ライフサイエンスコーパス: integrase inhibitor

1 ds for the development of a new class of HIV integrase inhibitor.

2 n between boceprevir and raltegravir, an HIV integrase inhibitor.

3 viral DNA processing site for inhibition by integrase inhibitors.

4 as well as for the molecular pharmacology of integrase inhibitors.

5 oward the potential design of improved HIV-1 integrase inhibitors.

6 ter molecule could open a route to new HIV-1 integrase inhibitors.

7 and offer new catechol isosteres for use in integrase inhibitors.

8 h the identification and characterization of integrase inhibitors.

9 rmation which may guide the future design of integrase inhibitors.

10 oumermycin monomeric derivatives were active integrase inhibitors.

11 irst-line regimen based on second-generation integrase inhibitors.

12 to CAB and cross-resistance to all licensed integrase inhibitors.

13 unsuitable for testing individuals receiving integrase inhibitors.

14 e (PDR) on the efficacy of second generation integrase inhibitors.

15 cleoside reverse transcriptase inhibitors or integrase inhibitors.

16 rus harboring resistance to first-generation integrase inhibitors.

17 tion with clinical reverse transcriptase and integrase inhibitors.

18 dapivirine, rilpivirine, maraviroc, and new integrase inhibitors.

19 IN119 is under selection by HLA alleles and integrase inhibitors.

20 ted PI monotherapies and future options with integrase inhibitors.

21 the viral genome after intensification with integrase inhibitors.

22 ymmetric total synthesis of the potent HIV-1 integrase inhibitor 5 is described.

23 ARV regimens were predominantly based on integrase inhibitors (51.96%).

24 therapy regimens were predominantly based on integrase inhibitors (51.96%).

25 have witnessed the development of allosteric integrase inhibitors, a highly promising class of small

26 Similarly, raltegravir, a pharmacologic integrase inhibitor, abolished HIV-1-induced cell killin

27 ctures additionally informed on the modes of integrase inhibitor action and the means by which HIV ac

28 These studies demonstrate integrase inhibitor activity in vivo and suggest that ce

29 The potency of integrase inhibitors against 3'-processing and their abi

30 The potency of an allosteric integrase inhibitor, ALLINI-2, for rendering produced vi

31 Allosteric integrase inhibitors (ALLINIs) affect multiple viral pro

32 losteric human immunodeficiency virus type 1 integrase inhibitors (ALLINIs) are a new class of antivi

33 Allosteric HIV-1 integrase inhibitors (ALLINIs) have garnered special int

34 inding to the viral RNA genome by allosteric integrase inhibitors (ALLINIs) or through mutations with

35 f HIV-1 integrase inhibitors, the allosteric integrase inhibitors (ALLINIs), engage integrase distal

36 Macaques receiving the integrase inhibitor alone experienced greater viral load

37 protease and integrase, and the most potent integrase inhibitors also inhibited HIV protease.

38 avir has been shown to be non-inferior to an integrase inhibitor and superior to a non-nucleoside rev

39 bitors and drugs in novel classes, including integrase inhibitors and CCR5 antagonists.

40 reen a library of chemicals related to known integrase inhibitors and found a new compound, quinaliza

41 cell depletion, raising the possibility that integrase inhibitors and interventions directed towards

42 that is applicable to a wide range of potent integrase inhibitors and is consistent with the availabl

43 dicted to lead to increases in resistance to integrase inhibitors and non-nucleoside reverse transcri

44 e low prevalence of CRR to second-generation integrase inhibitors and to first-line NRTIs during 2018

45 , 1.76 per 10 U/L; P < .01), and exposure to integrase inhibitors (aOR, 1.28 per year; P = .02) were

46 In 2007, raltegravir became the first integrase inhibitor approved for use in the treatment of

47 zyl-4-hydroxy-1,5-naphthyridin-2(1H)-one HIV-integrase inhibitors are disclosed.

48 Integrase inhibitors are emerging anti-human immunodefic

49 Human immunodeficiency virus type 1 (HIV-1) integrase inhibitors are in clinical trials, and raltegr

50 nd optimization of pyridine-based allosteric integrase inhibitors are reported here.

51 e between pre- and post-integration latency, integrase inhibitors are routinely used, preventing nove

52 The first integrase inhibitors are undergoing clinical trial, but

53 leoside reverse transcriptase inhibitors and integrase inhibitors are used to treat infection with HI

54 C as a single tablet and represent the first integrase inhibitor based complete FDC regimen.

55 The findings support guidelines recommending integrase inhibitor based regimens in first-line antiret

56 nhibitor-based, 100% (95% CI, 91%-100%); and integrase inhibitor based, 95% (95% CI, 83%-99.4%).

