ライフサイエンスコーパス: CETP

1 CETP and ABCG1 may be important mediators of these effec

2 CETP and ABCG1, both of which participate in the HDL-med

3 CETP genotypes did not associate with variation in marke

4 CETP inhibition has been regarded as a promising strateg

5 CETP inhibition increased plasma high-density lipoprotei

6 CETP inhibition increased postprandial insulin and promo

7 CETP inhibitors block the transfer of cholesteryl ester

8 CETP inhibitors form a complex between themselves, CETP,

9 CETP PTV carrier status was associated with reduced risk

10 CETP-D HDL-2 caused a 2- to 3-fold stimulation of net ch

11 CETP-deficient cells had 4-fold more CE but an approxima

12 ) or normal coronaries were genotyped for 11 CETP tSNPs.

13 To date, 4 CETP inhibitors have entered phase 3 cardiovascular outc

14 alleles at two loci (LIPC, P = 1.3 x 10(-7); CETP, P = 7.4 x 10(-7)) that were previously associated

15 With the goal of identifying a CETP inhibitor with high in vitro potency and optimal in

16 Anacetrapib (MK-0859) is a CETP inhibitor currently under development.

17 ger receptor class B type 1) to the liver, a CETP-independent m-RCT path exists, in which LDL mediate

18 The current study assessed the effects of a CETP inhibitor on postprandial insulin, ex vivo insulin

19 e evaluated HDL-C modification from use of a CETP inhibitor.

20 tures of CETP in complex with torcetrapib, a CETP inhibitor that has been tested in phase 3 clinical

21 transport in humans, raising hope of using a CETP inhibitor to elevate HDL levels.

22 ective, but an initial clinical trial with a CETP inhibitor was stopped prematurely because of increa

23 , whereas LPL, TRIB1, ABCA1, APOA1-C3-A4-A5, CETP, and APOE displayed significant strongest associati

24 r genes involved in lipid metabolism (ABCA1, CETP, APOE, and LIPC) with metabolites belonging to the

25 dividual rare variants in PCSK9, ANGPTL4 and CETP in the Action to Control Cardiovascular Risk in Dia

26 OC2 (Apolipoproteins E, C1, C4, and C2), and CETP (Cholesteryl Ester Transfer Protein).

27 in hydrophobic contacts between the CEs and CETP, and a continuous tunnel traversing across the CETP

28 lesterol, LPL, ABCA1, ZNF259/APOA5, LIPC and CETP for HDL cholesterol, CELSR2, APOB and NCAN/MAU2 for

29 elated strongly with that of KC markers, and CETP messenger RNA and protein colocalized specifically

30 0), LIPC (rs10468017), TIMP3 (rs9621532) and CETP (rs3764261) were confirmed with genome-wide signifi

31 of pleiotropy for APOE, TOMM40, TCF7L2, and CETP variants, many with opposing effects (eg, the same

32 SW872 adipocytes stably expressing antisense CETP cDNA and synthesizing 20% of normal CETP were creat

33 ucose and 4 lipids loci (TCF7L2, LPL, APOA5, CETP, and APOC1/APOE/TOMM40) significantly associated wi

34 A4-APOC3-APOA1 and APOE-APOC clusters, APOB, CETP, GCKR, LDLR, LPL, LIPC, LIPG and PCSK9) and also in

35 2, TNFA), gene-alcohol (ALDH2, APOA5, APOC3, CETP, LPL), gene-smoking (APOC3, CYBA, LPL, USF1), gene-

36 Several SNPs (e.g. in APOE, CETP, LPL, APOB and LDLR) influenced multiple phenotypes

37 nd replicated for baseline Lp-PLA(2) mass at CETP and for Lp-PLA(2) activity at the APOC1-APOE and PL

38 ompared with noncarriers, carriers of PTV at CETP displayed higher high-density lipoprotein cholester

39 ompared with noncarriers, carriers of PTV at CETP had higher high-density lipoprotein cholesterol (ef

40 as and amides as potent and orally available CETP inhibitors.

