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Year Number of Results
1990 1
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17,868 results

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Page 1
Structure and dynamics of GPCR signaling complexes.
Hilger D, Masureel M, Kobilka BK. Hilger D, et al. Nat Struct Mol Biol. 2018 Jan;25(1):4-12. doi: 10.1038/s41594-017-0011-7. Epub 2018 Jan 8. Nat Struct Mol Biol. 2018. PMID: 29323277 Free PMC article. Review.
Recent breakthroughs in the structural determination of GPCRs and GPCR-transducer complexes represent important steps toward deciphering GPCR signal transduction at a molecular level. ...Here, we summarize current insights into the structural plasticity of GPCR …
Recent breakthroughs in the structural determination of GPCRs and GPCR-transducer complexes represent important steps toward decipher …
New Insights into Modes of GPCR Activation.
Wang W, Qiao Y, Li Z. Wang W, et al. Trends Pharmacol Sci. 2018 Apr;39(4):367-386. doi: 10.1016/j.tips.2018.01.001. Epub 2018 Jan 31. Trends Pharmacol Sci. 2018. PMID: 29395118 Review.
In addition, we also discuss the relationship among the five modes to show the complex picture of GPCR activation. The complex activation modes regulate precisely GPCR downstream signaling, including physiological and pathological signaling. Thus, there is the poten …
In addition, we also discuss the relationship among the five modes to show the complex picture of GPCR activation. The complex activa …
Structure, function and drug discovery of GPCR signaling.
Cheng L, Xia F, Li Z, Shen C, Yang Z, Hou H, Sun S, Feng Y, Yong X, Tian X, Qin H, Yan W, Shao Z. Cheng L, et al. Mol Biomed. 2023 Dec 4;4(1):46. doi: 10.1186/s43556-023-00156-w. Mol Biomed. 2023. PMID: 38047990 Free PMC article. Review.
Furthermore, it highlights recent advancements in GPCR-related drug discovery and development. Particular emphasis is placed on GPCR selective drugs, allosteric and biased signaling, polyphamarcology, and antibody drugs. Our goal is to provide researchers with a tho …
Furthermore, it highlights recent advancements in GPCR-related drug discovery and development. Particular emphasis is placed on GP …
Multiplexed selectivity screening of anti-GPCR antibodies.
Dahl L, Kotliar IB, Bendes A, Dodig-Crnković T, Fromm S, Elofsson A, Uhlén M, Sakmar TP, Schwenk JM. Dahl L, et al. Sci Adv. 2023 May 3;9(18):eadf9297. doi: 10.1126/sciadv.adf9297. Epub 2023 May 3. Sci Adv. 2023. PMID: 37134173 Free PMC article.
G protein-coupled receptors (GPCRs) control critical cellular signaling pathways. Therapeutic agents including anti-GPCR antibodies (Abs) are being developed to modulate GPCR function. However, validating the selectivity of anti-GPCR Abs is challenging becaus …
G protein-coupled receptors (GPCRs) control critical cellular signaling pathways. Therapeutic agents including anti-GPCR antibodies ( …
GPCR Allosteric Modulator Discovery.
Wu Y, Tong J, Ding K, Zhou Q, Zhao S. Wu Y, et al. Adv Exp Med Biol. 2019;1163:225-251. doi: 10.1007/978-981-13-8719-7_10. Adv Exp Med Biol. 2019. PMID: 31707706 Review.
The rapid development of GPCR structural biology leads to the discovery of several allosteric sites and sheds light on understanding the mechanism of GPCR allosteric ligands, which is critical for discovering novel therapeutics. This book chapter summarized differen …
The rapid development of GPCR structural biology leads to the discovery of several allosteric sites and sheds light on understanding …
Membrane phosphoinositides regulate GPCR-beta-arrestin complex assembly and dynamics.
Janetzko J, Kise R, Barsi-Rhyne B, Siepe DH, Heydenreich FM, Kawakami K, Masureel M, Maeda S, Garcia KC, von Zastrow M, Inoue A, Kobilka BK. Janetzko J, et al. Cell. 2022 Nov 23;185(24):4560-4573.e19. doi: 10.1016/j.cell.2022.10.018. Epub 2022 Nov 10. Cell. 2022. PMID: 36368322 Free PMC article.
Once internalized, some GPCRs remain complexed with beta-arrestins, while others interact only transiently; this difference affects GPCR signaling and recycling. Cell-based and in vitro biophysical assays reveal the role of membrane phosphoinositides (PIPs) in beta-arresti …
Once internalized, some GPCRs remain complexed with beta-arrestins, while others interact only transiently; this difference affects GPCR …
GPCR-Hippo Signaling in Cancer.
Luo J, Yu FX. Luo J, et al. Cells. 2019 May 8;8(5):426. doi: 10.3390/cells8050426. Cells. 2019. PMID: 31072060 Free PMC article. Review.
Through the activation related G proteins and possibly rearrangements of actin cytoskeleton, GPCR signaling can potently modulate the phosphorylation states and activity of YAP and TAZ, two homologous oncogenic transcriptional co-activators, and major effectors of the Hipp …
Through the activation related G proteins and possibly rearrangements of actin cytoskeleton, GPCR signaling can potently modulate the …
AI-driven GPCR analysis, engineering, and targeting.
Velloso JPL, Kovacs AS, Pires DEV, Ascher DB. Velloso JPL, et al. Curr Opin Pharmacol. 2024 Feb;74:102427. doi: 10.1016/j.coph.2023.102427. Epub 2024 Jan 13. Curr Opin Pharmacol. 2024. PMID: 38219398 Review.
This article investigates the role of recent advances in Artificial Intelligence (AI) to revolutionise the study of G protein-coupled receptors (GPCRs). AI has been applied to many areas of GPCR research, including the application of machine learning (ML) in GPCR cl …
This article investigates the role of recent advances in Artificial Intelligence (AI) to revolutionise the study of G protein-coupled recept …
GPCR structural characterization by NMR spectroscopy in solution.
Yang L, Liu D, Wüthrich K. Yang L, et al. Acta Biochim Biophys Sin (Shanghai). 2022 Aug 25;54(9):1207-1212. doi: 10.3724/abbs.2022106. Acta Biochim Biophys Sin (Shanghai). 2022. PMID: 36017890 Free PMC article. Review.
Determining conformational dynamics and intermolecular interactions are key to understand GPCR function as a basis for drug design. X-ray crystallography and cryo-electron microscopy (cryo-EM) contribute molecular architectures of GPCRs and GPCR-signaling complexes. …
Determining conformational dynamics and intermolecular interactions are key to understand GPCR function as a basis for drug design. X …
GPCR-G protein signalling and its mutational landscape in cancer-Driver or passenger.
Feng C, Ooms JF, Danen EHJ, Heitman LH. Feng C, et al. Br J Pharmacol. 2025 Sep;182(17):3975-3989. doi: 10.1111/bph.70102. Epub 2025 Jun 12. Br J Pharmacol. 2025. PMID: 40501326 Review.
However, the functional redundancy of GPCR signalling networks together with the widespread but low frequency distribution of GPCR mutations indicate that they may rather act as passengers. The future of GPCR drug discovery hinges on overcoming challenges rel …
However, the functional redundancy of GPCR signalling networks together with the widespread but low frequency distribution of GPCR …
17,868 results
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