hexapeptide SF-FLRN (that functions as a tethered ligand) and was inhibited by hirudin.

25 Membrane-tethered ligands are recombinant proteins comprised of a

26 pecific labeling is achieved by presenting a tethered ligand at the synapses of genetically defined n

27 However, targeting PAR1 with an orthosteric-tethered ligand binding-site antagonist results in bleed

28 lithium compounds have been prepared with a tethered ligand, (CH(3)OCH(2)CH(2))(2)NCH(2)C(CH(3))(2)-

29 More generally, tethered ligands competing with those free in solution a

30 ived agonist peptide (TRAP, a portion of the tethered ligand created by thrombin's proteolytic activi

31 a new amino terminus which then serves as a tethered ligand, docking intramolecularly to the body of

32 fication of the docking interactions between tethered ligand domain and receptor is critical for unde

33 Since peptides mimicking the PAR1 tethered ligand domain can also activate PAR2, we asked

34 of PAR1 antagonists, which compete with the tethered ligand domain rather than preventing PAR1 cleav

35 The tethered ligand domain shows a considerable degree of di

36 Cleavage exposes a tethered ligand domain that binds to and activates the c

37 for thrombin, which is also activated by the tethered-ligand domain sequence (SFLLRN) and which promo

38 ast cells, and peptides corresponding to the tethered ligand domains of PAR-1 and PAR-2 increased [Ca

39 Synthetic "agonist peptides" that mimic the tethered ligand domains of thrombin receptor and PAR2 ac

40 ases cleave PARs at specific sites to expose tethered ligand domains that bind to and activate the cl

41 The novel PAR1-tethered ligand exposed by MMP-2 stimulates PAR1-depende

42 eptor-1 (PAR-1) can be activated by both the tethered ligand exposed by thrombin cleavage and a synth

43 nerating a new amino terminus that acts as a tethered ligand for the receptor.

44 tide (GYPGQV) representing the newly exposed tethered ligand from the amino terminus of PAR4 after pr

45 The protease-activated receptors are tethered ligand G protein-coupled receptors that are act

46 ity behavior would be expected for a matrix-"tethered" ligand; i.e., a ligand which acts from the mat

47 rin receptors dissociate streptavidin-biotin tethered ligands in focal adhesions within 60 min of cel

48 A membrane-tethered ligand-independent Notch1 construct also showed

49 equilibrium system the compound with the exo-tethered ligand inverts faster than its endo analog.

50 protease-activated receptor-1 (PAR-1) whose tethered ligand is generated by thrombin.

51 nd release from the cell surface of membrane-tethered ligands is an important mechanism of regulating

52 sis of interactions of proteins with surface-tethered ligands is introduced.

53 aved at an N-terminal arginine to unmask its tethered ligand, is generally regarded as a target for t

54 psin, SLIGRL-NH2 (corresponding to the PAR-2 tethered ligand), mast cell tryptase, and a filtrate of

55 ns, we have explored the utility of membrane tethered ligands (MTLs).

56 c trypsin and a peptide corresponding to the tethered ligand of PAR-2, which is exposed by trypsin cl

57 rsibly to inhibit receptor activation by the tethered ligand of PAR1.

58 vation because peptides corresponding to the tethered ligand of the thrombin receptor were also able

59 eceptor-activating peptides derived from the tethered ligands of the PAR receptors.

60 The tethered ligand, once exposed, is always available to in

61 lasmin-cleavage sites removes the N-terminal tethered ligand or preligand, thereby providing an effec

62 let [Ca2+]i induced by alpha-thrombin or the tethered ligand peptide (TLP; SFLLRNPNDKYEPF) have been

63 s agonists for probing PAR function, but the tethered ligand peptide for PAR4, GYPGKF, lacks potency

64 o-terminal domain, but Ca2+ responses to the tethered ligand peptide SFLLRNPNDKYEPF were not affected

65 ie2, whereas thrombin and the canonical PAR3 tethered-ligand peptide did not.

66 APC, FXa, and the noncanonical PAR3 tethered-ligand peptide induced prolonged activation of

67 FXa and the noncanonical PAR3 tethered-ligand peptide induced Tie2- and PAR3-dependent

68 In vivo, the APC-derived PAR3 tethered-ligand peptide, but not the thrombin-derived PA

69 PAR3 tethered-ligand peptides beginning at amino acid 42, but

70 Peptides that mimic the tethered ligand portion of the thrombin receptor have th

71 ontrol protein function: the photoswitchable tethered ligand (PTL) approach.

72 by binding covalently to the photoswitchable tethered ligand (PTL) retinal.

