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用于治疗肥胖症的二酰甘油酰基转移酶抑制剂

DGAT inhibitors for obesity.

作者信息

Matsuda Daisuke, Tomoda Hiroshi

机构信息

Kitasato University, School of Pharmacy, 5-9-1 Shirokane, Minato-ku, Tokyo 108-8641, Japan.

出版信息

Curr Opin Investig Drugs. 2007 Oct;8(10):836-41.

Abstract

Obesity is characterized by the accumulation of triacylglycerol in adipocytes. Diacylglycerol acyltransferase (DGAT) catalyzes the final reaction of triacylgycerol synthesis. Two isozymes of DGAT, DGAT1 and DGAT2, have been reported. Increased DGAT2 activity has a role in steatosis, while DGAT1 plays a role in very (V)LDL synthesis; increased plasma VLDL concentrations may promote obesity and thus DGAT1 is considered a potential therapeutic target of inhibition for obesity control. Several DGAT inhibitors of natural and synthetic origin have been reported, and their future prospect as anti-obesity drugs is discussed in this review.

摘要

肥胖的特征是脂肪细胞中三酰甘油的积累。二酰甘油酰基转移酶(DGAT)催化三酰甘油合成的最后一步反应。已报道了DGAT的两种同工酶,即DGAT1和DGAT2。DGAT2活性增加在脂肪变性中起作用,而DGAT1在极低密度脂蛋白(VLDL)合成中起作用;血浆VLDL浓度升高可能会促进肥胖,因此DGAT1被认为是控制肥胖的潜在抑制性治疗靶点。已报道了几种天然和合成来源的DGAT抑制剂,本综述讨论了它们作为抗肥胖药物的未来前景。

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