Results 61 to 70 of about 11,641 (225)

Opening the Field of Integrin Biology to “Biased Agonism” [PDF]

Circulation Research, 2011
See related article, pages 1269–1279 Integrins are α- and β-subunit heterodimeric receptors that mediate divalent cation-dependent cell-cell and cell-matrix adhesion through tightly regulated interactions with ligands central to inflammation, immunity, hemostasis, and tumor metastasis.1 Integrins have been viewed to function within a 2-state model. In
openaire   +2 more sources

Mechanistic insights into the versatile stoichiometry and biased signaling of the apelin receptor-arrestin complex

Nature Communications
The apelin receptor (APJR) plays a pivotal role in regulating cardiovascular and metabolic health1,2. Understanding the mechanisms of biased agonism at APJR is crucial for drug discovery, as stimulation of the β-arrestin pathway may lead to some adverse ...
Yang Yue, Chanjuan Xu, Lijie Wu, Man Na, Kexin Xu, Xuan Chen, Yuxuan Song, Sichun Weng, Lu Xu, Fei Li, Xi Lin, Arthur Wang, Jianfeng Liu, Fei Xu   +13 more
doaj   +1 more source

Comparative efficacy of GLP‐1 RA, tirzepatide and SGLT‐2 inhibitors in metabolic liver disease: A network meta‐analysis

British Journal of Clinical Pharmacology, EarlyView.
Aim Metabolic liver disease, including nonalcoholic fatty liver disease (NAFLD) and nonalcoholic steatohepatitis, is a major cause of chronic liver dysfunction worldwide, creating an urgent need for effective treatments. This systematic literature review (SLR) and network meta‐analysis (NMA) systematically reviews and compares the efficacy and safety ...
Andrej Belančić, Christina Antza, Anastasios Poutachidis, Smaro Palaska, Elvira Meni Maria Gkrinia, Andrea Katrin Faour, Yusuf Ziya Sener, Seher Sener, Rehena Sultana   +8 more
wiley   +1 more source

Assessment of the molecular mechanisms of action of novel 4-phenylpyridine-2-one and 6-phenylpyrimidin-4-one allosteric modulators at the M1 muscarinic acetylcholine receptors [PDF]

, 2018
Positive allosteric modulators (PAMs) that target the M1 muscarinic acetylcholine (ACh) receptor (M1 mAChR) are potential treatments for cognitive deficits in conditions such as Alzheimer's disease and schizophrenia.
Andrew B. Tobin, Arthur Christopoulos, Arthur Spathis, Ben Capuano, Celine Valant, Davoren, Ehlert, Ehlert, Elham Khajehali, Emma T. van der Westhuizen, Furchgott, Manuela Jörg, Mistry, Patrick M. Sexton, Peter J. Scammells, Shailesh N. Mistry   +15 more
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Biased agonism: An emerging paradigm in GPCR drug discovery [PDF]

Bioorganic & Medicinal Chemistry Letters, 2016
G protein coupled receptors have historically been one of the most druggable classes of cellular proteins. The members of this large receptor gene family couple to primary effectors, G proteins, that have built in mechanisms for regeneration and amplification of signaling with each engagement of receptor and ligand, a kinetic event in itself. In recent
Zoran, Rankovic, Tarsis F, Brust, Laura M, Bohn   +2 more
openaire   +2 more sources

Exploring new avenues: Psychedelic‐assisted therapy for young people

British Journal of Clinical Pharmacology, EarlyView.
Rates of mental illness in young people are increasing, whereas the development of novel mental health treatments has not significantly progressed. Psychedelic‐assisted therapy, using substances such as psilocybin and 3,4‐methylenedioxymethamphetamine (MDMA), has shown potential in the treatment of mental illnesses in the adult population, including ...
Ioanna Artemis Vamvakopoulou, Dasha Nicholls, David J. Nutt, Martina Di Simplicio   +3 more
wiley   +1 more source

The pharmacology and function of receptors for short-chain fatty acids [PDF]

, 2015
Despite some blockbuster G protein–coupled receptor (GPCR) drugs, only a small fraction (∼15%) of the more than 390 nonodorant GPCRs have been successfully targeted by the pharmaceutical industry.
Bolognini, Daniele, Milligan, Graeme, Moss, Catherine E., Tobin, Andrew B.   +3 more
core   +1 more source

Serotonin 5‐HT7 receptor signaling in neuropsychiatric disorders

Bulletin of the Korean Chemical Society, EarlyView.
5‐HT7R recruits Gs, G12, and β‐arrestin signaling to regulate neuronal plasticity, circuit function, and kinase‐linked intracellular responses. This review summarizes how these pathway‐selective modules contribute to autism spectrum disorder, depression, and schizophrenia, highlighting 5‐HT7R as a pathway‐informed therapeutic target. Abstract Serotonin
Eunseo Park, Hyunah Choo
wiley   +1 more source

G protein-coupled receptor-biased signaling: potential drug discovery to facilitate treatment of metabolic diseases

Acta Materia Medica
G protein-coupled receptors (GPCRs) are important, potential drug targets for the treatment of metabolic disorders, such as obesity. GPCRs crosstalk with several transducers, including heterotrimeric G proteins, GPCR kinases (GRKs), and β-arrestins. GPCR-
Shengnan Shen, Qiwen Liao, Liwei Gu, Yongping Zhu, Yanqing Liu, Xinwei Zhang, Junzhe Zhang, Qiaoli Shi, Yuxiang Sun, Jigang Wang, Ligen Lin   +10 more
doaj   +1 more source

Evaluation of Biased and Balanced Salvinorin A Analogs in Preclinical Models of Pain

Frontiers in Neuroscience, 2020
In the search for safer, non-addictive analgesics, kappa opioid receptor (KOPr) agonists are a potential target, as unlike mu-opioid analgesics, they do not have abuse potential.
Kelly F. Paton, Andrew Biggerstaff, Sophia Kaska, Rachel S. Crowley, Anne C. La Flamme, Anne C. La Flamme, Thomas E. Prisinzano, Thomas E. Prisinzano, Bronwyn M. Kivell   +8 more
doaj   +1 more source