Glycerol-3-phosphate acyltransferase (GPAT) is the rate-limiting enzyme in the de novo pathway of glycerolipid synthesis. It catalyzes the conversion of glycerol-3-phosphate and long-chain acyl-CoA to lysophosphatidic acid. In mammals, four isoforms of GPATs have been identified based on subcellular localization, substrate preferences, and NEM sensitivity, and they have been classified into two groups, one including GPAT1 and GPAT2, which are localized in the mitochondrial outer membrane, and the other including GPAT3 and GPAT4, which are localized in the endoplasmic reticulum membrane. GPATs play a pivotal role in the regulation of triglyceride and phospholipid synthesis. Through gain-of-function and loss-of-function experiments, it has been confirmed that GPATs play a critical role in the development of obesity, hepatic steatosis, and insulin resistance. In line with this, the role of GPATs in metabolism was supported by studies using a GPAT inhibitor, FSG67. Additionally, the functional characteristics of GPATs and the relation between three isoforms (GPAT1, 3, and 4) and insulin resistance has been described in this review.

3-磷酸​​甘油酰基转移酶（GPAT）是甘油脂合成从头途径中的限速酶。它催化3-磷酸甘油和长链酰基辅酶A转化为溶血磷脂酸。在哺乳动物中，已根据亚细胞定位，底物偏好和NEM敏感性鉴定出GPAT的四种同工型，并将它们分为两组，一组包括GPAT1和GPAT2，它们位于线粒体外膜，而另一组包括GPAT1和GPAT2。 GPAT3和GPAT4，位于内质网膜中。GPAT在甘油三酸酯和磷脂合成的调节中起关键作用。通过功能获得和功能丧失实验，已证实GPAT在肥胖，肝脂肪变性，和胰岛素抵抗。与此相符，使用GPAT抑制剂FSG67的研究支持了GPAT在代谢中的作用。此外，本篇综述还描述了GPAT的功能特征以及三种同工型（GPAT1、3和4）与胰岛素抵抗之间的关系。