自由脂肪酸受体FFA4的逆激素作用控制了脂肪生成和成熟脂肪细胞的功能
W S Alshammari1, E M Duncan1, L Vita1
1Centre for Translational Pharmacology, School of Molecular Bioscience, University of Glasgow, Glasgow, UK.
Cellular signalling
|March 8, 2025
概括
对FFA4受体的药理向会影响脂肪细胞的功能. 一种FFA4抗剂抑制了脂肪生成和葡萄糖吸收,同时增强了脂解,表明对代谢障碍的治疗潜力.
科学领域:
- 代谢障碍 代谢障碍 代谢障碍
- 脂肪细胞生物学 脂肪细胞生物学
- G蛋白结合受体 (GPCR) 信号传递
背景情况:
- 脂肪细胞功能障碍是代谢障碍的核心,需要药理干预.
- 自由脂肪酸受体4 (FFA4) 是由自由脂肪酸 (FFAs) 激活的GPCR,并调节脂肪细胞功能.
- 了解FFA4信号,特别是涉及脂肪细胞衍生的FFAs,对于治疗开发至关重要.
研究的目的:
- 研究FFA4药理性激素和对抗作用对人类和小鼠脂肪细胞中的脂肪生成,脂解和葡萄糖吸收的影响.
- 阐明FFA4调节脂肪细胞功能背后的机制.
- 评估针对FFA4的治疗方法在治疗脂肪细胞功能障碍方面的潜力.
主要方法:
- 利用人类和小鼠脂肪细胞细胞模型.
- 药理学FFA4激动剂 (TUG-891) 和抗剂 (AH7614) 的使用.
- 评估了对脂肪生成,异上腺素刺激的脂解和葡萄糖吸收的影响.
主要成果:
- FFA4对手AH7614作为反向激动剂,抑制脂肪生成,抑制葡萄糖吸收,并增强脂解.
- FFA4激动剂TUG-891对脂肪生成和脂解产生了适度的影响,对葡萄糖吸收没有影响.
- AH7614的作用与在脂肪生成过程中抑制自身隐性FFA4反循环以及在脂解过程中可能调节连接体独立信号相关.
结论:
- FFA4信号传递在脂肪细胞功能中起着复杂的作用,对激进和对抗有不同的反应.
- AH7614的反向激动性表明一种增强脂解和抑制脂肪生成的机制.
- 向FFA4为具有脂肪细胞功能障碍的代谢障碍提供了潜在的治疗策略.
更多相关视频
08:34Mechanism of Regulation of Adipocyte Numbers in Adult Organisms Through Differentiation and Apoptosis Homeostasis
Published on: June 3, 2016
14.9K
06:08Author Spotlight: Semi-Automated Isolation of the Stromal Vascular Fraction from Murine White Adipose Tissue Using a Tissue Dissociator
Published on: May 19, 2023
2.0K
相关概念视频
Overview of Fatty Acid Metabolism
30.1K
Lipids also are sources of energy that power cellular processes. Like carbohydrates, lipids are composed of carbon, hydrogen, and oxygen, but these atoms are arranged differently. Most lipids are nonpolar and hydrophobic. Major types include fats and oils, waxes, phospholipids, and steroids.
Fatty acids are catabolized in a process called beta-oxidation, which takes place in the matrix of the mitochondria and converts their fatty acid chains into two-carbon units of acetyl groups. The acetyl...
Fatty acids are catabolized in a process called beta-oxidation, which takes place in the matrix of the mitochondria and converts their fatty acid chains into two-carbon units of acetyl groups. The acetyl...
30.1K
Fats as Energy Storage Molecules
24.7K
Triglycerides are a form of long-term energy storage molecules. They are made of glycerol and three fatty acids. To obtain energy from fat, triglycerides must first be broken down by hydrolysis into their two principal components, fatty acids and glycerol. This process, called lipolysis, takes place in the cytoplasm. The resulting fatty acids are oxidized by β-oxidation into acetyl-CoA, which is used by the Krebs cycle. The glycerol that is released from triglycerides after lipolysis...
24.7K
GPCRs Regulate Adenylyl Cylase Activity
5.1K
Some GPCRs transmit signals through adenylyl cyclase (AC), a transmembrane enzyme. AC helps synthesize second messenger cyclic adenosine monophosphate (cAMP). AC catalyzes cyclization reaction and converts ATP to cAMP by releasing a pyrophosphate. The pyrophosphate is further hydrolyzed to phosphate by the enzyme pyrophosphatase, which drives cAMP synthesis to completion. However, cAMP is rapidly degraded to 5′ AMP by the enzymes phosphodiesterase (PDE), preventing overstimulation of...
5.1K
TGF - β Signaling Pathway
7.2K
The TGF-β signaling pathway regulates cell growth, differentiation, adhesion, motility, and development. TGF-β ligands that induce TGF-β signaling are synthesized in their latent form. Several proteases or cell surface receptors such as integrins act upon the latent form, releasing the active ligand. There are three types of mammalian TGF-βs: (TGF-β1, TGF-β2, and TGF-β3) that bind as homodimers or heterodimers to TGF-β receptors. The TGF-β receptors...
7.2K
Master Transcription Regulators
6.8K
Master transcription regulators are regulatory proteins that are predominantly responsible for regulating the expression of multiple genes. Often these genes work in concert to drive a complex process. Activation of a master transcription regulator can lead to a cascade of transcriptional activation necessary for that outcome. These regulators can directly bind to the regulatory sequences of the various genes involved, or they can indirectly regulate transcription by binding to regulatory...
6.8K
Adrenergic Receptors: β Subtype
1.5K
β-adrenoceptors have varied sensitivities towards adrenaline, noradrenaline, and isoprenaline. The order of agonist potency is as follows:
Isoprenaline > Adrenaline > Noradrenaline
Neurotransmitter binding to these receptors causes activation of adenylyl cyclase resulting in increased concentrations of cAMP and modulation of calcium ion channels within the cell. They are further classified into β1, β2, and β3 subtypes.
β1-adrenoceptors: β1-adrenoceptors...
Isoprenaline > Adrenaline > Noradrenaline
Neurotransmitter binding to these receptors causes activation of adenylyl cyclase resulting in increased concentrations of cAMP and modulation of calcium ion channels within the cell. They are further classified into β1, β2, and β3 subtypes.
β1-adrenoceptors: β1-adrenoceptors...
1.5K