41 analyses evaluating the association between CETP and HMGCR scores, changes in lipid and lipoprotein

42 We find a strong association between CETP Asp442Gly (rs2303790), an East Asian-specific mutat

43 BPI-CETP chimeras are inhibited by LPS but cannot be inhibit

44 Our study indicates that the APOA5, BUD13, CETP, and LIPA genes may contribute to the risk of MetS

45 sociated with the APOA5, APOC1, BRAP, BUD13, CETP, LIPA, LPL, PLCG1, and ZPR1 genes.

46 cern that large, CE-rich HDL(2) generated by CETP inhibition might impair reverse cholesterol transpo

47 Modification of the lipoprotein profile by CETP inhibitors is promising, but the beneficial effect

48 nnel mechanism for neutral lipid transfer by CETP.

49 the mechanism of CE/triglyceride transfer by CETP.

50 The capacity of cellular CETP to transport CE and TG into storage droplets was di

51 subjects with homozygous deficiency of CETP (CETP-D) to promote cholesterol efflux from macrophages a

52 The consequences of chronic CETP deficiency in lipid-storing cells normally expressi

53 Overall, chronic CETP deficiency disrupts lipid homeostasis and compromis

54 Data relating circulating CETP concentrations to CVD incidence in the community ar

55 In conclusion, CETP inhibition does not appear to affect size-specific

56 Arg468Gln) and a genetic score for decreased CETP function on 28-day sepsis survival using Cox propor

57 In addition, a genetic score for decreased CETP function was associated with significantly decrease

58 l of APOE*3-Leiden mice that did not express CETP (50.0% versus 42.9%, Log-rank P=0.87).

59 y in lipid-storing cells normally expressing CETP have not been reported.

60 We discuss the two failed CETP inhibitors, torcetrapib and dalcetrapib, and attemp

61 Despite two failures, CETP inhibitors are still in clinical development.

62 RECENT FINDINGS: Torcetrapib, the first CETP inhibitor tested in a phase III clinical trial (ILL

63 by particle size; 95% CI: -0.10 to 0.05 for CETP versus -0.24 SD, 95% CI -0.30 to -0.18 for HMGCR).

64 sis, demonstrating an intracellular role for CETP as well.

65 ytic cells strongly support a novel role for CETP in intracellular lipid transport and storage.

66 To date, four CETP inhibitors have advanced to phase 3 cardiovascular

67 MIN6N8 beta-cells incubated with plasma from CETP inhibitor-treated individuals (compared with placeb

68 ian-specific coding variants in known genes (CETP p.Asp459Gly, PCSK9 p.Arg93Cys and LDLR p.Arg257Trp)

69 Genetic CETP inhibition associates with reductions in risk of is

70 in CETP Tg mice virtually abolished hepatic CETP expression and largely reduced plasma CETP concentr

71 Hepatic KC content as well as hepatic CETP expression correlated strongly with plasma CETP con

72 Guerin vaccination largely increased hepatic CETP expression and plasma CETP.

73 located in LDLR, PCSK9, APOB, CELSR2, HMGCR, CETP, the TOMM40-APOE-C1-C2-C4 cluster, and the APOA5-A4

74 CETP is known, little is known regarding how CETP binds to HDL.

75 in promoter was used to stably express human CETP in livers of mice and was compared with an AAV8-lac

76 transgenic (Tg) mouse model expressing human CETP.

77 In high-fat fed hamsters, human CETP transgenic mice, and cynomolgus monkeys, the in viv

78 activity at an oral dose of 1 mg/kg in human CETP/apoB-100 dual transgenic mice and increased HDL cho

79 ale APOE*3-Leiden mice with or without human CETP expression using the cecal-ligation and puncture mo

80 Our results identify CETP as a critical regulator of HDL levels and clinical

81 esterolemia that were naturally deficient in CETP (cholesteryl ester transfer protein) and fed a West

82 Given ongoing therapeutic development in CETP inhibition and other HDL-raising strategies, furthe

83 zed CE and TG into lipid storage droplets in CETP-deficient cells was just 40% of control, suggesting

