Results 91 to 100 of about 792,601 (194)

Structural and Functional Analysis of a β2-Adrenergic Receptor Complex with GRK5. [PDF]

, 2017
The phosphorylation of agonist-occupied G-protein-coupled receptors (GPCRs) by GPCR kinases (GRKs) functions to turn off G-protein signaling and turn on arrestin-mediated signaling.
Adams, Christopher M., Benovic, Jeffrey L., Betz, Robin M., Chung, Ka Young, Dror, Ron O., Du, Yang, Duc, Nguyen Minh, Kobilka, Brian K., Komolov, Konstantin E., Leib, Ryan D., Patra, Dhabaleswar, Rodrigues, João P.G.L.M., Skiniotis, Georgios   +12 more
core   +2 more sources

Application of FRET- and BRET-based live-cell biosensors in deorphanization and ligand discovery studies on orphan G protein-coupled receptors

SLAS Discovery
Bioluminescence- and fluorescence-based resonance energy transfer assays have gained considerable attention in pharmacological research as high-throughput scalable tools applicable to drug discovery. To this end, G protein-coupled receptors represent the
Joanna J. Sajkowska, Choi Har Tsang, Paweł Kozielewicz   +2 more
doaj   +1 more source

Orphan G protein-coupled receptors MrgA1 and MrgC11 are distinctively activated by RF-amide-related peptides through the G{alpha}q/11 pathway [PDF]

, 2002
MrgA1 and MrgC11 belong to a recently identified family of orphan G-protein coupled receptors, called mrgs (mas-related genes). They are only expressed in a specific subset of sensory neurons that are known to detect painful stimuli. However, the precise
Anderson, David J., Dong, Xinzhong, Han, Sang-Kyou, Hwang, Jong-Ik, Simon, Melvin I., Zylka, Mark J.   +5 more
core  

The role of dimerisation in the cellular trafficking of G-protein-coupled receptors [PDF]

, 2010
The concept that G-protein-coupled receptors can exist as homomeric and/or heteromeric complexes is now well established. Despite this, how dynamic such interactions are and if this may be modulated during receptor trafficking remain topics of debate ...
Milligan, Graeme
core   +1 more source

Expression analysis of G Protein-coupled receptors in mouse macrophages [PDF]

, 2008
Background. Monocytes and macrophages express an extensive repertoire of G Protein-Coupled Receptors (GPCRs) that regulate inflammation and immunity.
Glass, Christopher K., Hume, David A., Kellie, Stuart, Lattin, Jane E., Saijo, Kaoru, Schroder, Kate, Su, Andrew I., Sweet, Matthew J., Walker, John R., Wiltshire, Tim, Zhang, Jie   +10 more
core   +3 more sources

Novel Allosteric Modulators of G Protein-coupled Receptors*

Journal of Biological Chemistry, 2015
G protein-coupled receptors (GPCRs) are allosteric proteins, because their signal transduction relies on interactions between topographically distinct, yet conformationally linked, domains.
P. Gentry, P. Sexton, A. Christopoulos
semanticscholar   +1 more source

Uncovering new disease indications for G-protein coupled receptors and their endogenous ligands

BMC Bioinformatics, 2018
Background The Open Targets Platform integrates different data sources in order to facilitate identification of potential therapeutic drug targets to treat human diseases.
Johannes M Freudenberg, Ian Dunham, Philippe Sanseau, Deepak K Rajpal   +3 more
doaj   +1 more source

Representation Learning for Class C G Protein-Coupled Receptors Classification

Molecules, 2018
G protein-coupled receptors (GPCRs) are integral cell membrane proteins of relevance for pharmacology. The complete tertiary structure including both extracellular and transmembrane domains has not been determined for any member of class C GPCRs.
Raúl Cruz-Barbosa, Erik-German Ramos-Pérez, Jesús Giraldo   +2 more
doaj   +1 more source

Computational Modeling for the Activation Cycle of G-proteins by G-protein-coupled Receptors

, 2010
In this paper, we survey five different computational modeling methods. For comparison, we use the activation cycle of G-proteins that regulate cellular signaling events downstream of G-protein-coupled receptors (GPCRs) as a driving example.
Adriana Compagnoni, Alida Palmisano, Andrew D. Howard, Andrew Phillips, Andrew Phillips, Brian K. Kobilka, Corrado Priami, Federica Ciocchetta, Federica Ciocchetta, Gabriel Ciobanu, J'er^ome Feret, Jane Hillston, Janet D. Robishaw, John W. Pinney, Jos'e M. G. Vilar, Joseph Glavy, Joël Bockaert, Kristen L. Pierce, Louis M. Luttrell, Luca Cardelli, Luca Cardelli, Luca Cardelli, Luca Cardelli, Luca Cardelli, Maciej Koutny, Maria Luisa Guerriero, Mor Peleg, Nan Hao, Ozan Kahramanogullari, Tau M. Yi, Tommy White, William M. Oldham, Yifei Bao, Yifei Bao   +33 more
core   +2 more sources

An expanding range of targets for kynurenine metabolites of tryptophan [PDF]

, 2013
The kynurenine pathway of tryptophan metabolism accounts for most of the tryptophan that is not committed to protein synthesis and includes compounds active in the nervous and immune systems.
Darlington, L. Gail, Stone, Trevor W., Stoy, Nicholas   +2 more
core   +1 more source