Structure-based discovery of nonopioid analgesics acting through the α2A-adrenergic receptor
Because nonopioid analgesics are much sought after, we computationally docked more
than 301 million virtual molecules against a validated pain target, the α2A-adrenergic …
than 301 million virtual molecules against a validated pain target, the α2A-adrenergic …
Cloning of a delta opioid receptor by functional expression
CJ Evans, DE Keith Jr, H Morrison, K Magendzo… - Science, 1992 - science.org
Opiate drugs have potent analgesic and addictive properties. These drugs interact with
receptors that also mediate the response to endogenous opioid peptide ligands. However …
receptors that also mediate the response to endogenous opioid peptide ligands. However …
Activation of the α2B adrenoceptor by the sedative sympatholytic dexmedetomidine
D Yuan, Z Liu, J Kaindl, S Maeda, J Zhao, X Sun… - Nature chemical …, 2020 - nature.com
The α2 adrenergic receptors (α2ARs) are G protein-coupled receptors (GPCRs) that
respond to adrenaline and noradrenaline and couple to the Gi/o family of G proteins. α2ARs …
respond to adrenaline and noradrenaline and couple to the Gi/o family of G proteins. α2ARs …
Structural insights into ligand recognition, activation, and signaling of the α2A adrenergic receptor
The α2A adrenergic receptor (α2AAR) is a G protein (heterotrimeric guanine nucleotide–
binding protein)–coupled receptor that mediates important physiological functions in …
binding protein)–coupled receptor that mediates important physiological functions in …
Conformational cross-talk between α2A-adrenergic and μ-opioid receptors controls cell signaling
JP Vilardaga, VO Nikolaev, K Lorenz… - Nature chemical …, 2008 - nature.com
Morphine, a powerful analgesic, and norepinephrine, the principal neurotransmitter of
sympathetic nerves, exert major inhibitory effects on both peripheral and brain neurons by …
sympathetic nerves, exert major inhibitory effects on both peripheral and brain neurons by …
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 pain,. However, development of analgesic orthosteric A1R …
agents to treat neuropathic pain,. However, development of analgesic orthosteric A1R …
Structure-based discovery of opioid analgesics with reduced side effects
Morphine is an alkaloid from the opium poppy used to treat pain. The potentially lethal side
effects of morphine and related opioids—which include fatal respiratory depression—are …
effects of morphine and related opioids—which include fatal respiratory depression—are …
Molecular control of δ-opioid receptor signalling
Opioids represent widely prescribed and abused medications, although their signal
transduction mechanisms are not well understood. Here we present the 1.8 Å high …
transduction mechanisms are not well understood. Here we present the 1.8 Å high …
Elucidating the active δ-opioid receptor crystal structure with peptide and small-molecule agonists
Selective activation of the δ-opioid receptor (DOP) has great potential for the treatment of
chronic pain, benefitting from ancillary anxiolytic and antidepressant-like effects. Moreover …
chronic pain, benefitting from ancillary anxiolytic and antidepressant-like effects. Moreover …
Structure of the δ-opioid receptor bound to naltrindole
The opioid receptor family comprises three members, the µ-, δ-and κ-opioid receptors, which
respond to classical opioid alkaloids such as morphine and heroin as well as to …
respond to classical opioid alkaloids such as morphine and heroin as well as to …