相关实验视频

Updated: May 24, 2025

HPLC-based Assay to Monitor Extracellular Nucleotide/Nucleoside Metabolism in Human Chronic Lymphocytic Leukemia Cells

HPLC-based Assay to Monitor Extracellular Nucleotide/Nucleoside Metabolism in Human Chronic Lymphocytic Leukemia Cells

Published on: July 20, 2016

细胞外ATP和结构相关的分子增强腺A_2a受体刺激的cAMP生产

Fang I Wang¹, S Jeffrey Dixon², Peter Chidiac²

¹Department of Physiology and Pharmacology, Schulich School of Medicine & Dentistry, The University of Western Ontario, London, Canada.

Cellular signalling

|March 5, 2025

概括

细胞外ATP增强了腺A2a受体 (A2aR) 信号传递,作为一个积极调节器. 这一发现扩展了ATP的ATP.

科学领域:

药理学药理学是指药理学的学科.
分子生物学分子生物学
细胞信号传输细胞信号传输

背景情况:

已知细胞外ATP增强了B类G蛋白结合受体 (GPCRs) 中的信号传递.
腺A2a受体 (A2aR) 是A类GPCR,在许多生理过程中发挥作用,是治疗点.
细胞外ATP对A2aR等A类GPCRs的影响以前没有被探索过.

研究的目的:

研究细胞外ATP对腺A2a受体 (A2aR) 信号传递的影响.
探索调节A2aR活动的分子的结构-活性关系.
为了确定ATP的调节作用是否超出了B类GPCR.

主要方法:

使用了与A2aR共传染的细胞和发光cAMP生物传感器.
在激素激发后,对循环3',5'-腺单酸盐 (cAMP) 水平进行了监测.
评估了细胞外ATP和相关分子对A2aR功能的影响.

主要成果:

细胞外ATP显著增加了腺和A2aR激动剂的功效,大约是10倍.
在没有激动剂的情况下,ATP不会激活A2aR,排除了转化为腺的代谢.
其他核酸和酸化糖模仿ATP的增强作用,而非酸化糖需要更高的度.

结论:

细胞外ATP积极调节腺A2a受体 (A2aR) 信号传递.
这代表了ATP作为A类GPCRs的积极调节器的第一个证据.
酸盐组似乎对ATP在A2aR上的观察到的调节活性至关重要.

关键词:

氨酸5'-三酸盐是一种氨酸.氨酸A(2a) 受体的受体.亚丁烯基基环酶是什么?循环的3′,5′-腺单酸盐 G蛋白结合受体的受体是G蛋白结合受体的受体.调制调制是一种调制.糖酸盐是一种糖酸盐.

更多相关视频

Use of a Hanging Weight System for Coronary Artery Occlusion in Mice

Use of a Hanging Weight System for Coronary Artery Occlusion in Mice

Published on: April 19, 2011

Pressure Controlled Ventilation to Induce Acute Lung Injury in Mice

Pressure Controlled Ventilation to Induce Acute Lung Injury in Mice

Published on: May 5, 2011

相关概念视频

ATP Energy Storage and Release

ATP Energy Storage and Release

ATP is a highly unstable molecule. Unless quickly used to perform work, ATP spontaneously dissociates into ADP and inorganic phosphate (Pi), and the free energy released during this process is lost as heat. The energy released by ATP hydrolysis is used to perform work inside the cell and depends on a strategy called energy coupling. Cells couple the exergonic reaction of ATP hydrolysis with endergonic reactions, allowing them to proceed.
One example of energy coupling using ATP involves a...

Hydrolysis of ATP

Hydrolysis of ATP

The bonds of adenosine triphosphate (ATP) can be broken through the addition of water, releasing one or two phosphate groups in an exergonic process called hydrolysis. This reaction liberates the energy in the bonds for use in the cell—for instance, to synthesize proteins from amino acids.
If one phosphate group is removed, a molecule of ADP—adenosine diphosphate—remains, along with inorganic phosphate. ADP can be further hydrolyzed to AMP—adenosine...

Adrenergic Agonists: Chemistry and Structure-Activity Relationship

Adrenergic Agonists: Chemistry and Structure-Activity Relationship

Adrenergic agonists' structure-activity relationship (SAR) determines their selectivity and efficacy. These agonists comprise a phenylethylamine moiety with an aromatic ring and an ethylamine side chain.
Aromatic ring substitutions: Substituting the aromatic ring with –OH groups at positions 3 and 4 yields catecholamines (e.g., epinephrine), which have a high affinity for adrenoceptors. Hydrogen bonding between –OH groups and receptors enhances adrenergic activity.
Separation of...

Adrenergic Agonists: Indirect-Acting Agents

Adrenergic Agonists: Indirect-Acting Agents

Indirect-acting adrenergic agonists potentiate the effects of endogenous catecholamines through different mechanisms without directly binding to adrenoceptors.
One mechanism involves depleting stored catecholamines by displacing them from synaptic vesicles. These agents, known as "displacers," are transported into vesicles at the expense of noradrenaline. Examples include amphetamine and tyramine, which lack a catechol moiety, resulting in prolonged action, improved oral...

Adrenergic Receptors: ɑ Subtype

Adrenergic Receptors: ɑ Subtype

Adrenoceptors are classified into α and ꞵ classes based on their potencies to catecholamine agonists. α-adrenoceptors show the following order of catecholamine potency:
Adrenaline ≥ Noradrenaline >> Isoprenaline
α-adrenoceptors are further divided into α1 and α2-adrenoceptors.
α1-Adrenoceptors: These receptors are located postsynaptically on the effector organs and cause constriction of smooth muscle mediated by activation of phospholipase...

Adrenergic Agonists: Direct-Acting Agents

Adrenergic Agonists: Direct-Acting Agents

Drugs that mimic the action of endogenous catecholamines like noradrenaline and adrenaline are called adrenergic agonists or sympathomimetics. Based on their mechanism of action, sympathomimetics can be classified as direct-, indirect-, or mixed-acting sympathomimetics. Direct-acting adrenergic agonists activate adrenoceptors without affecting presynaptic neurons, making them independent of neuronal catecholamine-depleting agents like reserpine and guanethidine.
These agents can be classified...