57 individuals suggest excess weight gain with integrase inhibitor-based antiretroviral therapy.

58 transmission among pregnant women initiating integrase inhibitor-based ART 20 weeks before delivery w

59 s, whereas 97% of A5345 participants were on integrase inhibitor-based ART.

60 A total of 56/86 (65%) initiated an integrase inhibitor-based regimen and 30/86 (35%) a prot

61 nd chronic HIV infection, in particular when integrase inhibitor-based regimens were used.

62 in PLWH treated with newer drugs (including integrase inhibitor-based regimens), with fat gain due t

63 As shown with triple-drug integrase inhibitor-based regimens, rapid HIV-1 RNA supp

64 ion and might be better tolerated than other integrase inhibitor-based single-tablet regimens, but lo

65 would be the only single-tablet, once-daily, integrase-inhibitor-based regimen for initial treatment

66 s given, EVG/COBI/FTC/TDF would be the first integrase-inhibitor-based regimen given once daily and t

67 inistered subcutaneously and can release the integrase inhibitor cabotegravir (CAB) above protective

68 ong-acting injectable formulation of the HIV integrase inhibitor cabotegravir (CAB-LA) is currently i

69 The use of a combination of the integrase inhibitor, cabotegravir, and the non-nucleosid

70 progress toward a clinically effective HIV-1 integrase inhibitor can at least in part be attributed t

71 treated SIVmac251-infected macaques with an integrase inhibitor combined with a CD8-depleting antibo

72 rystal structure studies illustrate specific integrase-inhibitor contacts that prevent cross-linking

73 For this purpose, we used a known HIV-1 integrase inhibitor containing aryl di-O-acetyl groups (

74 al load, and initiation of treatment with an integrase inhibitor-containing (InSTI-containing) regime

75 ment is associated with long-term failure of integrase inhibitor-containing first-line regimens, and

76 that the rapid decay observed in patients on integrase-inhibitor-containing regimens is not necessari

77 ng-acting injectable cabotegravir is a novel integrase inhibitor currently in advanced clinical devel

78 The HIV integrase inhibitor d[G(3)(TG(3))(3)] forms an extremely

79 e promising lead compounds for further HIV-1 integrase inhibitor development.

80 The integrase inhibitor dolutegravir could have a major role

81 The integrase inhibitor dolutegravir is being considered in

82 The integrase inhibitor dolutegravir is currently a preferre

83 al comparing three-drug ART based on the HIV integrase inhibitor dolutegravir with standard care (non

84 n the plasma drug concentration of the viral integrase inhibitor dolutegravir.

85 human immunodeficiency virus type-1 (HIV-1) integrase inhibitors dolutegravir (S/GSK1349572) (3) and

86 Impact of Integrase-inhibitor DOlutegravir On the viral Reservoir

87 A major integrase inhibitor DRM was observed in 9.4% (n = 3/32;

88 Despite leading to increases in integrase-inhibitor drug resistance, cabotegravir-PrEP i

89 lability were analyzed for NTD reports for 4 integrase inhibitors (DTG, raltegravir, elvitegravir, bi

90 The integrase inhibitor elvitegravir (EVG) has been co-formu

91 ty of the human immunodeficiency virus (HIV) integrase inhibitor elvitegravir to comparator ritonavir

92 e CYP3A without anti-HIV activity) and a new integrase inhibitor, elvitegravir (EVG).

93 In addition, the approval of the second integrase inhibitor, elvitegravir, and a novel pharmacoe

94 appears to be a more favorable effect of the integrase inhibitor EVG over efavirenz on immune activat

95 Additionally, in integrase inhibitor-experienced patients, only R263K and

96 Besides BMI and ALT, integrase inhibitor exposure was associated with higher

97 index, Ethiopian origin, HIV duration, lower integrase inhibitor exposure, and advanced disease at di

98 macophore of aryl beta-diketo acids (DKA) as integrase inhibitors, fails in certain cases of highly e

99 ir recommended as a preferred or alternative integrase inhibitor for pregnant women living with HIV.

100 well as the promises and challenges of using integrase inhibitors for HIV/AIDS management.

101 ine recommendations to use second-generation integrase inhibitors for treatment-experienced patients.

