ライフサイエンスコーパス: CCR5 antagonist

1 c prostate cancer burden was reduced by oral CCR5 antagonist.

2 roc (VCV), an investigational small-molecule CCR5 antagonist.

3 atient is necessary prior to treating with a CCR5 antagonist.

4 e inflamed lesion, which can be blocked by a CCR5 antagonist.

5 ase with previous HIV-1 strains resistant to CCR5 antagonists.

6 classes, including integrase inhibitors and CCR5 antagonists.

7 d was completely resistant to small molecule CCR5 antagonists.

8 human immunodeficiency virus type 1 (HIV-1) CCR5 antagonists.

9 combination with a variety of small molecule CCR5 antagonists.

10 to retrieve new chemical entities as potent CCR5 antagonists.

11 present a particularly attractive target for CCR5 antagonists.

12 animal models of stroke that administered a CCR5 antagonist and assessed infarct size or behavioural

13 competition underlies inhibitory effects of CCR5 antagonists and explains why adaptive HIV-1 mutatio

14 by which HIV envelopes acquire resistance to CCR5 antagonists and may have more general implications

15 eness to maraviroc, a known immunomodulatory CCR5 antagonist, and to the ceramide-lowering agent Adip

16 were cross resistant to other small-molecule CCR5 antagonists, and were isolated from the patient's p

17 Maraviroc, a CCR5 antagonist antiretroviral drug, might provide benef

18 ins isolated from a patient treated with the CCR5 antagonist aplaviroc (APL) that were drug resistant

19 Furthermore, the CCR5 antagonist aplaviroc was converted to a full agonis

20 ternative coreceptor for HIV-1 entry, CXCR4; CCR5 antagonists are not effective in patients harboring

21 In addition to virologic effects, CCR5 antagonists are under investigation for immune-modu

22 an oxime-piperidine compound, is a specific CCR5 antagonist as determined in multiple receptor bindi

23 e series of piperidine- and piperazine-based CCR5 antagonists as anti-HIV-1 agents reported by Scheri

24 a-associated herpesvirus, is a high affinity CCR5 antagonist, but lacks efficacy as a coreceptor inhi

25 Therefore, we propose that a CCR5 antagonist can serve for HCC cancer prevention and

26 derived recruited macrophages using the CCR2/CCR5 antagonist cenicriviroc in the Mdr2(-/-) mice resul

27 e identification of a novel potent series of CCR5 antagonists containing the imidazolidinylpiperidiny

28 CCR5 antagonists demonstrate promise; however, rigorousl

29 Maraviroc is a new CCR5 antagonist designed to block HIV entry.

30 ration of a clinically utilized FDA-approved CCR5 antagonist, devised for HIV treatment, produces sim

31 he design and development of next generation CCR5 antagonists, docking models for major classes of CC

32 ance to vicriviroc (VCV), an investigational CCR5 antagonist, during 28 weeks of therapy.

33 Thus optimal use of CCR5 antagonists either alone or in combination with oth

34 ist-resistant viruses, then continued use of CCR5 antagonists even in the face of virologic failure c

35 (SCH 351125) as an orally bioavailable human CCR5 antagonist for the treatment of HIV-1 infection.

36 for HIV), we curated data on CCR3, CCR4, and CCR5 antagonists from ChEMBL to develop and validate mac

37 CCR5 is a co-receptor for HIV and CCR5 antagonists have been investigated as inhibitors of

38 A large number of small-molecule CCR5 antagonists have been reported that show potent act

39 d 1,3,4-trisubstituted pyrrolidines as human CCR5 antagonists have recently been disclosed.

40 Additional testing also identified it as an CCR5 antagonist (IC(50), 0.9 muM), and it showed moderat

41 ated by mapping onto it a diverse set of six CCR5 antagonists identified by five different pharmaceut

42 , which may impose constraints on the use of CCR5 antagonists in certain regions of the world.

43 research will further elucidate the role of CCR5 antagonists in combating HIV disease.

44 Further studies of CCR5 antagonists in the dampening of immune activation a

45 ese viruses remained sensitive to most other CCR5 antagonists, including vicriviroc and aplaviroc.

46 CCR5 antagonists inhibit HIV entry by binding to a corec

47 CCR5 antagonists inhibit HIV-1 entry by blocking the int

48 Although resistance to one CCR5 antagonist is often associated with broad cross-res

49 Maraviroc, a CCR5 antagonist, is active against R5 but not X4 or dual

50 CC Envs exhibited partial resistance to the CCR5 antagonist maraviroc (MVC) on cells expressing high

51 failure on treatment regimens containing the CCR5 antagonist maraviroc (MVC).

52 The CCR5 antagonist maraviroc is approved for use in treatme

53 Although only the CCR5 antagonist maraviroc is US Food and Drug Administra

54 We tested the in vitro effect of the CCR5 antagonist maraviroc on lymphocyte function and che

55 y to the fusion inhibitor enfuvirtide or the CCR5 antagonist maraviroc were observed.

56 INK128 enhanced the antiviral potency of the CCR5 antagonist maraviroc, and had favorable antiviral i

57 onuclear cells (PBMC) in the presence of the CCR5 antagonist maraviroc, despite the fact that maravir

58 ood mononuclear cells in the presence of the CCR5 antagonist maraviroc, suggesting that non-CCR5 entr

59 xosomes on POMC neurons were suppressed by a CCR5 antagonist Maraviroc.

