نتایج جستجو برای: gpcr

تعداد نتایج: 4523  

Journal: :Journal of alcoholism and drug dependence 2015
Takato Hiranita

Interactions between distinct receptor proteins have been assessed in vitro and in vivo. Among these studies are G-Protein-Coupled Receptor (GPCR) heteromers. GPCR heteromers form a popular area for study in molecular pharmacology and are expected to contribute valuable information to clinical needs for development of medications discovery in various neuropsychiatric diseases and symptoms. For ...

2014
Stéphanie Rosciglione Caroline Thériault Marc-Olivier Boily Marilène Paquette Christine Lavoie

The role of Gαs in G protein-coupled receptor (GPCR) signalling at the cell surface is well established. Recent evidence has revealed the presence of Gαs on endosomes and its capacity to elicit GPCR-promoted signalling from this intracellular compartment. Here, we report an unconventional role for Gαs in the endocytic sorting of GPCRs to lysosomes. Cellular depletion of Gαs specifically delays ...

Journal: :The Biochemical journal 2010
Beata Jastrzebska Yaroslav Tsybovsky Krzysztof Palczewski

Activation of GPCRs (G-protein-coupled receptors) leads to conformational changes that ultimately initiate signal transduction. Activated GPCRs transiently combine with and activate heterotrimeric G-proteins resulting in GTP replacement of GDP on the G-protein alpha subunit. Both the detailed structural changes essential for productive GDP/GTP exchange on the G-protein alpha subunit and the str...

Journal: :Nature Reviews Drug Discovery 2006

Journal: :Methods in molecular biology 2014
Miles D Thompson David E C Cole Pedro A Jose Peter Chidiac

The identification and characterization of the genes encoding G protein-coupled receptors (GPCRs) and the proteins necessary for the processes of ligand binding, GPCR activation, inactivation, and receptor trafficking to the membrane are discussed in the context of human genetic disease. In addition to functional GPCR variants, the identification of genetic disruptions affecting proteins necess...

2012
Jianshe Yan Tian Jin

Chemotaxis is crucial for many physiological processes including the recruitment of leukocytes to sites of infection, trafficking of lymphocytes in the human body, and metastasis of cancer cells. A family of small proteins, chemokines, serves as the signals, and a family of G-protein coupled receptors (GPCRs) detects chemokines and direct cell migration. One of the basic questions in chemotaxis...

Journal: :Bioinformatics 2015
Wallace K. B. Chan Hongjiu Zhang Jianyi Yang Jeffrey R. Brender Junguk Hur Arzucan Özgür Yang Zhang

MOTIVATION G protein-coupled receptors (GPCRs) are probably the most attractive drug target membrane proteins, which constitute nearly half of drug targets in the contemporary drug discovery industry. While the majority of drug discovery studies employ existing GPCR and ligand interactions to identify new compounds, there remains a shortage of specific databases with precisely annotated GPCR-li...

2017
Danielle Kamato Venkata Vijayanand Bhaskarala Nitin Mantri Tae Gyu Oh Dora Ling Reearna Janke Wenhua Zheng Peter J Little Narin Osman

G protein coupled receptor (GPCR) signalling covers three major mechanisms. GPCR agonist engagement allows for the G proteins to bind to the receptor leading to a classical downstream signalling cascade. The second mechanism is via the utilization of the β-arrestin signalling molecule and thirdly via transactivation dependent signalling. GPCRs can transactivate protein tyrosine kinase receptors...

2015
Hidetoshi Kumagai Yuichi Ikeda Yoshihiro Motozawa Mitsuhiro Fujishiro Tomohisa Okamura Keishi Fujio Hiroaki Okazaki Seitaro Nomura Norifumi Takeda Mutsuo Harada Haruhiro Toko Eiki Takimoto Hiroshi Akazawa Hiroyuki Morita Jun-ichi Suzuki Tsutomu Yamazaki Kazuhiko Yamamoto Issei Komuro Masashi Yanagisawa Nathalie Signoret

G protein-coupled receptors (GPCRs) play a critical role in many physiological systems and represent one of the largest families of signal-transducing receptors. The number of GPCRs at the cell surface regulates cellular responsiveness to their cognate ligands, and the number of GPCRs, in turn, is dynamically controlled by receptor endocytosis. Recent studies have demonstrated that GPCR endocyt...

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