84 lective elimination of KCs from the liver in CETP Tg mice virtually abolished hepatic CETP expression

85 However, cholesterol mass in CETP-deficient adipocytes was actually reduced.

86 ETP previously associated with reductions in CETP activity, thus mimicking the effect of pharmacologi

87 [CI]: 1.19-1.91; P = 0.001) and rs1532624 in CETP (OR = 0.82; CI: 0.69-0.99; P = 0.034); rs4420638 wa

88 The hydrolysis of cellular CE and TG in CETP-deficient cells was reduced by >50%, although hydro

89 We identified a rare missense variant in CETP (cholesteryl ester transfer protein gene; rs1800777

90 the effect of a gain-of-function variant in CETP (rs1800777, p.Arg468Gln) and a genetic score for de

91 Genetic variants in CETP associated with increased HDL-C raise the risk of I

92 We selected 2 common genetic variants in CETP previously associated with reductions in CETP activ

93 DL cholesterol and apolipoprotein AI were in CETP, LPL, LIPC, APOA5-A4-C3-A1, and ABCA1; and SNPs ass

94 First, we tested individual CETP variants in a discovery cohort of 1,149 ICH cases a

95 Inefficient CETP-mediated translocation of CE and TG from the endopl

96 RATIONALE: Therapies that inhibit CETP (cholesteryl ester transfer protein) have failed to

97 lasma HDL-C; as such, medicines that inhibit CETP and raise HDL-C are in clinical development.

98 usion, increasing HDL-C levels by inhibiting CETP activity is associated with inhibition of intimal h

99 manized mouse models suggest that inhibiting CETP may preserve high-density lipoprotein levels and im

100 odels that apolipoprotein (apo) C-I inhibits CETP, and that high mono-unsaturated fat diets prevent t

101 ETP expression in mice (which naturally lack CETP) on macrophage RCT, including in mice that lack the

102 APOE*3-Leiden.CETP mice treated with anacetrapib had preserved levels

103 erosclerosis in hyperlipidemic APOE*3-Leiden.CETP mice, a well-established model for human-like lipop

104 d the underlying mechanisms in APOE*3-Leiden.CETP mice, a well-established model for human-like lipop

105 ked to increased HDL levels in APOE*3-Leiden.CETP mice.

106 etected at LPL, TRIB1, APOA1-C3-A4-A5, LIPC, CETP, and LDLR (P range from 4.84x10(-4) to 4.62x10(-18)

107 in ANGPTL3, APOB, ABCA1, NR1H3, APOA1, LIPC, CETP, LDLR, and APOC1) and replicated 14 variants.

108 TRA1 genes/regions and the novel genes LIPC, CETP, and ABCA1 in the high-density lipoprotein (HDL) ch

109 itively differentiate from highly lipophilic CETP inhibitors in its complete elimination from fat tis

110 We used an allele associated with lower CETP expression (rs247617) to mimic CETP inhibition and

111 Variants in the genes LPL, CETP, APOA5 (and its cluster), GCKR (and its cluster), L

112 oprotein receptor/apobec-1 double-null mice, CETP expression reduced high-density lipoprotein cholest

113 cavenger receptor class B, type I-null mice, CETP expression reduced high-density lipoprotein cholest

114 In apobec-1-null mice, CETP expression reduced plasma high-density lipoprotein

115 th lower CETP expression (rs247617) to mimic CETP inhibition and an allele associated with lower HMGC

116 PS but cannot be inhibited by small molecule CETP inhibitors as effectively as native CETP.

117 ule CETP inhibitors as effectively as native CETP.

118 teractions that are not observed with native CETP.

119 Evacetrapib, a relatively new CETP inhibitor, exhibited favorable changes in the lipid

120 nse CETP cDNA and synthesizing 20% of normal CETP were created.

121 TA-8995, a novel CETP inhibitor, is well tolerated and has beneficial eff

122 te may provide opportunities to design novel CETP inhibitors possessing more drug-like physical prope

123 erminus of BPI did not retain any observable CETP function.

