发现了DS-1150b,这是一种用于激活GLUT4转位的新型桑化合物
Masaki Meguro1, Fuminao Doi1, Tsuyoshi Soneda2
1Shinagawa R&D Center, Daiichi Sankyo Co., Ltd., 1-2-58 Hiromachi, Shinagawa-ku, Tokyo 140-8710, Japan.
Bioorganic & medicinal chemistry letters
|March 23, 2025
概括
研究人员发现了DS-1150b,这是一种新型化合物,可以增强葡萄糖载体4 (GLUT4) 转位. 这一发现通过改善骨肌肉中的葡萄糖吸收,为2型糖尿病提供了潜在的新疗法.
科学领域:
- 生物化学 生物化学
- 药理学 药理学是指药理学的学科.
- 内分泌学 在内分泌学.
背景情况:
- 葡萄糖载体4 (GLUT4) 对于胰岛素刺激的葡萄糖吸收至关重要.
- 功能障碍的GLUT4有助于导致2型糖尿病.
- 准GLUT4转位是一种新的治疗策略.
研究的目的:
- 确定增强GLUT4转位的新型化合物.
- 在临床前模型中评估已确定化合物的疗效.
主要方法:
- 使用了高通量查 (HTS) 和药物化学.
- 对DS-1150b进行了测试,以确定其在L6-myotubes中促进GLUT4转位的能力.
- 在Zucker脂肪大鼠中进行了口服葡萄糖耐受性测试 (oGTT).
主要成果:
- 鉴定出了烯化合物DS-1150b,它是一种强大的GLUT4转位增强剂.
- DS-1150b在老鼠的L6-myotubes中促进了GLUT4转位.
- DS-1150b在肥胖和糖尿病的老鼠模型中显示出降血糖效应.
结论:
- DS-1150b代表了对2型糖尿病的有前途的新型治疗剂.
- 增强GLUT4转位是管理高血糖的一个可行的策略.
- 对DS-1150b和相关化合物的进一步研究是有必要的.
相关概念视频
Secondary Active Transport
One example of how cells use the energy contained in electrochemical gradients is demonstrated by glucose transport into cells. The ion vital to this process is sodium (Na+), which is typically present in higher concentrations extracellularly than in the cytosol. Such a concentration difference is due, in part, to the action of an enzyme “pump” embedded in the cellular membrane that actively expels Na+ from a cell. Importantly, as this pump contributes to the high concentration of...
Secondary Active Transport
One example of how cells use the energy contained in electrochemical gradients is demonstrated by glucose transport into cells. The ion vital to this process is sodium (Na+), which is typically present in higher concentrations extracellularly than in the cytosol. Such a concentration difference is due, in part, to the action of an enzyme "pump" embedded in the cellular membrane that actively expels Na+ from a cell. Importantly, as this pump contributes to the high concentration of...
Glucose Transporters
Glucose transporters facilitate the transport of glucose across the cell membrane. In addition to glucose, some glucose transporters can also aid the movement of other hexoses such as fructose, mannose, and galactose.
Facilitated diffusion-glucose transporters (GLUTs) are encoded by the solute-linked carrier (SLC) family 2, subfamily A gene family, or SLC2A. The 14 GLUT protein members are distributed into three classes:
Facilitated diffusion-glucose transporters (GLUTs) are encoded by the solute-linked carrier (SLC) family 2, subfamily A gene family, or SLC2A. The 14 GLUT protein members are distributed into three classes:


