Trends in GPCR drug discovery: new agents, targets and indications

AS Hauser, MM Attwood, M Rask-Andersen… - Nature reviews Drug …, 2017 - nature.com
G protein-coupled receptors (GPCRs) are the most intensively studied drug targets, mostly
due to their substantial involvement in human pathophysiology and their pharmacological …

Neuroinflammation and central sensitization in chronic and widespread pain

RR Ji, A Nackley, Y Huh, N Terrando… - …, 2018 - pmc.ncbi.nlm.nih.gov
Chronic pain is maintained in part by central sensitization, a phenomenon of synaptic
plasticity and increased neuronal responsiveness in central pain pathways after painful …

Poorly controlled postoperative pain: prevalence, consequences, and prevention

TJ Gan - Journal of pain research, 2017 - Taylor & Francis
This review provides an overview of the clinical issue of poorly controlled postoperative pain
and therapeutic approaches that may help to address this common unresolved health-care …

Molecular recognition of morphine and fentanyl by the human μ-opioid receptor

Y Zhuang, Y Wang, B He, X He, XE Zhou, S Guo… - Cell, 2022 - cell.com
Morphine and fentanyl are among the most used opioid drugs that confer analgesia and
unwanted side effects through both G protein and arrestin signaling pathways of μ-opioid …

The physiology, signaling, and pharmacology of dopamine receptors

JM Beaulieu, RR Gainetdinov, DR Sibley - Pharmacological reviews, 2011 - Elsevier
G protein-coupled dopamine receptors (D1, D2, D3, D4, and D5) mediate all of the
physiological functions of the catecholaminergic neurotransmitter dopamine, ranging from …

Psychedelics reopen the social reward learning critical period

R Nardou, E Sawyer, YJ Song, M Wilkinson… - Nature, 2023 - nature.com
Psychedelics are a broad class of drugs defined by their ability to induce an altered state of
consciousness,. These drugs have been used for millennia in both spiritual and medicinal …

Structure-based discovery of opioid analgesics with reduced side effects

A Manglik, H Lin, DK Aryal, JD McCorvy, D Dengler… - Nature, 2016 - nature.com
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 …

Biased signalling: from simple switches to allosteric microprocessors

JS Smith, RJ Lefkowitz, S Rajagopal - Nature reviews Drug discovery, 2018 - nature.com
G protein-coupled receptors (GPCRs) are the largest class of receptors in the human
genome and some of the most common drug targets. It is now well established that GPCRs …

Seven-transmembrane receptors

KL Pierce, RT Premont, RJ Lefkowitz - Nature reviews Molecular cell …, 2002 - nature.com
Seven-transmembrane receptors, which constitute the largest, most ubiquitous and most
versatile family of membrane receptors, are also the most common target of therapeutic …

Structural insights into µ-opioid receptor activation

W Huang, A Manglik, AJ Venkatakrishnan… - Nature, 2015 - nature.com
Activation of the μ-opioid receptor (μOR) is responsible for the efficacy of the most effective
analgesics. To shed light on the structural basis for μOR activation, here we report a 2.1 Å X …