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Page 1
Intracellular GPCR modulators enable precision pharmacology.
Krumm BE, Roth BL. Krumm BE, et al. NPJ Drug Discov. 2025;2(1):8. doi: 10.1038/s44386-025-00011-8. Epub 2025 May 12. NPJ Drug Discov. 2025. PMID: 40371403 Free PMC article. Review.
G-protein-coupled receptors (GPCRs) have proven to be the most successful target class for drug discovery but their complicated signal transduction pathways cause difficulties for drug development. Recently, ligands have been identified that engage an intracellular …
G-protein-coupled receptors (GPCRs) have proven to be the most successful target class for drug discovery but their complicate …
Neurokinin-1 receptor: functional significance in the immune system in reference to selected infections and inflammation.
Douglas SD, Leeman SE. Douglas SD, et al. Ann N Y Acad Sci. 2011 Jan;1217:83-95. doi: 10.1111/j.1749-6632.2010.05826.x. Epub 2010 Nov 22. Ann N Y Acad Sci. 2011. PMID: 21091716 Free PMC article. Review.
The G protein-coupled receptor (GPCR), neurokinin-1 receptor (NK1R), and its preferred ligand, substance P (SP), are reviewed in relationship to the immune system and selected infections. ...The proinflammatory signals modulated by SP are important in bacterial, viral, fun …
The G protein-coupled receptor (GPCR), neurokinin-1 receptor (NK1R), and its preferred ligand, substance P (SP), are reviewed in rela …
Chemical modification of class II G protein-coupled receptor ligands: frontiers in the development of peptide analogs as neuroendocrine pharmacological therapies.
Chapter MC, White CM, DeRidder A, Chadwick W, Martin B, Maudsley S. Chapter MC, et al. Pharmacol Ther. 2010 Jan;125(1):39-54. doi: 10.1016/j.pharmthera.2009.07.006. Epub 2009 Aug 15. Pharmacol Ther. 2010. PMID: 19686775 Free PMC article. Review.
Recent research and clinical data have begun to demonstrate the huge potential therapeutic importance of ligands that modulate the activity of the secretin-like, Class II, G protein-coupled receptors (GPCRs). Ligands that can modulate the activity of these Class …
Recent research and clinical data have begun to demonstrate the huge potential therapeutic importance of ligands that modulate the activity …
The Hydrophobic Ligands Entry and Exit from the GPCR Binding Site-SMD and SuMD Simulations.
Jakowiecki J, Orzeł U, Chawananon S, Miszta P, Filipek S. Jakowiecki J, et al. Molecules. 2020 Apr 21;25(8):1930. doi: 10.3390/molecules25081930. Molecules. 2020. PMID: 32326322 Free PMC article.
Most G protein-coupled receptors that bind the hydrophobic ligands (lipid receptors and steroid receptors) belong to the most populated class A (rhodopsin-like) of these receptors. Typical examples of lipid receptors are: rh …
Most G protein-coupled receptors that bind the hydrophobic ligands (lipid receptors and steroid receptors) belong to th …
PAXIP1-AS1 is associated with immune infiltration and predicts poor prognosis in ovarian cancer.
Chen B, Lu X, Zhou Q, Chen Q, Zhu S, Li G, Liu H. Chen B, et al. PLoS One. 2023 Aug 15;18(8):e0290031. doi: 10.1371/journal.pone.0290031. eCollection 2023. PLoS One. 2023. PMID: 37582104 Free PMC article.
Low PAXIP1-AS1 expression predicted a poorer overall survival (OS) (HR: 0.71; 95% CI: 0.55-0.92; P = 0.009), progression free interval (PFS) (HR: 1.776; 95% CI: 1.067-2.955; P = 0.001) and disease specific survival (DSS) (HR: 0.67; 95% CI: 0.51-0.89; P = 0.006). ... …
Low PAXIP1-AS1 expression predicted a poorer overall survival (OS) (HR: 0.71; 95% CI: 0.55-0.92; P = 0.009), progression free interval (PFS) …
Bioinformatic analysis for the identification of potential gene interactions and therapeutic targets in atrial fibrillation.
