作为心脏病的药理目标的 (pro) renin受体
Heiko Funke-Kaiser1, Thomas Unger2
1CCR Pharma (CCRP) Therapeutics, Berlin, Germany. heiko@funke-kaiser.com.
概括
(亲素受体 ((P) RR) 除了素-血管素系统 (RAS) 之外,具有多种功能,影响心脏和脏疾病. 研究探讨小分子阻断剂 (RERBs) 向 (P) RR的治疗开发.
科学领域:
- 分子生物学分子生物学
- 心血管科学 心血管科学
- 脏科学 脏科学
背景情况:
- 该 (pro) renin受体 ((P) RR) 涉及到氨酸 - 血管新生素系统 (RAS) 和RAS独立的信号通路.
- 其多样化的分子功能有助于各种病理生理过程.
研究的目的:
- 审查 (P) RR的分子功能和病理生理学意义,特别是在心脏病和脏病中.
- 总结了对 (P) RR对抗剂的药物发现和开发工作.
主要方法:
- 关于 (P) RR分子功能的文献综述.
- 分析 (P) RR参与心脏病的发病.
- 基于小分子的氨酸/氨酸受体阻断剂 (RERB) 开发的概述.
主要成果:
- (P) RR介导多个信号传导通路,导致RAS依赖和独立的效应.
- (P) RR激活与心脏病的发展和进展有关.
- 小分子RERB正在开发,作为潜在的治疗方法.
结论:
- (P) RR是心脏病的重要分子标.
- 使用RERB的目标 (P) RR提供了一个有前途的治疗策略.
相关概念视频
Heart Failure Drugs: Inhibitors of Renin-Angiotensin System
463
The activation of the sympathetic nervous system and the renin-angiotensin-aldosterone system (RAAS) contributes to cardiac remodeling, and inhibiting the RAAS is a pharmacological target in heart failure management. As a result, neurohumoral modulation is a crucial treatment principle for managing heart failure. This approach involves using medications like ACE inhibitors (ACEIs), angiotensin receptor blockers (ARBs), β-blockers, mineralocorticoid receptor antagonists (MRAs), and neutral...
463
Antihypertensive Drugs: Direct Renin Inhibitors
679
The renin-angiotensin-aldosterone system (RAAS) is an intricate physiological pathway involving numerous enzymes and hormones, including renin, angiotensin-converting enzyme (ACE), angiotensin I and II, and aldosterone. Imbalances within this system increase the production of angiotensin II and aldosterone. Increased angiotensin II levels promote vasoconstriction and blood pressure elevation. Concurrently, higher aldosterone levels stimulate sodium and water reabsorption in the kidneys,...
679
Antihypertensive Drugs: Angiotensin-Converting Enzyme Inhibitors
689
Angiotensin-converting enzyme (ACE), a vital component of the renin-angiotensin-aldosterone system, is abundant in lung endothelial cells. ACE converts the inactive decapeptide, angiotensin I, into the active octapeptide, angiotensin II. This potent vasoconstrictor narrows blood vessels, increasing resistance to blood flow and elevating blood pressure. Angiotensin II also stimulates aldosterone production, encouraging kidney cells to reabsorb more sodium and water from urine, thereby increasing...
689
Antihypertensive Drugs: Angiotensin II Receptor Blockers
778
In the renin-angiotensin-aldosterone system, a hormone called angiotensin II plays a crucial role. It binds to the AT1 receptors in vascular smooth muscles coupled with Gq proteins. The activation of these receptors activates an enzyme called phospholipase C, which releases two molecules: inositol trisphosphate and diacylglycerol. These molecules cause a chain reaction that leads to the phosphorylation of myosin light chains and promotes interaction between actin and myosin, leading to smooth...
778
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
Heart Failure Drugs: Diuretics
420
Heart failure and kidney perfusion are interconnected in a complex way. Reduced renal perfusion and venous congestion are two significant factors that contribute to renal dysfunction in heart failure. The kidneys, primarily responsible for fluid balance in the body, are adversely affected due to compromised cardiac output and increased venous pressure. In response to reduced renal perfusion, the kidneys activate neurohumoral mechanisms to restore balance. However, these mechanisms can be...
420


