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GRK2 在胰岛素抵抗及相关病症中的代谢作用。

The Metabolic Role of GRK2 in Insulin Resistance and Associated Conditions.

机构信息

Dipartimento di Scienze Biomediche Avanzate, Università Federico II di Napoli, 80131 Napoli, Italy.

Dipartimento di Medicina, Chirurgia ed Odontoiatria, Università degli Studi di Salerno, 84081 Baronissi, Italy.

出版信息

Cells. 2021 Jan 15;10(1):167. doi: 10.3390/cells10010167.

Abstract

Insulin resistance (IRES) is a pathophysiological condition characterized by the reduced response to insulin of several tissues, including myocardial and skeletal muscle. IRES is associated with obesity, glucose intolerance, dyslipidemia, and hypertension, evolves toward type 2 diabetes, and increases the risk of developing cardiovascular diseases. Several studies designed to explore the mechanisms involved in IRES allowed the identification of a multitude of potential molecular targets. Among the most promising, G Protein Coupled Receptor Kinase type 2 (GRK2) appears to be a suitable one given its functional implications in many cellular processes. In this review, we will discuss the metabolic role of GRK2 in those conditions that are characterized by insulin resistance (diabetes, hypertension, heart failure), and the potentiality of its inhibition as a therapeutic strategy to revert both insulin resistance and its associated phenotypes.

摘要

胰岛素抵抗(IR)是一种病理生理状态,其特征为包括心肌和骨骼肌在内的多个组织对胰岛素的反应降低。IR 与肥胖、葡萄糖耐量受损、血脂异常和高血压相关,向 2 型糖尿病发展,并增加了发生心血管疾病的风险。一些旨在探索 IR 相关机制的研究确定了许多潜在的分子靶点。在最有前途的靶点中,G 蛋白偶联受体激酶 2(GRK2)似乎是一个合适的靶点,因为它在许多细胞过程中具有功能意义。在这篇综述中,我们将讨论 GRK2 在那些以胰岛素抵抗(糖尿病、高血压、心力衰竭)为特征的情况下的代谢作用,以及其抑制作为一种逆转胰岛素抵抗及其相关表型的治疗策略的潜力。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1452/7830135/c8ccf330537a/cells-10-00167-g001.jpg

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