Yu SD, Yu JY, Guo Y, Liu XY, Liang T, Chen LZ, Chu YP, Zhang HP. Yu SD, et al. Eur Rev Med Pharmacol Sci. 2021 Mar;25(5):2281-2290. doi: 10.26355/eurrev_202103_25260. Eur Rev Med Pharmacol Sci. 2021. PMID: 33755965 Free article.
In the GO biological process, cellular component, and molecular function analyses, positive regulation of cell migration, anchoring junctions, and cell adhesion molecule binding were enriched significantly. The Hippo signalling pathway was the most significantly enriched …
In the GO biological process, cellular component, and molecular function analyses, positive regulation of cell migration, anchoring junction …
First metabolic profiling of 4-n-nonylphenol in human liver microsomes by integrated approaches to testing and assessment: Metabolites, pathways, and biological effects.
Xie R, Xu Y, Ma M, Wang X, Zhang L, Wang Z. Xie R, et al. J Hazard Mater. 2023 Apr 5;447:130830. doi: 10.1016/j.jhazmat.2023.130830. Epub 2023 Jan 20. J Hazard Mater. 2023. PMID: 36682248
Two secondary metabolites with carbonyl groups on side chains (M4, M7) presented most abundant in HLM, which were also predicted to have high binding affinities towards HPG-axis-related receptors (AR, ER, and PR). ESRs (estrogen receptors) were shared core protein t …
Two secondary metabolites with carbonyl groups on side chains (M4, M7) presented most abundant in HLM, which were also predicted to have hig …
In Silico Modeling of Novel Drug Ligands for Treatment of Concussion Associated Tauopathy.
Zhao W, Ho L, Wang J, Bi W, Yemul S, Ward L, Freire D, Mazzola P, Brathwaite J, Mezei M, Sanchez R, Elder GA, Pasinetti GM. Zhao W, et al. J Cell Biochem. 2016 Oct;117(10):2241-8. doi: 10.1002/jcb.25521. Epub 2016 Jul 12. J Cell Biochem. 2016. PMID: 26910498 Free PMC article.
The objective of this study was to develop an in silico screening model for characterization of potential novel ligands from commercial drug libraries able to functionally activate certain olfactory receptors (ORs), which are members of the class A rhodopsin- …
The objective of this study was to develop an in silico screening model for characterization of potential novel ligands from commercial drug …
Computational systems pharmacology analysis of cannabidiol: a combination of chemogenomics-knowledgebase network analysis and integrated in silico modeling and simulation.
Bian YM, He XB, Jing YK, Wang LR, Wang JM, Xie XQ. Bian YM, et al. Acta Pharmacol Sin. 2019 Mar;40(3):374-386. doi: 10.1038/s41401-018-0071-1. Epub 2018 Sep 10. Acta Pharmacol Sin. 2019. PMID: 30202014 Free PMC article.
In the present work, chemogenomics-knowledgebase systems pharmacology analysis was applied for systematic network studies to generate CBD-target, target-pathway, and target-disease networks by combining both the results from the in silico analysis and the reported experime …
In the present work, chemogenomics-knowledgebase systems pharmacology analysis was applied for systematic network studies to generate CBD-ta …
Unveiling the Role of DPYS: A New Prognostic Biomarker in Sarcoma.
Lyu G, Li D. Lyu G, et al. Curr Protein Pept Sci. 2025;26(9):761-772. doi: 10.2174/0113892037362065250227064739. Curr Protein Pept Sci. 2025. PMID: 40192045
BACKGROUND: Dihydropyrimidinase (DPYS), a pivotal enzyme in the pyrimidine synthesis pathway, has been increasingly studied for its potential role in cancer therapy. While its presence has been noted in various cancers, its specific impact on sarcoma (SARC) still needs to …
BACKGROUND: Dihydropyrimidinase (DPYS), a pivotal enzyme in the pyrimidine synthesis pathway, has been increasingly studied for its p …
12 results