10 Result(s)
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Lauren T. May
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The urgent need for designing greener drugs
The pervasive contamination of ecosystems with active pharmaceutical ingredients poses a serious threat to biodiversity, ecosystem services and public health. Urgent action is needed to design greener drugs th...
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Physicochemical graph neural network for learning protein–ligand interaction fingerprints from sequence data
In drug discovery, determining the binding affinity and functional effects of small-molecule ligands on proteins is critical. Current computational methods can predict these protein–ligand interaction properti...
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Open AccessPublisher Correction to: Adenosine receptor signalling in Alzheimer’s disease
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Open AccessAdenosine receptor signalling in Alzheimer’s disease
Alzheimer’s disease (AD) is the most common dementia in the elderly and its increasing prevalence presents treatment challenges. Despite a better understanding of the disease, the current mainstay of treatment...
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Positive allosteric mechanisms of adenosine A1 receptor-mediated analgesia
The adenosine A1 receptor (A1R) is a promising therapeutic target for non-opioid analgesic agents to treat neuropathic pain1,2. However, development of analgesic orthosteric A1R agonists has failed because of a l...
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Open AccessStructural Basis for Binding of Allosteric Drug Leads in the Adenosine A1 Receptor
Despite intense interest in designing positive allosteric modulators (PAMs) as selective drugs of the adenosine A1 receptor (A1AR), structural binding modes of the receptor PAMs remain unknown. Using the first X-...
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Structure of the adenosine-bound human adenosine A1 receptor–Gi complex
The class A adenosine A1 receptor (A1R) is a G-protein-coupled receptor that preferentially couples to inhibitory Gi/o heterotrimeric G proteins, has been implicated in numerous diseases, yet remains poorly targe...
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Open AccessCorrespondence: Reply to ‘Compound 17b and formyl peptide receptor biased agonism in relation to cardioprotective effects in ischaemia-reperfusion injury’
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A kinetic view of GPCR allostery and biased agonism
Allosteric modulation and biased agonism at GPCRs could be manifestations of the same underlying 'conformational selection' mechanism, and these can be harmonized by considering the influence of ligand–recepto...
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Open AccessSmall-molecule-biased formyl peptide receptor agonist compound 17b protects against myocardial ischaemia-reperfusion injury in mice
Effective treatment for managing myocardial infarction (MI) remains an urgent, unmet clinical need. Formyl peptide receptors (FPR) regulate inflammation, a major contributing mechanism to cardiac injury follow...
