更新于：2024-11-01

Cholesterol ester

更新于：2024-11-01

基本信息

别名

胆固醇酯类

简介-

关联

项与 Cholesterol ester 相关的药物

Tiqueside

靶点

Cholesterol ester

作用机制

胆固醇酯抑制剂

在研机构-

原研机构

Pfizer Inc.

在研适应症-

非在研适应症

高胆固醇血症

最高研发阶段终止

首次获批国家/地区-

首次获批日期1800-01-20

CGP-43371

靶点

Cholesterol ester

作用机制

胆固醇酯抑制剂

在研机构-

原研机构

Novartis Pharma AG

在研适应症-

非在研适应症

动脉粥样硬化 [+2]

最高研发阶段终止

首次获批国家/地区-

首次获批日期1800-01-20

CVT-1

靶点

Cholesterol ester

作用机制

胆固醇酯抑制剂

在研机构-

原研机构

Gilead Sciences, Inc.

在研适应症-

非在研适应症

高胆固醇血症

最高研发阶段终止

首次获批国家/地区-

首次获批日期1800-01-20

100 项与 Cholesterol ester 相关的临床结果

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100 项与 Cholesterol ester 相关的转化医学

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0 项与 Cholesterol ester 相关的专利（医药）

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114

项与 Cholesterol ester 相关的文献（医药）

2023-12-01·International Journal of Biological Macromolecules

Targeting structural flexibility in low density lipoprotein by integrating cryo-electron microscopy and high-speed atomic force microscopy

Article

作者: Peters, Judith ; Bezault, Armel ; Kandiah, Eaazhisai ; Gutsche, Irina ; Prassl, Ruth ; Hoerl, Gerd ; Leitinger, Gerd ; Schachner-Nedherer, Anna-Laurence ; Hinterdorfer, Peter ; Stainer, Sarah ; Traore, Daouda A K ; Cisse, Aline ; Kornmueller, Karin ; Desfosses, Ambroise

Low-density lipoprotein (LDL) plays a crucial role in cholesterol metabolism. Responsible for cholesterol transport from the liver to the organs, LDL accumulation in the arteries is a primary cause of cardiovascular diseases, such as atherosclerosis. This work focuses on the fundamental question of the LDL molecular structure, as well as the topology and molecular motions of apolipoprotein B-100 (apo B-100), which is addressed by single-particle cryo-electron microscopy (cryo-EM) and high-speed atomic force microscopy (HS-AFM). Our results suggest a revised model of the LDL core organization with respect to the cholesterol ester (CE) arrangement. In addition, a high-density region close to the flattened poles could be identified, likely enriched in free cholesterol. The most remarkable new details are two protrusions on the LDL surface, attributed to the protein apo B-100. HS-AFM adds the dimension of time and reveals for the first time a highly dynamic direct description of LDL, where we could follow large domain fluctuations of the protrusions in real time. To tackle the inherent flexibility and heterogeneity of LDL, the cryo-EM maps are further assessed by 3D variability analysis. Our study gives a detailed explanation how to approach the intrinsic flexibility of a complex system comprising lipids and protein.

2023-06-01·Oncology letters

Evaluation of sterol‑o‑acyl transferase 1 and cholesterol ester levels in plasma, peritoneal fluid and tumor tissue of patients with endometrial cancer: A pilot study.

Article

作者: Wilson, Teresa ; Braundmeier-Fleming, Andrea ; Groesch, Kathleen ; Ayyagari, Vijayalakshmi N ; Li, Miao ; Brard, Laurent ; Pasman, Zvi ; Diaz-Sylvester, Paula ; Shah, Ejaz M

Endometrial cancer (EC) is the most prevalent gynecological malignancy. Abnormal accumulation of sterol-O-acyl transferase 1 (SOAT1) and SOAT1-mediated cholesterol ester (CE) contributes to cancer progression in various malignancies, including ovarian cancer. Therefore, it was hypothesized that similar molecular changes may occur in EC. The present study aimed to evaluate the diagnostic and/or prognostic potential of SOAT1 and CE in EC by: i) Determining SOAT1 and CE levels in plasma, peritoneal fluid and endometrial tissue from patients with EC and control subjects; ii) performing receiver operating characteristic curve analysis to determine diagnostic performance; iii) comparing SOAT1 and CE expression to that of the tumor proliferation marker Ki67; and iv) assessing the association between SOAT1 expression and survival. Enzyme-linked immunosorbent assay was used to determine the levels of SOAT1 protein in tissue, plasma and peritoneal fluid. The mRNA and protein expression levels of SOAT1 and Ki67 in tissues were detected by reverse transcription-quantitative polymerase chain reaction and immunohistochemistry, respectively. CE levels were determined colorimetrically in plasma and peritoneal fluid. SOAT1-associated survival data from the cBioPortal cancer genomics database were used to assess prognostic relevance. The results revealed that SOAT1 and CE levels were significantly elevated in tumor tissue and peritoneal fluid samples collected from the EC group. By contrast, the plasma levels of SOAT1 and CE in the EC and control groups were similar. Significant positive associations between CE and SOAT1, SOAT1/CE and Ki67, and SOAT1/CE and poor overall survival in patients with EC suggested that SOAT1/CE may be associated with malignancy, aggressiveness and poor prognosis. In conclusion, SOAT1 and CE may serve as potential biomarkers for prognosis and target-specific treatment of EC.

2023-03-01·Current Atherosclerosis Reports

Benefit of Combination Ezetimibe/Simvastatin Among High-Risk Populations: Lessons from the IMPROVE-IT Trial

Review

作者: Oliver, Walter ; Giugliano, Robert P

PURPOSE OF REVIEWThe Improved Reduction of Outcomes: Vytorin Efficacy International Trial (IMPROVE-IT) demonstrated the clinical benefit of the combination of ezetimibe-simvastatin compared to placebo-simvastatin following acute coronary syndrome (ACS). This review highlights key findings from this study with particular attention to the practice-changing impact on guidelines for low-density lipoprotein cholesterol (LDL-C) reduction after ACS, especially among high-risk populations.RECENT FINDINGSConsistent reductions in LDL-C have been reported with newer lipid-lowering therapies (proprotein convertase subtilisin/kexin type 9 inhibitors, cholesterol ester transfer proteins, bempedoic acid) in combination with statin in high-risk subgroups. Since high-risk subgroups remain a focus of guidelines, exploration of high-risk subgroups can help define the optimal use of new therapies. Ezetimibe reduced the LDL-C by 16.7 mg/dL compared to placebo at 1 year, resulting in a significant reduction in the primary composite endpoint (absolute risk difference 2.0%; relative risk difference 6.4%, hazard ratio, 0.936; 95% confidence interval, 0.89 to 0.99; P = 0.016). The benefits achieved with ezetimibe in both LDL-C reduction and the primary clinical composite across 10 pre-specified high-risk subgroups, including the elderly; women; patients with diabetes, prior coronary artery bypass graft, history of stroke, polyvascular disease, low baseline LDL-C, renal dysfunction, prior heart failure, and an elevated TIMI risk score for secondary prevention, were similar or greater than in the corresponding non-high-risk subgroups. Safety events were similar between ezetimibe and placebo across the high-risk subgroups. These data support the addition of ezetimibe to statin therapy in high-risk patients who require additional therapy to lower the LDL-C post-ACS.