Biased Agonism at the Angiotensin Receptor [PDF]
Circulation, 2017 Article, see p 1056 Dilated cardiomyopathy (DCM) is a myocardial disease characterized by ventricular dilation and reduced pumping power. Numerous factors, including infections, congenital defects, genetic mutations, and exposure to chemotherapeutic agents or alcohol, can damage the myocardium and predispose the heart to DCM.
Anthony Yiu-Ho, Woo +2 more
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Pepducins as a potential treatment strategy for asthma and COPD. [PDF]
, 2018 Current therapies to treat asthma and other airway diseases primarily include anti-inflammatory agents and bronchodilators. Anti-inflammatory agents target trafficking and resident immunocytes and structural cells, while bronchodilators act to prevent or
Benovic, Jeffrey L. +4 more
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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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Allosteric coupling and biased agonism in G protein‐coupled receptors [PDF]
The FEBS Journal, 2021 G protein‐coupled receptors (GPCRs) are essential cell membrane signaling molecules and represent the most important class of drug targets. Some signaling pathways downstream of a GPCR may be responsible for drug adverse effects, while others mediate therapeutic efficacy.
Andreas Bock, Marcel Bermudez
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In vitro and in vivo pharmacological activities of 14-o-phenylpropyloxymorphone, a potent mixed mu/delta/kappa-opioid receptor agonist with reduced constipation in mice [PDF]
, 2018 Pain, particularly chronic pain, is still an unsolved medical condition. Central goals in pain control are to provide analgesia of adequate efficacy and to reduce complications associated with the currently available drugs.
Lattanzi, Roberta +4 more
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Bitopic binding mode of an M1 muscarinic acetylcholine receptor agonist associated with adverse clinical trial outcomes [PDF]
, 2018 The realisation of the therapeutic potential of targeting the M1 muscarinic acetylcholine receptor (M1 mAChR) for the treatment of cognitive decline in Alzheimer's disease has prompted the discovery of M1 mAChR ligands showing efficacy in alleviating ...
Bradley, Sophie J. +14 more
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Signal Transduction and Pathogenic Modifications at the Melanocortin-4 Receptor: A Structural Perspective [PDF]
, 2019 The melanocortin-4 receptor (MC4R) can be endogenously activated by binding of melanocyte-stimulating hormones (MSH), which mediates anorexigenic effects. In contrast, the agouti-related peptide (AgRP) acts as an endogenous inverse agonist and suppresses
Biebermann, Heike +10 more
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Functional divergence in the role of N-linked glycosylation in smoothened signaling [PDF]
, 2015 The G protein-coupled receptor (GPCR) Smoothened (Smo) is the requisite signal transducer of the evolutionarily conserved Hedgehog (Hh) pathway. Although aspects of Smo signaling are conserved from Drosophila to vertebrates, significant differences have ...
A Helenius +83 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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7‑hydroxymitragynine is an active metabolite of mitragynine and a key mediator of its analgesic effects [PDF]
, 2019 Mitragynina speciosa, more commonly known as kratom, is a plant native to Southeast Asia, the leaves of which have been used traditionally as a stimulant, analgesic, and treatment for opioid addiction.
Ansonoff, Michael +12 more
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