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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Quantifying biased agonism: understanding the links between affinity and efficacy [PDF]
Nature Reviews Drug Discovery, 2013 Sudarshan Rajagopal
openaire +4 more sources
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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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
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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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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
A grounded theory of local ownership as meta-conflict in Afghanistan [PDF]
, 2020 Internationally-sponsored interventions in fragile and conflict-affected states are often resisted by domestic actors who have deep local knowledge, profoundly different expectations of political processes, and keen desires to shape their country’s ...
Collins, Andrew, Thiessen, Chuck
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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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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
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Pinpointing brainstem mechanisms responsible for autonomic dysfunction in Rett syndrome:therapeutic perspectives for 5-HT1A agonists [PDF]
, 2014 Rett syndrome is a neurological disorder caused by loss of function of methyl-CpG-binding protein 2 (MeCP2). Reduced function of this ubiquitous transcriptional regulator has a devastating effect on the central nervous system.
Abdala, Ana Paula +2 more
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