124 on is explained, in part, by the activity of CETP, a major determinant of plasma HDL-C levels.

125 We performed 2 candidate-gene analyses of CETP.

126 The inverse association of CETP activity with CVD incidence remained robust in time

127 We tested association of CETP PTV carrier status with both plasma lipids and CHD.

128 opments, and the discovery of new classes of CETP inhibitors.

129 LCAT and apoE contents of CETP-D HDL-2 were markedly increased compared with contr

130 from subjects with homozygous deficiency of CETP (CETP-D) to promote cholesterol efflux from macroph

131 The development of CETP (cholesteryl ester transfer protein) inhibitors has

132 ealthy participants received a daily dose of CETP inhibitor (n=10) or placebo (n=15) for 14 days in a

133 tudy, we explore the large scale dynamics of CETP by means of multimicrosecond molecular dynamics sim

134 ssay of macrophage RCT to test the effect of CETP expression in mice (which naturally lack CETP) on m

135 However, the beneficial effect of CETP inhibition on cardiovascular outcome remains to be

136 tion and atherosclerosis, and the effects of CETP inhibition on cholesterol efflux and reverse choles

137 ene may provide insight into the efficacy of CETP inhibition.

138 Hepatic expression of CETP correlated strongly with that of KC markers, and CE

139 bariatric surgery, showed that expression of CETP is markedly higher in liver than adipose tissue.

140 ies have shown that blocking the function of CETP can increase the level of HDL cholesterol in blood

141 We review the genetics of CETP and coronary disease, preclinical data on CETP inhi

142 Inhibition of CETP also lowers triglyceride composition in HDL particl

143 Genetic inhibition of CETP and HMGCR resulted in near-identical associations w

144 Inhibition of CETP has been shown to raise human plasma HDL cholestero

145 suggested that pharmacological inhibition of CETP may be beneficial.

146 larify associations of genetic inhibition of CETP on detailed lipoprotein measures and compare those

147 Inhibition of CETP was strongly associated with lower proportion of tr

148 trast, the associations of the inhibition of CETP were stronger on lower remnant and very-low-density

149 hat genetic or pharmacological inhibition of CETP would preserve high-density lipoprotein levels and

150 sing the level of HDL-C is the inhibition of CETP.

151 Torcetrapib, an inhibitor of CETP, increased risk of death and ischemic cardiovascula

152 strategy for attenuating the interaction of CETP with HDL.

153 0 amino acids resulted in a complete loss of CETP function even though the chimera was able to retain

154 mation about the lipid transfer mechanism of CETP.

155 the recently proposed "tunnel mechanism" of CETP from cryo-EM studies for the transfer of neutral li

156 s have documented the efficacy and safety of CETP inhibitors in combination with commonly used statin

157 A genetic score of CETP variants found to increase HDL-C by approximately 2

158 fat diets prevent the normal stimulation of CETP activity by dietary cholesterol.

159 Although the crystal structure of CETP is known, little is known regarding how CETP binds

160 Here, we report the crystal structures of CETP in complex with torcetrapib, a CETP inhibitor that

161 However, short term suppression of CETP biosynthesis in cells alters cellular cholesterol h

162 variants in the gene locus of the target of CETP inhibitors were associated with lower risk of small

163 ants in the genes that encode the targets of CETP inhibitors and statins was associated with discorda

164 Chimeras containing the amino terminus of CETP and the carboxy terminus of BPI did not retain any

165 narrowing neck of the hydrophobic tunnel of CETP and thus block the connection between the N- and C-

166 TP and coronary disease, preclinical data on CETP inhibition and atherosclerosis, and the effects of

167 However, trials of other CETP inhibitors have shown neutral or adverse effects on

168 Whether pharmacologic CETP inhibition will reduce the risk of cardiovascular d

169 thus mimicking the effect of pharmacological CETP inhibition.

170 Plasma CETP is predominantly derived from KCs, and plasma CETP

171 METHODS AND Plasma CETP activity was measured in 1978 Framingham Heart Stud

172 s predominantly derived from KCs, and plasma CETP level predicts hepatic KC content in humans.

