甲状腺激素和甲状腺激素相关的类受体的G蛋白结合受体
H Jüppner1, A B Abou-Samra, M Freeman
1Endocrine Unit, Massachusetts General Hospital, Boston 02114.
概括
研究人员克隆了一种新型的副甲状腺激素-副甲状腺激素相关 (PTH-PTHrP) 受体,证明其对两种配体的同等结合亲和力及其在新的调节激素受体家族中的作用.
科学领域:
- 分子内分泌学分子内分泌学
- 接收器生物学 接收器生物学
- 的恒温稳定 的恒温稳定.
背景情况:
- 副甲状腺激素 (PTH) 和副甲状腺激素相关的 (PTHrP) 是的关键调节者.
- 了解它们的受体相互作用对于代谢研究至关重要.
研究的目的:
- 克隆和描述编码PTH-PTHrP受体的互补DNA (cDNA).
- 调查新型受体的结合亲和力和信号传递能力.
主要方法:
- 克隆受体cDNA使用COS-7表达和鱼脏细胞cDNA库.
- 评估对PTH和PTHrP的联结亲和力.
- 通过PTH和PTHrP测量腺酸环酶刺激.
主要成果:
- 成功克隆了一个具有7个跨膜域的585氨基酸受体.
- 表达的受体对PTH和PTHrP表现出相同的结合亲和力.
- 这两种配体都同样刺激了腺酸环酶活性.
结论:
- 克隆受体结合并对PTH和PTHrP进行反应.
- 结构同质性表明一种新的G蛋白连接受体家族用于调节激素,包括素受体.
相关概念视频
G-protein Coupled Receptors
G-protein coupled receptors are ligand binding receptors that indirectly affect changes in the cell. The actual receptor is a single polypeptide that transverses the cell membrane seven times creating intracellular and extracellular loops. The extracellular loops create a ligand specific pocket which binds to neurotransmitters or hormones. The intracellular loops holds onto the G-protein.
G-protein Coupled Receptors
G-protein coupled receptors are ligand binding receptors that indirectly affect changes in the cell. The actual receptor is a single polypeptide that transverses the cell membrane seven times creating intracellular and extracellular loops. The extracellular loops create a ligand specific pocket which binds to neurotransmitters or hormones. The intracellular loops holds onto the G-protein.
G Protein-coupled Receptors
G Protein-Coupled Receptors or GPCRs are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to sensory stimuli such as light, odors, hormones, cytokines, or neurotransmitters.
GPCRs are also called heptahelical, 7TM, or serpentine receptors, and consist of seven (H1-H7) transmembrane alpha-helices that span the bilayer to form a cylindrical core. The transmembrane helices are connected by three extracellular loops and three...
GPCRs are also called heptahelical, 7TM, or serpentine receptors, and consist of seven (H1-H7) transmembrane alpha-helices that span the bilayer to form a cylindrical core. The transmembrane helices are connected by three extracellular loops and three...
GPCRs Regulate Adenylyl Cylase Activity
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 cells.
Two...
Two...
G Protein-coupled Receptors
G Protein-Coupled Receptors or GPCRs are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to sensory stimuli such as light, odors, hormones, cytokines, or neurotransmitters.
GPCRs are also called heptahelical, 7TM, or serpentine receptors, and consist of seven (H1-H7) transmembrane alpha-helices that span the bilayer to form a cylindrical core. The transmembrane helices are connected by three extracellular loops and three...
GPCRs are also called heptahelical, 7TM, or serpentine receptors, and consist of seven (H1-H7) transmembrane alpha-helices that span the bilayer to form a cylindrical core. The transmembrane helices are connected by three extracellular loops and three...
Transducer Mechanism: G Protein–Coupled Receptors
G Protein–Coupled Receptors (GPCRs) are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to various stimuli. GPCRs regulate critical physiological pathways and are excellent drug targets for treating diseases such as diabetes, cancer, obesity, depression, or Alzheimer's. Nearly 35% of approved drugs implement their therapeutic effects by selectively interacting with specific GPCRs.
GPCRs are also called heptahelical, 7TM, or...
GPCRs are also called heptahelical, 7TM, or...


