作为一个有前途的药物标,酸丁胆特异性脂酶C是一种有前途的药物标
Chatchakorn Eurtivong1, Euphemia Leung2, Nabangshu Sharma3,4
1Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Mahidol University, 447 Si Ayutthaya Road, Ratchathewi, Bangkok 10400, Thailand.
Molecules (Basel, Switzerland)
|August 12, 2023
概括
酸丁胆特异性脂酶C (PC-PLC) 酶与癌症等疾病有关. 这篇评论探讨了PC-PLC.
科学领域:
- 生物化学 生化学
- 酶学 是一种酶学.
- 分子生物学分子生物学
背景情况:
- 酸丁胆特异性脂酶C (PC-PLC) 产生关键的信号分子酸丁胆和二甲甘油 (DAG).
- PC-PLC与包括癌症,动脉样硬化,炎症和神经元细胞死亡在内的病理状况有关.
- 在蛋白质水平上对PC-PLC的研究是有限的,没有人类基因被确定,只有一种 prokaryotic 结构可用.
研究的目的:
- 审查PC-PLC的病理作用.
- 为了突出开发PC-PLC抑制剂的进展.
- 确定PC-PLC抑制剂开发的未来挑战.
主要方法:
- 关于PC-PLC病理影响的文献综述.
- 分析当前的PC-PLC抑制剂类别及其药物化学.
- 对PC-PLC抑制剂的细胞和体内证据的评估.
主要成果:
- PC-PLC活动表明,人类的功能相当于其细菌对应物.
- 存在各种类型的抑制剂,包括2 - 氨基胺酸,桑酸和脂类类似物.
- 缺乏细胞和体内数据阻碍了许多抑制剂的临床进展.
结论:
- 由于其在各种疾病中的作用,PC-PLC是一个重要的治疗点.
- 需要进一步的研究来验证PC-PLC抑制剂在细胞和体内模型中的疗效.
- 弥合药物化学和临床应用之间的差距对于开发有效的PC-PLC向疗法至关重要.
相关概念视频
Synthesis of Phosphatidylcholine in the ER Membrane
3.2K
The ER synthesizes lipids for building cell membranes and performing cellular functions such as energy storage and signaling. The lipid synthesis machinery embedded in the ER membrane primarily collects all reactants from the cytosol. Following synthesis, the secretory pathway and the ER contact sites distribute these lipids to other cellular organelles. Additionally, the energy-rich triacylglycerides are transported from the ER via lipid droplets.
The major components of all eukaryotic cell...
The major components of all eukaryotic cell...
3.2K
Phosphoinositides and PIPs
8.6K
Phosphoinositides are a group of phospholipids containing a glycerol backbone with two fatty acid chains and a phosphate attached to a myoinositol sugar ring. The inositol head group extends into the cytoplasm, where it is modified by adding phosphate groups to form phosphatidylinositol phosphates or PIPs.
Different phosphoinositides are synthesized and recruited on the cytosolic face of the plasma membrane. The localization of specific phosphoinositides concentrated in separate membrane...
Different phosphoinositides are synthesized and recruited on the cytosolic face of the plasma membrane. The localization of specific phosphoinositides concentrated in separate membrane...
8.6K
IP3/DAG Signaling Pathway
12.2K
Membrane lipids such as phosphatidylinositol (PI) are precursors for several membrane-bound and soluble second messengers. Specific kinases phosphorylate PI and produce phosphorylated inositol phospholipids. One such inositol phospholipids are the phosphatidylinositol-4,5 bisphosphate [PI(4,5)P2], present in the inner half of the lipid bilayer. Upon ligand binding, GPCR stimulates Gq proteins to turn on phospholipase Cꞵ. Activated phospholipase Cꞵ cleaves PI(4,5)P2 and...
12.2K
Asymmetric Lipid Bilayer
7.3K
Biological membranes show uneven distribution of different types of lipids in the inner and outer layers, resulting in transverse asymmetric membranes. The treatment of the erythrocyte membrane with the enzyme phospholipase confirmed the asymmetric nature of the lipid bilayer. The enzyme hydrolyzes lipids into fatty acids and hydrophilic groups. The phospholipase acts only on the outer layer of the membrane, while the inner layer remains intact. The phospholipase treatment resulted in 80%...
7.3K
Overview of Fatty Acid Metabolism
30.8K
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...
30.8K
Transducer Mechanism: Enzyme-Linked Receptors
2.5K
Enzyme-linked receptors are cell-surface receptors acting as an enzyme or associating with an enzyme intracellularly. They make excellent drug targets. Drugs can bind to the extracellular ligand-binding domain or directly affect their enzymatic domain and alter their activity.
Major types that are helpful drug targets include:
Major types that are helpful drug targets include:
2.5K