173 increased hepatic CETP expression and plasma CETP.

174 high-density lipoprotein cholesterol, plasma CETP activity was related inversely to the incidence of

175 on of a community-based sample, lower plasma CETP activity was associated with greater CVD risk.

176 n with des-fluoro-anacetrapib reduced plasma CETP activity by 89 +/- 6.9%, increased plasma apolipopr

177 c CETP expression and largely reduced plasma CETP concentration, consequently improving the lipoprote

178 er KC content, accompanied by reduced plasma CETP concentration.

179 on the role of KCs in determining the plasma CETP concentration were performed in a transgenic (Tg) m

180 P expression correlated strongly with plasma CETP concentration.

181 on led to the potent and comparatively polar CETP inhibitor 26 showing robust high density lipoprotei

182 Compound 10g is a potent CETP inhibitor that maximally inhibited cholesteryl este

183 Anacetrapib, another potent CETP inhibitor, raises HDL-C levels by approximately 138

184 derivatives was identified exhibiting potent CETP inhibition.

185 rease blood pressure, suggesting that potent CETP inhibition by itself might not lead to increased bl

186 Anacetrapib and evacetrapib, two potent CETP inhibitors, are now being tested in large clinical

187 The mechanisms by which potent CETP inhibition increases ABCA1-specific CEC and pre-bet

188 re could help in devising methods to prevent CETP function as a cardiovascular disease therapeutic.

189 efore, despite considerable initial promise, CETP inhibition provides insufficient cardiovascular ben

190 hibiting cholesteryl ester transfer protein (CETP) activity raises high-density lipoprotein cholester

191 odulates cholesteryl ester transfer protein (CETP) activity to raise high-density lipoprotein cholest

192 ition of cholesteryl ester transfer protein (CETP) activity with des-fluoro-anacetrapib, an analog of

193 s5882 in cholesteryl ester transfer protein (CETP) and rs4148217 in ATP-binding cassette subfamily G

194 ition of cholesteryl ester transfer protein (CETP) by anacetrapib reduces LDL cholesterol levels and

195 Cholesteryl ester transfer protein (CETP) catalyzes the transfer of cholesteryl ester from h

196 Cholesteryl ester transfer protein (CETP) facilitates exchange of triglycerides and choleste

197 Cholesteryl ester transfer protein (CETP) facilitates the transfer of cholesteryl ester and

198 decrease cholesteryl ester transfer protein (CETP) gene activity increase plasma HDL-C; as such, medi

199 s in the cholesteryl ester transfer protein (CETP) gene have been associated with exceptional longevi

200 s of the cholesteryl ester transfer protein (CETP) gene with coronary artery disease (CAD) with taggi

201 lations, Cholesteryl Ester Transfer Protein (CETP) inhibition and ATP-binding cassette transporter me

202 g potent cholesteryl ester transfer protein (CETP) inhibition at reduced lipophilicity was identified

203 ffect of cholesteryl ester transfer protein (CETP) inhibition on risk of ischemic events and on total

204 Cholesteryl ester transfer protein (CETP) inhibition reduces vascular event risk, but confus

205 with the cholesteryl ester transfer protein (CETP) inhibitor anacetrapib exhibit a reduction in both

206 novel cholesterol esterase transfer protein (CETP) inhibitor TA-8995 in patients with mild dyslipidae

207 rapib, a cholesteryl ester transfer protein (CETP) inhibitor, in subjects with low high-density lipop

208 rapib, a cholesteryl ester transfer protein (CETP) inhibitor, increases HDL cholesterol levels, but t

209 Cholesteryl ester transfer protein (CETP) inhibitors (JTT-705 and torcetrapib) are currently

210 high in cholesteryl ester transfer protein (CETP) inhibitors as cardioprotective agents.

