Results 101 to 110 of about 589,835 (315)

Biased antagonism of a series of bicyclic CXCR2 intracellular allosteric modulators

Frontiers in Pharmacology
Targeting the human chemokine receptor (CXCR2) holds significant potential in treating inflammatory diseases and cancer. In this study, we investigate the biased properties of previously reported CXCR2 antagonists (i.e., the MVH compounds).
Brent Van Bosstraeten, Katrijn Boon, Max Van Hoof, Wim Dehaen, Martyna Szpakowska, Andy Chevigné, Dominique Schols, Steven De Jonghe, Tom Van Loy   +8 more
doaj   +1 more source

Phosphoinositides and inositol phosphates as molecular glues

FEBS Letters, EarlyView.
Inositol phosphates (IPs) and phosphoinositides (PIPs) regulate diverse eukaryotic processes. Beyond recruiting signaling proteins or acting as structural cofactors, recent studies suggest they mediate protein–protein interactions as natural molecular glues.
Aleshia Seaton‐Terry, Alexander J. Cutright, Mong Na Claire Loi, Jessica Martin, Joseph W. Gilligan, Jakub N. Kubina, Michael J. Arambula, Susanna Tanada Palmu, Daniella Zhou, Raymond D. Blind   +9 more
wiley   +1 more source

Frizzled Proteins are bona fide G Protein-Coupled Receptors

, 2009
Receptors of the Frizzled family initiate Wnt ligand-dependent signaling controlling multiple steps in organism development and highly conserved in evolution. Misactivation of the Wnt/Frizzled signaling is cancerogenic.
Silke Buestorf, Vladimir L. Katanaev
core  

Membrane cholesterol access into a G-protein-coupled receptor

Nature Communications, 2017
G-protein-coupled receptors trigger several signalling pathways and their activity was proposed to be allosteric modulated by cholesterol. Here the authors use molecular dynamics simulations and ligand binding assays to show that membrane cholesterol can
Ramon Guixà-González, José L. Albasanz, Ismael Rodriguez-Espigares, Manuel Pastor, Ferran Sanz, Maria Martí-Solano, Moutusi Manna, Hector Martinez-Seara, Peter W. Hildebrand, Mairena Martín, Jana Selent   +10 more
doaj   +1 more source

PARK(ing) time–How park deficiency affects the biological clock in a Drosophila model of Parkinson's disease

FEBS Letters, EarlyView.
Drosophila park mutants serve as a model for Parkinson's disease. We used this strain to investigate the connection between oxidative stress and the circadian clock mechanism. We showed that increased oxidative stress affects the physiology of pacemaker cells, disrupting their daily structural plasticity. Lack of rhythmic signaling from pacemaker cells
Kamila Zientara, Kinga Skoczek, Elzbieta Pyza, Milena Damulewicz   +3 more
wiley   +1 more source

Mechanistic insights into G-protein coupling with an agonist-bound G-protein-coupled receptor [PDF]

G-protein-coupled receptors (GPCRs) activate heterotrimeric G proteins by promoting guanine nucleotide exchange. Here, we investigate the coupling of G proteins with GPCRs and describe the events that ultimately lead to the ejection of GDP from its ...
Mathiesen, Jesper M., Batebi, Hossein, Lan, Baoliang, Pérez-Hernández, Guillermo, Liu, Xiangyu, Tiemann, Johanna K.S., Papasergi-Scott, Makaía M., Kamprad, Antje, Rahman, Sabrina N., Reinhardt, Franziska, Shi, Mingyu, Scheerer, Patrick, Kobilka, Brian K., Hildebrand, Peter W., Guixà-González, Ramon, Stadler, Peter F., Speck, David, Tiemann, Johanna K. S., Skiniotis, Georgios   +18 more
core   +1 more source

Biochemical pharmacology of the positive allosteric modulation of the GABAb receptor "in Vitro" and "in Vivo" [PDF]

, 2007
Allosteric modulators of G-protein coupled receptors (GPCRs) interact with binding sites on the receptor molecule that are topographically distinct from the classic orthosteric site.
Gjoni, Tina
core   +1 more source

Three phosphatase families form a community: The phosphohydrolases that act upon inositol pyrophosphates

FEBS Letters, EarlyView.
Inositol pyrophosphates are energy‐rich signaling molecules that perform critical functions in cells. Three different families of phosphatases hydrolyze the β phosphate of the inositol pyrophosphate molecules: two have narrow specificities and one is promiscuous.
Ronda J. Rolfes
wiley   +1 more source

Purification and characterization of heterologously produced cannabinoid receptor 1 and G proteins

, 2007
G protein coupled receptors form the largest group of transmembrane proteins, which are involved in signal transduction and are targeted directly or indirectly by 40-50% of the drugs in the market.
Chillakuri, Chandramouli, Chillakuri, C.
core  

C-terminal fusion of eGFP to the bradykinin B-2 receptor strongly affects down-regulation but not receptor internalization or signaling [PDF]

, 2006
A functional comparison was made between the wildtype bradykinin B, receptor (B(2)wt) and the chimera B(2)eGFP (enhanced green-fluorescent protein fused to the C-terminus of B(2)Wt), both stably expressed in HEK 293 cells.
Faussner, A., Schüssler, S., Jochum, M., Seidl, C., Kalatskaya, I.   +4 more
core   +1 more source