Neural Regeneration ResearchPeroxisome proliferator-activated receptor alpha is a member of the nuclear hormone receptor superfamily and functions as a transcription factor involved in regulating cellular metabolism.
Zijun Wu +5 more
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Measuring ligand efficacy at the mu-opioid receptor using a conformational biosensor. [PDF]
, 2018 The intrinsic efficacy of orthosteric ligands acting at G-protein-coupled receptors (GPCRs) reflects their ability to stabilize active receptor states (R*) and is a major determinant of their physiological effects.
Livingston, Kathryn E +4 more
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Three classes of ligands each bind to distinct sites on the orphan G protein-coupled receptor GPR84 [PDF]
, 2017 Medium chain fatty acids can activate the pro-inflammatory receptor GPR84 but so also can molecules related to 3,3′-diindolylmethane. 3,3′-Diindolylmethane and decanoic acid acted as strong positive allosteric modulators of the function of each other and
De Vos, Steve +8 more
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Glucagon-like peptide-1 receptor agonists in neoplastic diseases
Frontiers in EndocrinologyGlucagon-like peptide-1 receptor agonist (GLP-1RA), a novel hypoglycemic agent for the treatment of type 2 diabetes, has well-known effects such as lowering blood sugar, ameliorating inflammation, reducing weight, and lowering blood lipids.
Lisan Ji +8 more
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Resistance of Muscle to Tumor Metastases: A Role for A3 Adenosine Receptor Agonists
Neoplasia: An International Journal for Oncology Research, 2001 Tumor metastases are extremely rare in striated muscles. Lately, we have found that muscle cell conditioned medium (MCM) inhibits the proliferation of various tumor cells while maintaining the growth of normal murine bone marrow cells. This dual activity
Sara Bar-Yehuda +3 more
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Guideline on management of the acute asthma attack in children by Italian Society of Pediatrics. [PDF]
, 2018 BACKGROUND: Acute asthma attack is a frequent condition in children. It is one of the most common reasons for emergency department (ED) visit and hospitalization. Appropriate care is fundamental, considering both the high prevalence of asthma in children,
Chiappini, E +3 more
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Clinical Use of β2-adrenergic Receptor Agonists Based on Their Intrinsic Efficacy
Allergology International, 2005 Clinical choice of β2-adrenergic receptor agonists (β2-agonists) is based on the parameter of receptor selectivity, potency, and duration of action. The guidelines for asthma management describe nothing about intrinsic efficacy concerning the use of β2 ...
Hiroaki Kume
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Structurally similar allosteric modulators of α7 nicotinic acetylcholine receptors exhibit five distinct pharmacological effects. [PDF]
, 2015 Activation of nicotinic acetylcholine receptors (nAChRs) is associated with the binding of agonists such as acetylcholine to an extracellular site that is located at the interface between two adjacent receptor subunits.
D'Oyley, JM +4 more
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ToxinsTransient Receptor Potential (TRP) channels are ubiquitous proteins involved in a wide range of physiological functions. Some of them are expressed in nociceptors and play a major role in the transduction of painful stimuli of mechanical, thermal, or ...
Florian Beignon +7 more
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The efficiency of CD4 recruitment to ligand-engaged TCR controls the agonist/partial agonist properties of peptide-MHC molecule ligands. [PDF]
, 1997 One hypothesis seeking to explain the signaling and biological properties of T cell receptor for antigen (TCR) partial agonists and antagonists is the coreceptor density/kinetic model, which proposes that the pharmacologic behavior of a TCR ligand is ...
Bluestone, JA +4 more
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