211 Potent cholesteryl ester transfer protein (CETP) inhibitors have been shown to substantially increa

212 Some cholesteryl ester transfer protein (CETP) inhibitors lower low-density lipoprotein cholester

213 Cholesteryl ester transfer protein (CETP) inhibitors raise HDL-C in animals and humans and m

214 the new cholesteryl ester transfer protein (CETP) inhibitors torcetrapib, dalcetrapib, anacetrapib a

215 ledge of cholesteryl ester transfer protein (CETP) inhibitors, heart disease risk reduction, and huma

216 rials of cholesteryl ester transfer protein (CETP) inhibitors, which failed to show significant reduc

217 Cholesteryl ester transfer protein (CETP) is a serum component responsible for both choleste

218 ition of cholesteryl ester transfer protein (CETP) is considered a potential new mechanism for treatm

219 sis that cholesteryl ester transfer protein (CETP) is mainly derived from KCs and may predict KC cont

220 ition of cholesteryl ester transfer protein (CETP) leads to a marked increase in plasma levels of lar

221 Cholesteryl ester transfer protein (CETP) mediates the transfer of cholesterol esters (CE) f

222 Cholesteryl ester transfer protein (CETP) mediates the transfer of cholesteryl esters (CEs)

223 Cholesterol ester transfer protein (CETP) plays an important role in the regulation of HDL m

224 The cholesteryl ester transfer protein (CETP) plays an integral role in the metabolism of plasma

225 ition of cholesteryl ester transfer protein (CETP) raises HDL cholesterol levels and might therefore

226 levels, cholesterol ester transfer protein (CETP) rs3764261 and hepatic lipase (LIPC) rs8034802, wer

227 Cholesteryl ester transfer protein (CETP) transfers cholesteryl ester (CE) and triglyceride

228 Cholesteryl ester transfer protein (CETP) transfers cholesteryl esters from high-density lip

229 n plasma cholesteryl ester transfer protein (CETP) transports cholesteryl ester from the antiatheroge

230 Cholesteryl ester transfer protein (CETP), bactericidal/permeability inducing protein (BPI),

231 n of the cholesteryl ester transfer protein (CETP), which mediates the transfer of cholesteryl esters

232 DL levels by inhibiting CE transfer protein (CETP), which transfers CE from HDL to lower-density lipo

233 bitor of cholesteryl ester transfer protein (CETP).

234 8), C2-CFB-SKIV2L(rs429608), C3 (rs2241394), CETP (rs3764261) and ADAMTS-9 (rs6795735) were genotyped

235 rs662799, BUD13 rs11216129, BUD13 rs623908, CETP rs820299, and LIPA rs1412444 single nucleotide poly

236 rs662799, BUD13 rs11216129, BUD13 rs623908, CETP rs820299, LIPA rs1412444, alcohol consumption, smok

237 Strikingly, CETP-deficient adipocytes stored <50% of normal TG, prin

238 ficiency has led to the search for synthetic CETP inhibitors over the past 15 years.

239 e low-density lipoprotein receptor, and that CETP expression restores to normal the impaired RCT in m

240 ns, if confirmed, challenge the concept that CETP inhibition may lower CVD risk.

241 The present results demonstrate that CETP expression promotes macrophage RCT in mice, that th

242 Here, we test the hypothesis that CETP DNA sequence variants associated with higher HDL-C

243 However, the role that CETP plays in mediation of reverse cholesterol transport

244 Results showed that CETP binds to HDL via hydrophobic interactions rather th

245 Available data would suggest that CETP inhibitors will fail as lipid-altering medications

246 This preliminary report suggests that CETP V405 valine homozygosity is associated with slower

247 The CETP gene plays a critical role in lipoprotein metabolis

248 The CETP inhibitor torcetrapib was associated with a substan

249 The CETP modulator dalcetrapib raises HDL-C levels by approx

250 nd a continuous tunnel traversing across the CETP long axis appeared spontaneously.

251 Considered alone, the CETP score was associated with higher levels of HDL-C, l

252 er protein-truncating variants (PTVs) at the CETP gene were associated with plasma lipid levels and C

253 ; 1 in 975 participants carried a PTV at the CETP gene.

