Results 131 to 140 of about 11,589 (250)

ERNEST COST action overview on the (patho)physiology of GPCRs and orphan GPCRs in the nervous system

British Journal of Pharmacology, EarlyView.
G protein‐coupled receptors (GPCRs) are a large family of cell surface receptors that play a critical role in nervous system function by transmitting signals between cells and their environment. They are involved in many, if not all, nervous system processes, and their dysfunction has been linked to various neurological disorders representing important
Necla Birgül Iyison, Clauda Abboud, Dayana Abboud, Abdulrasheed O. Abdulrahman, Ana‐Nicoleta Bondar, Julie Dam, Zafiroula Georgoussi, Jesús Giraldo, Anemari Horvat, Christos Karoussiotis, Alba Paz‐Castro, Miriam Scarpa, Hannes Schihada, Nicole Scholz, Bilge Güvenc Tuna, Nina Vardjan   +15 more
wiley   +1 more source

Progress on the development of Class A GPCR‐biased ligands

British Journal of Pharmacology, EarlyView.
Class A G protein‐coupled receptors (GPCRs) continue to garner interest for their essential roles in cell signalling and their importance as drug targets. Although numerous drugs in the clinic target these receptors, over 60% GPCRs remain unexploited. Moreover, the adverse effects triggered by the available unbiased GPCR modulators, limit their use and
Paula Morales, Magdalena M. Scharf, Marcel Bermudez, Attila Egyed, Rafael Franco, Olivia K. Hansen, Nadine Jagerovic, Jan Jakubík, György M. Keserű, Dóra Judit Kiss, Pawel Kozielewicz, Olav Larsen, Maria Majellaro, Ana Mallo‐Abreu, Gemma Navarro, Rubén Prieto‐Díaz, Mette M. Rosenkilde, Eddy Sotelo, Holger Stark, Tobias Werner, Laura M. Wingler   +20 more
wiley   +1 more source

High‐throughput screen identifies MAS9 as a novel inhibitor of the C‐type lectin receptor‐2 (CLEC‐2)–podoplanin interaction

British Journal of Pharmacology, EarlyView.
Abstract Background and Purpose The C‐type lectin‐like receptor‐2 (CLEC‐2) is a platelet receptor for the endogenous ligand podoplanin. This interaction contributes to several (patho)physiological processes, such as lymphangiogenesis, preservation of blood and lymphatic vessel integrity organ development, and tumour metastasis.
Marcin A. Sowa, Yan Wu, Jan van Groningen, Ying Di, Helma van den Hurk, Johannes A. Eble, Jonathan M. Gibbins, Ángel García, Alice Y. Pollitt   +8 more
wiley   +1 more source

Nimodipine reduces microglial activation in vitro as evidenced by morphological phenotype, phagocytic activity and high‐throughput RNA sequencing

British Journal of Pharmacology, EarlyView.
Background and Purpose Nimodipine, an L‐type voltage‐gated calcium channel blocker, is an approved cerebral vasorelaxant. We hypothesized that nimodipine attenuates the pro‐inflammatory shift in microglial phenotypes. Here, we analysed the effects of nimodipine on morphological and functional microglial phenotypes as well as their transcriptomic ...
István Pesti, Valentin Varga, Erda Qorri, Rita Frank, Diana Kata, Krisztián Vinga, Péter Archibald Szarvas, Ákos Menyhárt, Károly Gulya, Ferenc Bari, Eszter Farkas   +10 more
wiley   +1 more source

Arrestin‐independent internalization of the GLP‐1 receptor is facilitated by a GRK, clathrin, and caveolae‐dependent mechanism

The FEBS Journal, Volume 292, Issue 7, Page 1675-1695, April 2025.
The glucagon‐like peptide‐1 (GLP‐1) receptor is regulated by distinct agonist‐induced and constitutive internalization pathways. Upon agonist stimulation, GLP‐1 receptor activates Gs and Gi/o, then recruits G protein–coupled receptor kinase 2/3/5/6 to phosphorylate the intracellular loops and C‐tail of the receptor.
Ee Von Moo, Thor Christian Møller, Frederikke Astrid Sørensen, Asuka Inoue, Hans Bräuner‐Osborne   +4 more
wiley   +1 more source

PI5P4K inhibitors: promising opportunities and challenges

The FEBS Journal, EarlyView.
Developing inhibitors is like climbing a steep, challenging mountain. PI5P4K inhibitors hold significant promise for the treatment of cancer, immune disorders, and neurological diseases. However, the path to success is fraught with hurdles, and researchers are therefore required to apply their expertise to overcome critical “checkpoints.” While some ...
Koh Takeuchi, Lisa Nagase, Shun Kageyama, Hirotaka Kanoh, Masashi Oshima, Aki Ogawa‐Iio, Yoshiki Ikeda, Yuki Fujii, Sei Kondo, Natsuki Osaka, Takeshi Masuda, Tsukasa Ishihara, Yoshikazu Nakamura, Yoshihisa Hirota, Takehiko Sasaki, Toshiya Senda, Atsuo T. Sasaki   +16 more
wiley   +1 more source

Lack of TRIC‐B dysregulates cytoskeleton assembly, trapping β‐catenin at osteoblast adhesion sites

The FEBS Journal, Volume 292, Issue 8, Page 1920-1933, April 2025.
In the presence of TRIC‐B, cytosolic Ca2+ activates protein kinase C, which phosphorylates the actin‐binding proteins fascin and MARCKS, leading to proper cytoskeletal organization. This allows an appropriate β‐catenin distribution inside the cell and its translocation into the nucleus, where it stimulates the transcription of osteoblastogenic genes ...
Barbara Maria Contento, Nadia Garibaldi, Alessandra Sala, Erika Palladino, Amanda Oldani, Alessandra Carriero, Antonella Forlino, Roberta Besio   +7 more
wiley   +1 more source

Inositol phosphates and calcium entry [PDF]

Nature, 1987
openaire   +2 more sources

Succinate receptor 1 signaling mutually depends on subcellular localization and cellular metabolism

The FEBS Journal, Volume 292, Issue 8, Page 2017-2050, April 2025.
SUCNR1, activated by succinate, is a Gi‐ and Gq‐coupled receptor present at the plasma membrane and in endosomes. There are conflicting reports about the pro‐/anti‐inflammatory effects of the succinate‐SUCNR1 signaling axis, and these are likely due to localization‐dependent signaling.
Aenne‐Dorothea Liebing, Philipp Rabe, Petra Krumbholz, Christian Zieschang, Franziska Bischof, Angela Schulz, Susan Billig, Claudia Birkemeyer, Thanigaimalai Pillaiyar, Mikel Garcia‐Marcos, Robert Kraft, Claudia Stäubert   +11 more
wiley   +1 more source

A Novel Method to Determine the Carbon Isotopic Composition of Inositol Hexaphosphate (Phytate) in Soil by Gas Chromatography-Combustion-Isotope Ratio Mass Spectrometry. [PDF]

Rapid Commun Mass Spectrom
ABSTRACT Rationale Understanding the decomposition of inositol hexaphosphate (phytate), the dominant form of organic phosphorus (OP) in soil, is vital for studying phosphorus (P) cycling in terrestrial ecosystems. However, the lack of multiple stable P isotopes complicates the study of phytate dynamics under natural conditions and over long periods ...
Sarangi V, Spohn M.
europepmc   +2 more sources