Gray Susan, Feinberg Mark W, Hull Sarah, Kuo Chay T, Watanabe Masafumi, Sen-Banerjee Sucharita, DePina Ana, Haspel Richard, Jain Mukesh K
Cardiovascular Division, Brigham and Women's Hospital, Thorn Building, 20 Shattuck Street, Boston, MA 02115, USA.
J Biol Chem. 2002 Sep 13;277(37):34322-8. doi: 10.1074/jbc.M201304200. Epub 2002 Jul 3.
Resistance to the stimulatory effects of insulin on glucose utilization is a key feature of type 2 diabetes, obesity, and the metabolic syndrome. Recent studies suggest that insulin resistance is primarily caused by a defect in glucose transport. GLUT4 is the main insulin-responsive glucose transporter and is expressed predominantly in muscle and adipose tissues. Whereas GLUT4 has been shown to play a critical role in maintaining systemic glucose homeostasis, the mechanisms regulating its expression are incompletely understood. We have cloned the murine homologue of KLF15, a member of the Krüppel-like family of transcription factors. KLF15 is highly expressed in adipocytes and myocytes in vivo and is induced when 3T3-L1 preadipocytes are differentiated into adipocytes. Overexpression of KLF15 in adipose and muscle cell lines potently induces GLUT4 expression. This effect is specific to KLF15 as overexpression of two other Krüppel-like factors, KLF2/LKLF and KLF4/GKLF, did not induce GLUT4 expression. Both basal (3.3-fold, p < 0.001) and insulin-stimulated (2.4-fold, p < 0.00001) glucose uptake are increased in KLF15-overexpressing adipocytes. In co-transfection assays, KLF15 and MEF2A, a known activator of GLUT4, synergistically activates the GLUT4 promoter. Promoter deletion and mutational analyses provide evidence that this activity requires an intact KLF15-binding site proximal to the MEF2A site. Finally, co-immunoprecipitation assays show that KLF15 specifically interacts with MEF2A. These studies indicate that KLF15 is an important regulator of GLUT4 in both adipose and muscle tissues.
对胰岛素刺激葡萄糖利用作用的抵抗是2型糖尿病、肥胖症和代谢综合征的关键特征。最近的研究表明,胰岛素抵抗主要由葡萄糖转运缺陷引起。葡萄糖转运蛋白4(GLUT4)是主要的胰岛素反应性葡萄糖转运体,主要在肌肉和脂肪组织中表达。虽然GLUT4已被证明在维持全身葡萄糖稳态中起关键作用,但其表达调控机制尚未完全明确。我们克隆了Krüppel样转录因子家族成员KLF15的小鼠同源物。KLF15在体内的脂肪细胞和肌细胞中高度表达,并且在3T3-L1前脂肪细胞分化为脂肪细胞时被诱导。在脂肪和肌肉细胞系中过表达KLF15可有效诱导GLUT4表达。这种效应是KLF15特有的,因为另外两个Krüppel样因子KLF2/LKLF和KLF4/GKLF的过表达并未诱导GLUT4表达。在过表达KLF15的脂肪细胞中,基础葡萄糖摄取(增加3.3倍,p<0.001)和胰岛素刺激的葡萄糖摄取(增加2.4倍,p<0.00001)均增加。在共转染实验中,KLF15和已知的GLUT4激活剂MEF2A协同激活GLUT4启动子。启动子缺失和突变分析提供了证据,表明这种活性需要在MEF2A位点近端有完整的KLF15结合位点。最后,免疫共沉淀实验表明KLF15与MEF2A特异性相互作用。这些研究表明,KLF15是脂肪和肌肉组织中GLUT4的重要调节因子。