73 Photoswitched tethered ligands (PTLs) can be used to remotely control

74 Photoswitched tethered ligands (PTLs) have enabled fast and reversible

75 ceptors can be conjugated to photoswitchable tethered ligands (PTLs) to enable photoactivation, or ph

76 PAR2) is a 7-transmembrane G-protein-coupled tethered ligand receptor that is expressed by pancreatic

77 s to utilize mechanism(s) independent of its tethered ligand receptor to selectively prime phospholip

78 These studies show that the tethered-ligand receptor mediates the GTPase activation

79 o the functioning G protein-linked thrombin (tethered ligand) receptor in human platelet membranes.

80 namics and the kinetics and spatial range of tethered ligand-receptor binding.

81 essions that relate key properties of single-tethered ligand-receptor interactions to multiple bond f

82 ligands that are distinct from the classical tethered ligand revealed by thrombin.

83 h sequences derived from these novel exposed tethered ligands, selectively stimulated PAR1-mediated m

84 cleavage and a synthetic peptide having the tethered ligand sequence (thrombin receptor agonist pept

85 nthetic agonist peptides (AP) that share the tethered ligand sequence also activate PAR2, often measu

86 ird residues of the human thrombin receptor "tethered ligand" sequence (SFLLR) led to a series of ago

87 vated by proteolytic-mediated exposure of a "tethered ligand" sequence and can also be activated by t

88 in the amino acid sequence of the receptors' tethered ligand sequences suggest that their respective

89 AP or SLIGRL-NH2, corresponding to the PAR-2 tethered ligand) stimulated both an 125I- efflux inhibit

90 d a decapeptide mimicking the Cat-S-revealed tethered ligand-stimulated PAR2 coupling to Galphas and

91 otency and constructed a series of synthetic tethered ligands (STLs).

92 as candidate therapeutics, we used membrane-tethered ligand technology.

93 Proteolytic cleavage of PAR(2) reveals a tethered ligand that activates PAR(2) and two major down

94 the extracellular domain of PAR1 generates a tethered ligand that activates PAR1 in an unusual intram

95 trypsin within the NH2-terminus, exposing a tethered ligand that binds and activates the receptor.

96 a new N-terminal domain that functions as a tethered ligand that binds intermolecularly to activate

97 their amino-terminal exodomains to unmask a tethered ligand that binds intramolecularly to the body

98 )) at Arg(36) downward arrowSer(37) reveal a tethered ligand that binds to the cleaved receptor.

99 ough cleavage of the N-terminus, unmasking a tethered ligand that can then interact with the receptor

100 erating a new N terminus that functions as a tethered ligand that cannot diffuse away.

101 2) at R(36) downward arrowS(37) and reveal a tethered ligand that excites nociceptors, causing neurog

102 ctivating peptide (AP), corresponding to the tethered ligand that is exposed upon trypsin cleavage, a

103 major product of III-beta1a processing is a tethered ligand that may act as a cell surface signaling

104 ical site, exposing a previously undescribed tethered ligand that triggers biased G-protein agonism a

105 noncanonical sites, which result in distinct tethered ligands that activate G-protein signaling pathw

106 AR1 signaling and we describe a novel set of tethered ligands that are distinct from the classical te

107 ivated receptors (PARs) to expose N-terminal tethered ligands that bind and activate the cleaved rece

108 Eph receptors and their membrane-tethered ligands, the ephrins, have important functions

109 gamma-thrombin, which does not stimulate the tethered ligand thrombin receptor and caused little or n

110 The tethered-ligand thrombin receptor appeared to mediate th

111 Using the characteristic time for a tethered ligand to bind to a surface receptor, we study

112 volving sequestration or modification of the tethered ligand to prevent or terminate its function.

113 or peptidomimetics can mimic binding of the tethered ligand to stimulate signaling without the nonsp

114 ar surface of PAR2, preventing access of the tethered ligand to the peptide-binding site.

115 In this population, the tethered ligand unmasked by thrombin cleavage must not b

116 However, the distinct non-canonical tethered ligands unmasked by neutrophil elastase and pro

117 hereby exposing a new N-terminal sequence, a tethered ligand, which initiates a cascade of molecular

118 Trypsin cleaves PAR-2 to expose a tethered ligand, which irreversibly activates the recept

119 the protease-mediated "shedding" of membrane-tethered ligands, which then activate EGFRs.

120 nt the interaction of the protease-generated tethered ligand with the body of the receptor.

121 s retained efficacy against both soluble and tethered ligands with lower cLogP values and an increase