Results 1 to 10 of about 830,364 (264)

Interaction of the Xanthine Nucleotide Binding Goα Mutant with G Protein-coupled Receptors [PDF]

, 1998
We constructed a double mutant version of the α subunit of Go that was regulated by xanthine nucleotides instead of guanine nucleotides (GoαX). We investigated the interaction between GoαX and G protein-coupled receptors in vitro.
Simon, Melvin I., Yu, Bo
core   +1 more source

Both Ligand- and Cell-Specific Parameters Control Ligand Agonism in a Kinetic Model of G Protein–Coupled Receptor Signaling [PDF]

, 2007
G protein–coupled receptors (GPCRs) exist in multiple dynamic states (e.g., ligand-bound, inactive, G protein–coupled) that influence G protein activation and ultimately response generation. In quantitative models of GPCR signaling that incorporate these
Kinzer-Ursem, Tamara L., Linderman, Jennifer J.   +1 more
core   +3 more sources

Gi- and Gs-coupled GPCRs show different modes of G-protein binding. [PDF]

, 2018
More than two decades ago, the activation mechanism for the membrane-bound photoreceptor and prototypical G protein-coupled receptor (GPCR) rhodopsin was uncovered.
Altenbach, Christian, Caro, Lydia N, Dror, Ron O, Ernst, Oliver P, Hollingsworth, Scott A, Hubbell, Wayne L, Latorraca, Naomi R, Van Eps, Ned   +7 more
core   +1 more source

GPER-induced signaling is essential for the survival of breast cancer stem cells. [PDF]

, 2020
G protein-coupled estrogen receptor-1 (GPER), a member of the G protein-coupled receptor (GPCR) superfamily, mediates estrogen-induced proliferation of normal and malignant breast epithelial cells.
Chan, Yu-Tzu, Chang, Wen-Wei, Chang, Wen-Ying, Chen, Yu-Ju, Lai, Alan C-Y, Lin, Ruey-Jen, Lin, Yu-Ju, Wang, Ya-Hui, Wang, Yi-Ting, Wu, Hsin-Yi, Wu, Jen-Chine, Yu, Alice L, Yu, Jyh-Cherng   +12 more
core   +2 more sources

Molecular mechanism of Gαi activation by non-GPCR proteins with a Gα-Binding and Activating motif [PDF]

, 2017
Heterotrimeric G proteins are quintessential signalling switches activated by nucleotide exchange on Gα. Although activation is predominantly carried out by G-protein-coupled receptors (GPCRs), non-receptor guanine-nucleotide exchange factors (GEFs) have
Baillie, George S., Blanco, Francisco J., Blanco-Canosa, Juan B., Cerione, Richard A., de la Cruz-Morcillo, Miguel Angel, DiGiacomo, Vincent, Garcia-Marcos, Mikel, Ibáñez de Opakua, Alain, Leyme, Anthony, Marivin, Arthur, Merino, Nekane, Nguyen, Lien T., Parag-Sharma, Kshitij, Ramachandran, Sekar, Villate, Maider   +14 more
core   +1 more source

Designer lipid-like peptides [PDF]

, 2011
A crucial bottleneck in membrane protein studies, particularly G-protein coupled receptors, is the notorious difficulty of finding an optimal detergent that can solubilize them and maintain their stability and function. Here we report rapid production of
Baaske, Philipp, Braun, Dieter, Brown, Emily, Corin, Karolina, Duhr, Stefan, Jerabek-Willemsen, Moran, Luo, Yuan, Ravel, Deepali B., Song, Junyao, Wang, Xiaoqiang, Wienken, Christoph J., Zhang, Shuguang   +11 more
core   +1 more source

Inhibition of Subsets of G Protein-coupled Receptors by Empty Mutants of G Protein α Subunits in Go, G11, and G16 [PDF]

, 2000
We previously reported that the xanthine nucleotide binding Goα mutant, GoαX, inhibited the activation of Gi-coupled receptors. We constructed similar mutations in G11α and G16α and characterized their nucleotide binding and receptor interaction.
Gu, Lingjie, Simon, Melvin I., Yu, Bo
core   +1 more source

Functional selectivity of GPCR-directed drug action through location bias. [PDF]

, 2017
G-protein-coupled receptors (GPCRs) are increasingly recognized to operate from intracellular membranes as well as the plasma membrane. The β 2 -adrenergic GPCR can activate G s -linked cyclic AMP (G s -cAMP) signaling from endosomes.
Conti, Marco, Huang, Bo, Irannejad, Roshanak, Mika, Delphine, Pessino, Veronica, von Zastrow, Mark, Wedegaertner, Philip B.   +6 more
core   +3 more sources

The tyrosine phosphatase CD148 is an essential positive regulator of platelet activation and thrombosis [PDF]

, 2009
Platelets play a fundamental role in hemostasis and thrombosis. They are also involved in pathologic conditions resulting from blocked blood vessels, including myocardial infarction and ischemic stroke.
Abtahian, Alexandra Mazharian, Arias-Salgado, Arias-Salgado, Arthur Weiss, Asselin, Auger, Avecilla, Baker, Best, Best, Cheli, Choudhuri, Dhanjal, Dorahy, Dubois, Ezumi, Gibbins, Gibbins, Harper, Hermiston, Holsinger, Jenson Lim, Jing W. Zhu, Jocelyn M. Auger, Kalia, Kato, Klages, Kovalenko, Kralisz, Kristin N. Kornerup, Le Pera, Lin, Lin, Liu, Mangin, McCarty, McNeill, Michael G. Tomlinson, Minuz, Moarefi, Mocsai, Morton, Neena Kalia, Nonne, Obergfell, Palka, Park, Pasquet, Pasquet, Pasquet, Pearce, Poole, Quek, Senis, Snell, Somani, Sorby, Steve G. Thomas, Steve P. Watson, Stuart Ellison, Superti-Furga, Suzuki-Inoue, Suzuki-Inoue, Tarvinder Dhanjal, Tsuboi, Vandendries, Wagner, Watanabe, Watson, Wonerow, Woodside, Xu, Xu, Yamaguchi, Yan Zhao, Yotis A. Senis, Young, Zhang, Zhu   +79 more
core   +2 more sources

Ligand-guided homology modeling drives identification of novel histamine H3 receptor ligands [PDF]

, 2019
In this study, we report a ligand-guided homology modeling approach allowing the analysis of relevant binding site residue conformations and the identification of two novel histamine H3 receptor ligands with binding affinity in the nanomolar range.
Hagenow, Stefanie, Schaller, David, Stark, Holger, Wolber, Gerhard   +3 more
core   +2 more sources