102 need to accelerate the study and approval of integrase inhibitors for use in young children.

103 very of 10 novel, structurally diverse HIV-1 integrase inhibitors, four of which have an IC50 value l

104 linking assays to probe the binding sites of integrase inhibitors from different chemical families an

105 a three-drug regimen that did not include an integrase inhibitor, future research should focus on par

106 d virological failure with resistance in the integrase inhibitor group compared with three participan

107 252 (87%) women in the integrase inhibitor group had plasma HIV-1 RNA less than

108 of adverse events compared with five in the integrase inhibitor group.

109 thesis of a complex chiral atropisomeric HIV integrase inhibitor has been accomplished.

110 human immunodeficiency virus type 1 (HIV-1) integrase inhibitor, has limited cross-resistance to ral

111 coformulations of nucleoside analogs and an integrase inhibitor have been used for parenteral antire

112 Previous screens for integrase inhibitors have assayed inhibition of reaction

113 Integrase inhibitors have been recently linked to a high

114 The structures of a large number of HIV-1 integrase inhibitors have in common two aryl units separ

115 leoside reverse transcriptase inhibitors and integrase inhibitors have slopes of approximately 1, cha

116 TIs (NNRTIs), protease inhibitors (PIs), and integrase inhibitors (IIs) did not affect HK2, except fo

117 e, tolerability, and access of a widely used integrase inhibitor in both resource limited and rich se

118 linical demonstration of the activity of any integrase inhibitor in subjects with HIV-1 resistant to

119 However, there are currently no integrase inhibitors in clinical use for AIDS.

120 automated LC-MS/MS methods to quantify five integrase inhibitors in plasma with the limits of quanti

121 cleotide (e.g., human immunodeficiency virus integrase) inhibitors, in applications such as antisense

122 (DTG), a human immunodeficiency virus (HIV) integrase inhibitor (INI), would be efficacious in INI-r

123 Integrase inhibitors (INIs) are a key component of antir

124 Two-metal binding HIV-1 integrase inhibitors (INIs) are potent inhibitors of HIV

125 ed the prevalence of PDDIs in the era of HIV integrase inhibitors (INIs), characterized by more favor

126 he era of human immunodeficiency virus (HIV) integrase inhibitors (INIs), characterized by more favor

127 Furthermore, one month of ART including an integrase inhibitor, initiated at day 3, but not day 4 o

128 s of these cells in individuals treated with integrase inhibitor (INSTI) based ART regimens compared

129 This proposed binding mechanism for integrase inhibitors involves interaction with a specifi

130 genotypes exclude testing for resistance to integrase inhibitors ("IR testing"), although this class

131 deficiency virus (HIV) treatments containing integrase inhibitors is unknown.

132 ncy levels described in models that only use integrase inhibitors may be overestimated.

133 AG1/2 and integrase and suggest that certain integrase inhibitors may have the potential to interfere

134 results further indicate that resistance to integrase inhibitors may include both integrase and LTR

135 tiretroviral drugs under study, particularly integrase inhibitors, may prove useful in treatment-naiv

136 lop a long-acting vaginal film to deliver an integrase inhibitor, MK-2048, for prevention of HIV-1 in

137 Integrase-inhibitor-naive patients with HIV resistant to

138 ble long-term efficacy and safety profile in integrase-inhibitor-naive patients with triple-class res

139 curcumin analog with the recently described integrase inhibitor NSC 158393 resulted in integrase inh

140 HIV-1 integrase, we sought to determine how integrase inhibitors of the diketo acid type would affec

141 Integrase inhibitors of the strand transfer reaction rem

142 ction analysis to investigate the effects of integrase inhibitors on each step in the reaction.

143 trate this by comparing the effect of RT and integrase inhibitors on viral dynamics.

144 For integrase inhibitors, only IC(50) is affected.

145 cells infected either in the presence of an integrase inhibitor or with an integrase-deficient virus

146 first ART regimens or regimens that include integrase inhibitors or two drugs.

147 by baseline regimen (ie, protease inhibitor, integrase inhibitor, or other).

148 Allosteric HIV-1 integrase inhibitors promote aberrant IN multimerization

149 It is unclear whether the integrase inhibitor raltegravir (RAL) reduces inflammati

150 148R(H)(K) that reduce susceptibility to the integrase inhibitor raltegravir have been identified in

151 Recent clinical trials of the integrase inhibitor raltegravir have demonstrated more r

152 Titration of PF74 against the integrase inhibitor raltegravir showed an additive antiv

153 y acquired significant resistance to APV, an integrase inhibitor raltegravir, and a GRL-09510 congene

154 rotease (Mpro) inhibitor ebselen and the HIV integrase inhibitor raltegravir, revealing the potential

155 tion of proviruses to the PNC was blocked by integrase inhibitor Raltegravir, suggesting it was due t

156 itors zidovudine (AZT) and tenofovir and the integrase inhibitor raltegravir.

