Results 31 to 40 of about 81,481 (258)

pdCSM-GPCR: predicting potent GPCR ligands with graph-based signatures [PDF]

, 2021
MOTIVATION: G protein-coupled receptors (GPCRs) can selectively bind to many types of ligands, ranging from light-sensitive compounds, ions, hormones, pheromones and neurotransmitters, modulating cell physiology.
Velloso, JPL, Ascher, DB, Pires, DEV
core   +1 more source

GPCR-induced YAP activation sensitizes fibroblasts to profibrotic activity of TGFβ1 - Table

, 2020
GPCR-induced YAP activation sensitizes fibroblasts to profibrotic activity of TGFβ1 ...
Magdalena Birker-Robaczewska (8447319), Oliver Nayler (302983), Maxime Boucher (6810887), Axel Klenk (8447322), Marie Schnoebelen (8447307), Diego Freti (8447310), Yasmina Bauer (147188), Rolf Studer (8447316), Katarina Zmajkovicova (8447304), John Gatfield (302973), Katalin Menyhart (2296135), Bérengère Renault (8447313)   +11 more
core   +1 more source

GPCRomics: An Approach to Discover GPCR Drug Targets [PDF]

, 2019
G protein-coupled receptors (GPCRs) are targets for ∼35% of approved drugs but only ∼15% of the ∼800 human GPCRs are currently such targets. GPCRomics, the use of unbiased, hypothesis-generating methods [e.g., RNA-sequencing (RNA-seq)], with tissues and ...
Insel, Paul A, Chinn, Amy M, Matthew W. Gorr, Gorr, Matthew W, Insel, PA, Amy M. Chinn, Gorr, MW, Sriram, Krishna, Chinn, AM, Salmerón, C, Michkov, A, Cristina Salmerón, Paul A. Insel, Sriram, K, Krishna Sriram, Alexander Michkov, Salmerón, Cristina, Shu Z. Wiley, Wiley, SZ, Wiley, Shu Z, Michkov, Alexander   +20 more
core   +1 more source

Precision-engineered Peptide and Protein Analogs: Establishing a New Discovery Platform for Potent GPCR Modulators

CHIMIA, 2021
Numerous members of the human G protein-coupled receptor (GPCR) superfamily are receptors of therapeutic interest. GPCRs are considered to be highly tractable for drug discovery, representing the targets of approximately one-third of currently licensed ...
Kalyan Bharati Akondi, Marianne Paolini-Bertrand, Oliver Hartley   +2 more
doaj   +1 more source

Similarity between class A and class B G-protein-coupled receptors exemplified through calcitonin gene-related peptide receptor modelling and mutagenesis studies [PDF]

, 2012
Modelling class B G-protein-coupled receptors (GPCRs) using class A GPCR structural templates is difficult due to lack of homology. The plant GPCR, GCR1, has homology to both class A and class B GPCRs. We have used this to generate a
Poyner, David, Reynolds, Christopher A., Hay, Debbie L., Poyner, David R, Barwell, James, Upton, Graham J.G., Poyner, David R., Reeves, Philip J., Upton, Graham J. G., Taddese, Bruck, Reeves, Philip J, Reynolds, Christopher A, Conner, Alex C., Hay, Debbie L, Conner, Alex C, Vohra, Shabana, Upton, Graham JG   +16 more
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GPCR Inhibition in Treating Lymphoma [PDF]

, 2022
G protein-coupled receptors (GPCRs) are important classes of cell surface receptors involved in multiple physiological functions. Aberrant expression, upregulation, and mutation of GPCR signaling pathways are frequent in many types of cancers, promoting ...
Raimondi M. V., Bertoni F., Giuffrida S., Spano' V., Cavalli A., Barraja P., Montalbano A., Bivacqua R., Barreca M.   +8 more
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Arrestin-3 differentially regulates platelet GPCR subsets

Platelets, 2020
The principal demonstrated role of the nonvisual arrestins in vivo is to limit G protein-coupled receptor (GPCR) signaling. Nonetheless, a direct demonstration of this fundamental ability in platelets remains lacking, despite the prominent role played by
James L. Hutchinson, Xiaojuan Zhao, Rob Hill, Stuart J. Mundell   +3 more
doaj   +1 more source

GPCR-induced YAP activation sensitizes fibroblasts to profibrotic activity of TGFβ1

, 2020
Tissue fibrosis is a pathological condition characterized by uncontrolled fibroblast activation that ultimately leads to organ failure. The TGFβ1 pathway, one of the major players in establishment of the disease phenotype, is dependent on the ...
Diego Freti, Oliver Nayler, Axel Klenk (8447322), Marie Schnoebelen (8447307), Diego Freti (8447310), Yasmina Bauer, Bérengère Renault, Rolf Studer (8447316), John Gatfield, Maxime Boucher, Katalin Menyhart (2296135), Bérengère Renault (8447313), Marie Schnoebelen, Katalin Menyhart, Magdalena Birker-Robaczewska, Magdalena Birker-Robaczewska (8447319), Oliver Nayler (302983), Maxime Boucher (6810887), Katarina Zmajkovicova, Yasmina Bauer (147188), Rolf Studer, Katarina Zmajkovicova (8447304), John Gatfield (302973), Axel Klenk   +23 more
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Below the Surface: IGF-1R Therapeutic Targeting and Its Endocytic Journey

Cells, 2019
Ligand-activated plasma membrane receptors follow pathways of endocytosis through the endosomal sorting apparatus. Receptors cluster in clathrin-coated pits that bud inwards and enter the cell as clathrin-coated vesicles.
Caitrin Crudden, Dawei Song, Sonia Cismas, Eric Trocmé, Sylvya Pasca, George A. Calin, Ada Girnita, Leonard Girnita   +7 more
doaj   +1 more source

GPCR transactivation signalling in vascular smooth muscle cells: role of NADPH oxidases and reactive oxygen species

Vascular Biology, 2019
The discovery and extension of G-protein-coupled receptor (GPCR) transactivation-dependent signalling has enormously broadened the GPCR signalling paradigm.
Raafat Mohamed, Reearna Janke, Wanru Guo, Yingnan Cao, Ying Zhou, Wenhua Zheng, Hossein Babaahmadi-Rezaei, Suowen Xu, Danielle Kamato, Peter J Little   +9 more
doaj   +1 more source