ライフサイエンスコーパス: GnRH receptor

1 assay in HEK-293 cells expressing the human GnRH receptor.

2 he latter were partial agonists in the human GnRH receptor.

3 erent species in the single functional human GnRH receptor.

4 = 3.0 nM in Ca(2+) flux assay) at the human GnRH receptor.

5 assay in HEK-293 cells expressing the human GnRH receptor.

6 otrophs and transfected cells expressing the GnRH receptor.

7 -4-ylamide (1) as a potent antagonist of the GnRH receptor.

8 he uninduced cells, which do not express the GnRH receptor.

9 neurons, which both secrete GnRH and express GnRH receptors.

10 receptors such as M1, M5, histamine H1, and GNRH receptors.

11 fect blocked by antagonism of mGluRs but not GnRH receptors.

12 ide antagonists with human, rat, and macaque GnRH receptors.

13 n of extra-pituitary cancer cells expressing GnRH receptors.

14 on in response to activation of cell surface GnRH receptors.

15 en together, these results indicate that the GnRH receptor activates both G(q) and G(s) signaling to

16 Neither EGF nor GnRH receptor activation caused translocation of phospho

17 d exploit the growth-inhibitory potential of GnRH receptor activation in abnormal cells in diseased h

18 Therefore, we compared the effects of GnRH receptor activation in transfected HEK293 cells (HE

19 Subsequently, GnRH receptor activation was completely abolished with a

20 ently decreased the impedance as a result of GnRH receptor activation with potencies of 9.3 +/- 0.1 (

21 ly following gonadotropin-releasing hormone (GnRH) receptor activation.

22 , and 7 (Ile(322) and Tyr(323)) of the human GnRH receptor allosterically increased ligand binding af

23 acid sequences uniquely present in the human GnRH receptor amino terminus and extracellular loop 2 ma

24 ntagonists optimized for affinity to the rat GnRH receptor and in vivo antiovulatory potency.

25 Therefore, differences in levels of GnRH receptor and signaling differentially affect the ap

26 ide diastereomers have high affinity for the GnRH receptor and were equipotent with acyline in the AO

27 ticipates in the functional coupling between GnRH receptors and PLD pathway.

28 ctivation of gonadotropin-releasing hormone (GnRH) receptors and inhibition of endoplasmic reticulum

29 f pituitary gonadotrophin releasing hormone (GnRH) receptors and the second after 9 days of gonadotro

30 ifferentiation (expression of alpha-subunit, GnRH receptor, and LH beta-subunit but not FSH beta-subu

31 orally bioavailable, potent, small molecule GnRH receptor antagonist N-{4,6-dimethoxy-2-[(3-morpholi

32 cophores for gonadotropin-releasing hormone (GnRH) receptor antagonist activity.

33 , which was abolished by pretreatment with a GnRH-receptor antagonist.

34 and SAR studies of 6-methyluracils as human GnRH receptor antagonists are discussed herein.

35 This is the first time that monocycle-based GnRH receptor antagonists are reported.

36 The use of GnRH receptor antagonists has been reported in the liter

37 2-a]pyrimidines 3 and 4, as nonpeptide human GnRH receptor antagonists, lead us to believe that the a

38 olo[1,2-a]pyrimidone core to generate potent GnRH receptor antagonists.

39 bled us to obtain smaller but equally potent GnRH receptor antagonists.

40 ly available gonadotropin-releasing hormone (GnRH) receptor antagonists have led to the discovery of

41 (Ser-203, Gln-208) and III (Leu-300) of the GnRH receptor appear to be primarily responsible for spe

42 because the gonadotropin-releasing hormone (GnRH) receptor appears to have interchanged the Asp(2.50

43 n vitro binding affinity is observed for the GnRH receptor as compared to the initial screening lead.

44 d G protein-coupled receptors, including the GnRH receptor as well as mono-amine receptors, have iden

45 d in position 2.50(87) for expression of the GnRH receptor at the cell surface, most likely through a

46 amolecular interaction networks in the human GnRH receptor by mutating remote residues that induce di

47 ctivation of gonadotropin-releasing hormone (GnRH) receptors causes inositol 1,4,5-trisphosphate (Ins

48 usly that GH3 cells transfected with the rat GnRH receptor cDNA (GGH3-1' cells) support the expressio

49 ceptors, the gonadotropin-releasing hormone (GnRH) receptor contains an apolar amino acid in this reg

50 lix 2 of the gonadotropin-releasing hormone (GnRH) receptor decreased the affinity for GnRH.

51 In contrast, agonist stimulation of GnRH receptors expressed in HEK293 cells caused sustaine

52 Activation of GnRH receptors, expressed at high or moderate levels, in

53 cellular loop is an important determinant of GnRH receptor expression and activation, and possibly th

54 Low levels of GnRH receptor expression in transfected SKOV3, EFO21, or

55 in pituitary alphaT3-1 cells with endogenous GnRH receptor expression.