157 virine, ritonavir-boosted lopinavir, and the integrase inhibitors raltegravir and elvitegravir.

158 Although antiretroviral regimens containing integrase inhibitors rapidly suppress HIV viral load in

159 tion of MLV(HCV) pseudoviruses was higher in integrase inhibitor recipients (71.8% vs. 21.3%).

160 Non-HCV-specific inhibition was detected in integrase inhibitor recipients.

161 289 were randomly assigned to receive the integrase inhibitor regimen and 286 to receive the prote

162 the safety and efficacy of the single tablet integrase inhibitor regimen containing elvitegravir, cob

163 citabine, and tenofovir disoproxil fumarate (integrase inhibitor regimen) or ritonavir-boosted atazan

164 HIV drug resistance testing beforehand shows integrase inhibitor resistance (resistance test policy),

165 Data on integrase inhibitor resistance come primarily from clini

166 When present in certain combinations, some integrase inhibitor resistance mutations increased resis

167 ever, 25 out of 41 mutations associated with integrase inhibitor resistance were present.

168 antiretroviral therapy, the proportion with integrase-inhibitor resistance after 20 years is project

169 We consider three groups at risk of integrase-inhibitor resistance emergence: people who sta

170 ts introduction could lead to an increase in integrase-inhibitor resistance undermining treatment pro

171 , resistance-associated mutations to RPV and integrase inhibitors, respectively.

172 Based upon a class of known HIV-1 integrase inhibitors, several pharmacophore models were

173 Cross-linking interference by eight integrase inhibitors shows that the most potent cross-li

174 on data derived from a large number of HIV-1 integrase inhibitors, similar structural features can be

175 antiretroviral drugs showed interference by integrase inhibitors (specifically, dolutegravir).

176 xil fumarate, saquinavir, atazanavir, and an integrase inhibitor starting at 12 days after inoculatio

177 ed to integrase, which is also the target of integrase inhibitors such as raltegravir.

178 h viral replication and raltegravir (RAL; an integrase inhibitor) suppression, mimicking active and A

179 It has been shown that L-731988, a potent integrase inhibitor, targets a conformation of the integ

180 for T30695, which is the most potent of the integrase inhibitors that have been identified thus far.

181 Unlike integrase inhibitors that interact with the DNA substrat

182 A separate class of HIV-1 integrase inhibitors, the allosteric integrase inhibitor

183 Among all the HIV-1 integrase inhibitors, the beta-diketo acids (DKAs) repre

184 evel replication of HIV-1 in the presence of integrase inhibitor therapy.

185 have compared the safety and efficacy of any integrase inhibitor to efavirenz when initiated during p

186 y virus (HIV)-infected individuals receiving integrase inhibitor treatment.

187 h incident proteinuria, while lamivudine and integrase inhibitor use were associated with a lower ris

188 significantly shorter in those receiving an integrase inhibitor- versus a protease inhibitor-based r

189 ase inhibitors, 7 protease inhibitors, and 1 integrase inhibitor was achieved in 0.25 g of meconium.

190 No resistance to integrase inhibitors was identified in patients receivin

191 human immunodeficiency virus type 1 (HIV-1) integrase inhibitor, was evaluated for distribution and

192 avir (S/GSK1349572), a once-daily, unboosted integrase inhibitor, was recently approved in the United

193 New integrase inhibitors were also identified.

194 Although integrase inhibitors were the last among this group to b

195 uctural leads for the development of new HIV integrase inhibitors which do not rely on this potential

196 rk has resulted in the identification of new integrase inhibitors which may be regarded as bis-caffeo

197 ence of reverse-transcriptase inhibitors and integrase inhibitors, which allows for the specific isol

198 nhibitors were quinolone antibiotics and HIV integrase inhibitors, which share common structural feat

199 Compound 8g was also the most potent integrase inhibitor with an IC50 value of 26 nM.

200 tructural basis and rationale for developing integrase inhibitors with the potential for unique and n

201 leoside reverse transcriptase inhibitors and integrase inhibitors (without cobicistat).