254 e comprised of 7 independent variants at the CETP locus and tested this score for association with HD

255 uggested a potential interaction between the CETP TaqIB polymorphism and intake of dietary fat on pla

256 We examined the association between the CETP TaqIB polymorphism and plasma HDL concentrations an

257 ary artery disease (CAD); (ii) excluding the CETP locus, there was not a predictable relationship bet

258 between bent and linear conformations in the CETP core tunnel as a consequence of the high degree of

259 f the existence of strongly bound CEs in the CETP core, very little is known about the mechanism of C

260 tudy tested whether genetic variation in the CETP gene is consistent with a protective effect of chol

261 Variants in the CETP gene region associated with increased circulating H

262 ce from genetic studies that variants in the CETP gene were associated with higher blood HDL choleste

263 iovascular events related to variants in the CETP gene, both alone and in combination with variants i

264 etabolism, and the TaqIB polymorphism of the CETP gene has been associated with elevated HDL concentr

265 METHODS AND We sequenced the exons of the CETP gene in 58 469 participants from 12 case-control st

266 al demonstrated the clinical efficacy of the CETP inhibitor anacetrapib among patients with pre-exist

267 ith des-fluoro-anacetrapib, an analog of the CETP inhibitor anacetrapib, prevents vein bypass-induced

268 ally relevant to the clinical effects of the CETP inhibitor anacetrapib.

269 We then studied the effect of the CETP inhibitor, anacetrapib, in adult female APOE*3-Leid

270 e data confirmed a significant effect of the CETP Taq1 gene on HDL concentrations and suggested a pot

271 ecent acute coronary syndrome to receive the CETP inhibitor dalcetrapib, at a dose of 600 mg daily, o

272 When combined with the HMGCR score, the CETP score was associated with the same reduction in LDL

273 eta-analysis of all 7 cohorts found that the CETP gain-of-function variant was significantly associat

274 Lipid modification) trial has shown that the CETP inhibitor anacetrapib decreased coronary heart dise

275 uman DNA sequence variants that truncate the CETP gene may provide insight into the efficacy of CETP

276 nhibitors form a complex between themselves, CETP, and HDL particles, which may interfere with the ma

277 Thus, CETP might not be essential for reverse cholesterol tran

278 Thus, CETP-D HDL has enhanced ability to promote cholesterol e

279 showed that increased cholesterol efflux to CETP-D HDL was ABCG1 dependent.

280 erates a hydrophobic environment, leading to CETP hydrophobic distal end interaction.

281 We have extended those observations to CETP.

282 d a hypothesis that the clinical response to CETP inhibitor therapy differs by ADCY9 genotype, prompt

283 Two CETP inhibitors, anacetrapib and evacetrapib, are in pha

284 Two CETP inhibitors, dalcetrapib and torcetrapib, have been

285 common SNPs and haplotype variants underlie CETP-related CAD risk, for which the common TaqIB varian

286 Various CETP inhibitors are currently being evaluated in phase I

287 increasing HDL-cholesterol (particularly via CETP inhibition) will increase AMD risk.

288 In our view, CETP inhibitors in combination with statins will be prof

289 reduction, but there is debate about whether CETP inhibition will reduce coronary heart disease risk.

290 structure, dynamics, and mechanism by which CETP transfers the neutral lipids has received tremendou

291 It predicts that while CETP inhibition would not result in an increased RCT rat

292 oprotein cholesterol (LDL-C) associated with CETP deficiency has led to the search for synthetic CETP

293 ng cardiovascular risk by raising HDL-C with CETP inhibition.

294 how various HDL-like particles interact with CETP by electron microscopy and molecular dynamics simul

295 unknown if HDL produced by interaction with CETP had pro-atherogenic or pro-inflammatory properties.

296 Among 58 469 participants with CETP gene-sequencing data available, average age was 51.

297 protein B (apoB) levels in participants with CETP scores at or above vs below the median.

298 or older from the Einstein Aging Study with CETP genotype available.

299 Treatment with CETP inhibitors, either alone or in combination with sta

300 Twelve variants within CETP demonstrated nominal association with ICH, with the