56 We now report the cloning of a type II GnRH receptor from marmoset cDNA.

57 role of this conserved residue (Leu(237)) in GnRH receptor function revealed that the binding affinit

58 r 2 gene PROKR2 (R85H and L173R), one in the GnRH receptor gene GNRHR (R262Q), and one in the Kallman

59 ike human or mouse, escapes the DN effect of GnRH receptor (Gn-RHR) mutants because rGnRHR mutants ro

60 escribe the mRNA expression pattern of these GnRH receptor (GnRH-R) subtypes in the brain, specifical

61 nced by agonist activation of the endogenous GnRH receptor (GnRH-R), which couples to G(q/11) as indi

62 RH neurons (GT1-7 cells), which also express GnRH receptors, GnRH, epidermal growth factor (EGF), and

63 Here, we investigated GR and GnRH receptor (GnRHR) cross-talk that involves co-locali

64 The primate GnRH receptor (GnRHR) is a GPCR (G-protein-coupled recep

65 in-releasing hormone (GnRH) to the pituitary GnRH receptor (GnRHR) is essential for reproductive func

66 GABAergic neurons express type-1 GnRH receptor (GnRHR-1).

67 orrelates directly with the concentration of GnRH receptors (GnRHR) on the cell surface, which is med

68 orrelates directly with the concentration of GnRH receptors (GnRHR) on the cell surface, which is med

69 ution of the gonadotropin-releasing hormone (GnRH) receptor (GnRHR) progressively decreases inositol

70 encoding the gonadotropin-releasing hormone (GnRH) receptor (GnRHR).

71 transfer via gonadotropin-releasing hormone (GnRH) receptors (GnRHR) to extracellular signal-regulate

72 The human GnRH receptor has a higher affinity for the cognate GnRH

73 upling to heterotrimeric G proteins, but the GnRH receptor has transferred the requirement for an aci

74 antitumor effects through the high-affinity GnRH receptors has been questioned because of the low le

75 t that following a gene duplication, the two GnRH receptors have evolved to serve different functions

76 ereby confirming the Galphaq-coupling of the GnRH receptor in pituitary alphaT3-1 cells.

77 y basic first intracellular (1i) loop of the GnRH receptor in signal transduction was evaluated by mu

78 The presence of two GnRH receptors in gonadotropes, together with the differ

79 ctivation of gonadotropin-releasing hormone (GnRH) receptors inhibits proliferation of transformed ce

80 xplore the signaling mechanisms by which the GnRH receptor is coupled to activation of another member

81 ndings indicate that cAMP signaling from the GnRH receptor is dependent on specific residues in the 1

82 The gonadotropin-releasing hormone (GnRH) receptor is a drug target for certain hormone-depe

83 The human gonadotropin-releasing hormone (GnRH) receptor is evolutionarily configured for high aff

84 le-like brain characteristics in adult male, GnRH receptor knock-out mice.

85 nvestigated which G proteins are involved in GnRH receptor-mediated signaling in L beta T2 pituitary

86 Gonadotropin-releasing hormone (GnRH) receptor mutants from patients with hypogonadotrop

87 ecently that gonadotropin-releasing hormone (GnRH) receptor occupancy results in activation of extrac

88 , direct, and mediated through high-affinity GnRH receptors present on the cell membranes of tumor ce

89 gonist, but not antagonist, occupancy of the GnRH receptor promotes physical intimacy (microaggregati

90 nance energy transfer to monitor the rate of GnRH receptor-receptor interactions.

91 Hence, GnRH receptors represent a therapeutic target for direct

92 high affinities (K(i) < 0.5 nM) for the rat GnRH receptor (rGnRHR).

93 GnRH receptor subtypes GnRHR1 and GnRHR2 were expressed

94 ble of targeting cancer cells expressing the GnRH receptor such as prostate, breast, ovarian, endomet

95 potent nonpeptidyl antagonist for the human GnRH receptor that is efficacious for the suppression of

96 rs we show that the unique resistance of the GnRH receptor to rapid desensitization contributes to a

97 dditional GnRH forms, we localized two known GnRH receptor types in a cichlid fish, Astatotilapia bur

98 en together, these data suggest that the two GnRH receptor types serve different functional roles in

99 line (EcRG293) that expresses high-affinity GnRH receptor under the control of an inducible promoter

100 The expression of GnRH receptors was assessed in a normal mouse cholangioc

101 bearing the gonadotropin-releasing hormone (GnRH) receptor, we could not detect binding or cytotoxic

102 se C-coupled gonadotropin-releasing hormone (GnRH) receptors, we previously reported marked suppressi

103 r modeling of the TM V and VI regions of the GnRH receptor, which predicts that Leu(237) is caged by

104 The gonadotropin-releasing hormone (GnRH) receptor, which is a unique G protein-coupled rece

105 It also bound to the monkey GnRH receptor with high affinity (K(i) = 3.9 nM).

106 -subunit and gonadotropin-releasing hormone (GnRH) receptor, yet are not fully differentiated in that