Fine Tuning Muscarinic Acetylcholine Receptor Signaling Through Allostery and Bias
Frontiers in Pharmacology, 2021 The M1 and M4 muscarinic acetylcholine receptors (mAChRs) are highly pursued drug targets for neurological diseases, in particular for Alzheimer’s disease and schizophrenia.
Emma T. van der Westhuizen +7 more
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JCI Insight, 2022 Biased agonism is a frontier field in GPCR research. Acquired hypocalciuric hypercalcemia (AHH) is a rare disease caused by calcium-sensing receptor (CaSR) autoantibodies, to date, showing either simple blocking or biased properties (i.e., stimulatory or
Noriko Makita +10 more
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Ligand-Specific Regulation of the Endogenous Mu-Opioid Receptor by Chronic Treatment with Mu-Opioid Peptide Agonist [PDF]
, 2013 Since the discovery of the endomorphins (EM), the postulated endogenous peptide agonists of the mu-opioid receptors, several analogues have been synthesized to improve their binding and pharmacological profiles.
Birkás, Erika +12 more
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Targeting the IGF-1R: The Tale of The Tortoise and The Hare
Frontiers in Endocrinology, 2015 The insulin-like growth factor type 1 receptor (IGF-1R) plays a key role in the development and maintenance of cancer. Since the first links between growth factor receptors and oncogenes were noted over three decades ago, targeting the IGF-1R has been of
Caitrin eCrudden +3 more
doaj +1 more source
Biased versus Partial Agonism in the Search for Safer Opioid Analgesics
Molecules, 2020 Opioids such as morphine—acting at the mu opioid receptor—are the mainstay for treatment of moderate to severe pain and have good efficacy in these indications.
Joaquim Azevedo Neto +5 more
doaj +1 more source
Rates of agonism among female primates: a cross-taxon perspective [PDF]
, 2013 Agonism is common in group-living animals, shaping dominance relationships and ultimately impacting individual tness. Rates of agonism vary considerably among taxa, however, and explaining this variation has been central in ecological models of female ...
Altmann +131 more
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Quinolones modulate ghrelin receptor signaling: potential for a novel small molecule scaffold in the treatment of cachexia [PDF]
, 2018 Cachexia is a metabolic wasting disorder characterized by progressive weight loss, muscle atrophy, fatigue, weakness, and appetite loss. Cachexia is associated with almost all major chronic illnesses including cancer, heart failure, obstructive ...
Cano, Rafael +8 more
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A Pharmacological Primer of Biased Agonism [PDF]
Endocrine, Metabolic & Immune Disorders - Drug Targets, 2011 Biased agonism is one of the fastest growing topics in G protein-coupled receptor pharmacology; moreover, biased agonists are used in the clinic today: carvedilol (Coreg®) is a biased agonist of beta-adrenergic receptors. However, there is a general lack of understanding of biased agonism when compared to traditional pharmacological terminology ...
openaire +2 more sources
Paradigm of biased PAR1 (protease-activated receptor-1) activation and inhibition in endothelial cells dissected by phosphoproteomics [PDF]
, 2017 Thrombin is the key serine protease of the coagulation cascade and mediates cellular responses by activation of PARs (protease-activated receptors). The predominant thrombin receptor is PAR1, and in endothelial cells (ECs), thrombin dynamically regulates
Hoogendijk, Arie J. +7 more
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Differential Signaling Profiles of MC4R Mutations with Three Different Ligands [PDF]
, 2020 The melanocortin 4 receptor (MC4R) is a key player in hypothalamic weight regulation and energy expenditure as part of the leptin-melanocortin pathway. Mutations in this G protein coupled receptor (GPCR) are the most common cause for monogenetic obesity,
Annibale, Paolo +8 more
core +3 more sources