60 ge migration, which is inhibited by the CCL5/CCR5 antagonist maraviroc.

61 ced sensitivities to VCV and to the licensed CCR5 antagonist maraviroc.

62 The CCR5 antagonists maraviroc or vicriviroc, developed to b

63 The FDA-approved CCR5 antagonist, maraviroc, reduced TGFbeta1(+)CCR5(+) n

64 There is one CCR5 antagonist, maraviroc, that is FDA-approved for tre

65 Moreover, treatment with a CCR5 antagonist, maraviroc, was protective against C5a-A

66 The principal obstacle to the CCR5-antagonist, maraviroc, from being more widely used

67 ts suggest that low-dose maraviroc and other CCR5 antagonists may be helpful for PD patients.

68 f basal breast cancer cells and suggest that CCR5 antagonists may be used as an adjuvant therapy to r

69 Additionally, CCR5 antagonists may not reduce the HIV-1 RNA load when

70 C-C chemokine receptor type 5 (CCR5) antagonists may improve both acute stroke outcome

71 ed the effects of a potent, highly selective CCR5 antagonist, Merck's compound 167 (CMPD 167), in an

72 Using a selective CCR5 antagonist, methionine-RANTES, CCL2 expression was

73 more potent than a mixture of mu agonist and CCR5 antagonist monovalent ligands.

74 We also investigated the effects of the CCR5 antagonist MVC on functional CCR5(+)CD8(+) T-cell r

75 predicted the binding site of the dual CCR2/CCR5 antagonist N-dimethyl-N-[4-[[[2-(4-methylphenyl)-6,

76 Clinical resistance to CCR5 antagonists occurs in two phases, competitive and n

77 Maraviroc (CCR5 antagonist) or CCL5 immunodepletion diminished 95%

78 C series) that contain mu opioid agonist and CCR5 antagonist pharmacophores linked through homologous

79 CCR5 antagonists reduced infarct volume (standard mean d

80 5) in RGCs or treating wild-type mice with a CCR5 antagonist repressed the effects of CNTF gene thera

81 adaptive amino acid changes had no impact on CCR5 antagonist resistance but made virus more sensitive

82 olates from three participants who developed CCR5 antagonist resistance during treatment with vicrivi

83 nature mutation that can effectively predict CCR5 antagonist resistance.

84 on mechanism that underlies the emergence of CCR5 antagonist resistance.

85 sistance.IMPORTANCE It is believed that each CCR5 antagonist-resistant isolate will develop its own u

86 In contrast to previous reports in which CCR5 antagonist-resistant viruses interact predominantly

87 opism shift proves to be a common feature of CCR5-antagonist-resistant viruses, then continued use of

88 We describe the use of two CCR5 antagonists, Schering-C (SCH-C), which is specific

89 HIV CCR5 antagonists select for env gene mutations that enab

90 CCR5 antagonists significantly improved 11 of 16 behavio

91 not efficiently blocked by a small-molecule CCR5 antagonist, suggesting that sMagi cells express as-

92 ibitors, and entry inhibitors, including the CCR5 antagonist TAK-779 and the CXCR4 antagonist AMD3100

93 RAPA enhanced the antiviral activity of the CCR5 antagonist TAK-779.

94 ced replication, cross-resistance to another CCR5 antagonist, TAK779, and increased sensitivity to am

95 Cenicriviroc, a small-molecule CCR5 antagonist that also has activity as a CCR2 antagon

96 Vicriviroc (VCV) is a CCR5 antagonist that blocks the viral entry of CCR5-trop

97 Maraviroc (MVC) is a CCR5 antagonist that inhibits HIV-1 entry by binding to

98 riviroc is a C-C motif chemokine receptor 5 (CCR5) antagonist that is in clinical development for the

99 We propose that the restoration of pre-CCR5 antagonist therapy HIV entry kinetics drives the se

100 le domain V1/V2 in competitive resistance to CCR5 antagonist therapy.

101 tool for determining patient eligibility for CCR5 antagonist therapy.

102 T-cell recovery, subjects added maraviroc, a CCR5 antagonist, to their existing ART for 24 weeks.

103 ologic failure from a phase IIb study of the CCR5 antagonist vicriviroc (VCV) and identified one indi

104 gonists, docking models for major classes of CCR5 antagonists were created by using site-directed mut

105 inus are broadly cross-resistant to multiple CCR5 antagonists, whereas viruses that require both the

106 -350634 (1), a prototypical piperazine-based CCR5 antagonist, which is a potent inhibitor of HIV-1 en

107 Vicriviroc (VCV) is a CCR5 antagonist with nanomolar activity against human im

108 to the synthesis of Maraviroc, the selective CCR5 antagonist with potent activity against HIV-1 infec

109 the discovery of SCH 351125 (1), a selective CCR5 antagonist with potent activity against RANTES bind

110 We recently described a novel class of CCR5 antagonists with strong anti-HIV potency.

111 (VCV) is a chemokine (C-C motif) receptor 5 (CCR5) antagonist with potent anti-HIV activity that curr

112 rmations by many CC Envs was seen with other CCR5 antagonists, with replication-competent viruses, an