CD36 inhibitors reduce postprandial hypertriglyceridemia and protect against diabetic dyslipidemia and atherosclerosis.
CD36 inhibitors reduce postprandial hypertriglyceridemia and protect against diabetic dyslipidemia and atherosclerosis.
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DOI：
10.1371/journal.pone.0037633
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发表时间：
2012
期刊：
影响因子：
3.7
通讯作者：
Marguerie G
中科院分区：
文献类型：
--
作者：
Geloen A;Helin L;Geeraert B;Malaud E;Holvoet P;Marguerie G
CD36 被认为是脂质和脂肪酸受体，在代谢综合征和相关心脏事件中发挥重要作用。然而，这种清道夫受体与不同细胞和组织中膜相关分子的多效活性和多种分子关联对其作为治疗靶点的潜力提出了质疑。目前的研究表明，有可能识别出可以阻断 CD36 结合和摄取功能的低分子量化学物质。这些抑制剂能够在不同且独立的啮齿动物模型中减少动脉脂质沉积、脂肪酸肠道转运、甘油三酯和葡萄糖的血浆浓度，改善胰岛素敏感性、葡萄糖耐量并降低HbAc1的血浆浓度。在药理学剂量下观察了这些抑制剂的抗CD36活性与该清道夫受体在动脉粥样硬化和糖尿病发展中已知的病理生理活性之间的相关性。因此，CD36 可能是一个有吸引力的治疗靶点。
CD36 is recognized as a lipid and fatty acid receptor and plays an important role in the metabolic syndrome and associated cardiac events. The pleiotropic activity and the multiple molecular associations of this scavenger receptor with membrane associated molecules in different cells and tissues have however questioned its potential as a therapeutic target. The present study shows that it is possible to identify low molecular weight chemicals that can block the CD36 binding and uptake functions. These inhibitors were able to reduce arterial lipid deposition, fatty acid intestinal transit, plasma concentration of triglycerides and glucose, to improve insulin sensitivity, glucose tolerance and to reduce the plasma concentration of HbAc1 in different and independent rodent models. Correlation between the anti-CD36 activity of these inhibitors and the known pathophysiological activity of this scavenger receptor in the development of atherosclerosis and diabetes were observed at pharmacological doses. Thus, CD36 might represent an attractive therapeutic target.
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DOI：
10.1083/jcb.138.3.707
发表时间：
1997-08-11
期刊：
The Journal of cell biology
影响因子：
--
作者：
Dawson DW;Pearce SF;Zhong R;Silverstein RL;Frazier WA;Bouck NP
通讯作者：
Bouck NP
CD36依赖性途径增强了巨噬细胞和脂肪组织炎症并损害胰岛素信号传导。
影响因子：
10.8
作者：
Kennedy DJ;Kuchibhotla S;Westfall KM;Silverstein RL;Morton RE;Febbraio M
通讯作者：
Febbraio M
影响因子：
6.5
作者：
Goudriaan, JR;Dahlmans, VEH;Voshol, PJ
通讯作者：
Voshol, PJ
影响因子：
6.5
作者：
Masuda, Daisaku;Hirano, Ken-ichi;Yamashita, Shizuya
通讯作者：
Yamashita, Shizuya
影响因子：
15.9
作者：
Febbraio, M;Podrez, EA;Silverstein, RL
通讯作者：
Silverstein, RL