GPCR

The Fine Research of the Activation Mechanism of GPCR Family C

C族G蛋白偶联受体激活机制的精细研究

Study of CCK receptor polymorphism may reveal some universal rules in GPCR superfamily .

研究CCK受体的多态性可能反映G蛋白偶联受体家族的一些普遍规律。

In the last 12 years more than a dozen GPCR crystal structures have been resolved .

在近12年内，12种以上的gpcr的结晶化技术已被解决。

This thesis contributes to the exploration of GPCR – Ligand docking with high accuracy .

本文为GPCR―配体高精度计算对接进行了有意的探索。

Present study proves that PKD is mainly regulated by the G protein coupled receptor ( GPCR ) .

目前研究证明，PKD在细胞内的激活主要受G蛋白偶联受体（GPCR）调控。

GPCR ( G-protein coupled receptors ) superfamily is one of the most important drug targets in human body .

G蛋白偶联受体（GPCR）是人体内一类重要的药物作用靶标。

Among the 50 kinds of most popular drugs approved recently , 20 % of them belonged to GPCR .

在当今前50种最畅销的上市药物中，20%属于G蛋白受体相关药物。

CCK receptor belongs to G-protein-coupled receptor ( GPCR ) superfamily .

CCK受体属于G蛋白偶联受体。

This was a major achievement , but the structure was relatively low resolution and could not shed light on the details of GPCR activation .

这是一项了不起的成就，但得到的结构分辨率很低，并不能阐明gpcr活化的细节。

Modulatory role of lipid rafts on GPCR signaling

脂筏在G蛋白偶联受体信号转导中的调控作用

These breakthroughs have opened the way to not only a detailed dissection of the mechanism of GPCR function but also to structure-based drug design .

这些重大突破不仅提供了gpcr起作用的机制的详细解剖，也提供了基于结构的药物设计的信息。

Conclusion : IRAS might not be a GPCR and ERK might be a signal transduction molecule of IRAS .

结论：IRAS不与G蛋白偶联，ERK可能是IRAS偶联的信号分子之一。

Receptor tyrosine kinases ( RTK ), G protein-coupled receptors ( GPCR ) and ion channel receptors are main cell surface receptors .

酪氨酸激酶型受体、G蛋白偶联受体和离子通道型受体是细胞表面三类主要受体。

Because membrane protein is hard to be separated and purified so far , there are not so many crystal structures of GPCR protein in PDB .

GPCR家族的蛋白均为跨膜结构蛋白，由于膜蛋白分离与纯化在目前情况下很困难，因此，现在PDB数据库中已知的晶体结构并不多。

Allosteric communication network of coupling residues in GPCR class A rhodopsin like family A fundamental goal in signal transduction study is to understand allosteric communication .

视紫质样GPCR中偶联氨基酸的变构通讯网络对变构通讯的理解是研究细胞信号转导的一个基本目标。

Another major breakthrough came with a structure of the GPCR in its active state , a state which had previously thought to be too unstable to be isolated .

另一项重大突破是获得了gpcr活化状态时的结构，这之前曾被认为是太不稳定而不能分离出来。

Background β - adrenergic receptor ( beta-AR ) is an important member of the G protein-coupled receptor ( GPCR ) family .

研究背景：β肾上腺素能受体（β-AR）是G蛋白偶联受体（GPCR）家族的重要成员。

RGS proteins accelerate the deactivation of G proteins to reduce GPCR signaling ; however , some also have an effector function and transmit signals .

一般来说RGS可加速G蛋白失活进而终止GPCR信号传导，但也有些RGS同时具有效应分子和信号传递功能。

When a GPCR binds a ligand , the extracellular signal is transmitted to the cell which will cause cell response and regulate the life activities of cell .

GPCR与配体相结合时，将细胞外的信号传递到细胞内，从而引起一系列细胞反应。

The new progress in the research on the constitutive activity and inverse agonists of GPCR displays an important significance in application of the receptor theory , and practical values for drug development .

愈来愈多的实验表明，GPCR组成性活性及反向激动剂的研究具有广阔和实际的应用前景，对其进行深入研究在受体学说领域和药物研发过程中具有重要理论意义。

G protein-coupled receptor kinases ( GRKs ) are known as a large family of serine / threonine kinase that regulate GPCR signaling .

G蛋白偶联受体激酶（G-protein-coupledreceptorkinases，GRKs）是调节GPCR的一类关键的丝/苏氨酸激酶。

Regulator of G-protein-signaling ( RGS ) proteins play a down-regulation effects in the signal transduction of G-protein-coupled receptor ( GPCR ) .

G蛋白信号转导调节（RGS）蛋白在G蛋白信号转导中起负性调节作用。

AVP 4-8 did not show any influence on cAMP production . CONCLUSION : AVP 4-8 stimulated signal transduction via a GPCR and a branching pathway in rat hippocampus .

与AVP不同，（4－8）不影响cAMP水平.结论：精加压素片段（4－8）通过未知GPCR和G0介导一分支信号途径。

Agonists for GPCR can regulate the expression level of GRK , and the abnormal expression of GRK in vivo can markedly influence physiological functions of organs and tissues .

GRK的表达水平可被GPCR的激动剂调节。GRK在体内的异常表达可以严重地影响器官和组织的功能。

An improved bipartite graph learning approach was developed to predict drug-target interaction network for four classes of enzymes , ion channels , G-protein coupled receptors ( GPCR ) and nuclear receptors .

根据已知的四类蛋白质家族（酶，GPCR，离子通道和核受体）以及与之相互作用的药物数据，提出了一种基于改进的二分图学习方法来预测药物靶标相互作用网络。

AIM : To predict the allosteric communication network formed by a set of amino acids coupled with Leu-125 in G protein coupled receptor ( GPCR ) class A rhodopsin like family .

目的：预测视紫质样GPCR中由Leu125等氨基酸组成的变构通讯网络。

The histamine H3 receptor ( H3R ) is a G-protein-coupled receptor ( GPCR ), which predominantly expressed in the central nervous system ( CNS ) .

H3受体是组胺受体家族中的一员，是一种G蛋白偶联受体，主要分布在中枢神经系统。

Available data indicate that the phosphorylation of RKIP by PKC stimulates both the Raf-1 / MEK / ERK1,2 and GPCR pathways .

有数据表明RKIP被PKC磷酸化后能同时激活Raf-1/MEK/ERK1,2和GPCR信号通路。

When the researchers introduced its associated membrane-impermeant fluorogen , it bound to the FAP-tagged GPCR on the cell surface , emitting a bright fluorescent glow .

当研究人员引入与其相应的膜不通透性荧光团并与细胞膜上有荧光团激活蛋白质标签的G-蛋白偶联受体结合时，发出明亮的荧光；

In particular , several classes of proteins such as enzymes , ion channels , G-protein-coupled receptors ( GPCR ) and nuclear receptors represent the vast majority of current drug targets for new drug development .

尤其在新药研发的过程中，几类蛋白诸如酶，离子通道，G蛋白偶联受体（GPCR）和核受体代表了当前药物靶标的绝大多数。