Structure-based virtual screening for ligands of G protein–coupled receptors: what can molecular docking do for you?
F Ballante, AJ Kooistra, S Kampen, C de Graaf… - Pharmacological …, 2021 - ASPET
G protein–coupled receptors (GPCRs) constitute the largest family of membrane proteins in
the human genome and are important therapeutic targets. During the last decade, the …
the human genome and are important therapeutic targets. During the last decade, the …
Opioid analgesia and opioid-induced adverse effects: a review
AK Paul, CM Smith, M Rahmatullah, V Nissapatorn… - Pharmaceuticals, 2021 - mdpi.com
Opioids are widely used as therapeutic agents against moderate to severe acute and
chronic pain. Still, these classes of analgesic drugs have many potential limitations as they …
chronic pain. Still, these classes of analgesic drugs have many potential limitations as they …
Molecular recognition of morphine and fentanyl by the human μ-opioid receptor
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 …
unwanted side effects through both G protein and arrestin signaling pathways of μ-opioid …
Structures of the entire human opioid receptor family
Opioids are effective analgesics, but their use is beset by serious side effects, including
addiction and respiratory depression, which contribute to the ongoing opioid crisis. The …
addiction and respiratory depression, which contribute to the ongoing opioid crisis. The …
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 …
Structure of the nanobody-stabilized active state of the kappa opioid receptor
The κ-opioid receptor (KOP) mediates the actions of opioids with hallucinogenic, dysphoric,
and analgesic activities. The design of KOP analgesics devoid of hallucinatory and …
and analgesic activities. The design of KOP analgesics devoid of hallucinatory and …
Advances in therapeutic peptides targeting G protein-coupled receptors
AP Davenport, CCG Scully, C de Graaf… - Nature Reviews Drug …, 2020 - nature.com
Dysregulation of peptide-activated pathways causes a range of diseases, fostering the
discovery and clinical development of peptide drugs. Many endogenous peptides activate G …
discovery and clinical development of peptide drugs. Many endogenous peptides activate G …
Molecular signatures of G-protein-coupled receptors
G-protein-coupled receptors (GPCRs) are physiologically important membrane proteins that
sense signalling molecules such as hormones and neurotransmitters, and are the targets of …
sense signalling molecules such as hormones and neurotransmitters, and are the targets of …
Pathophysiology of L-dopa-induced motor and non-motor complications in Parkinson's disease
Involuntary movements, or dyskinesia, represent a debilitating complication of levodopa (L-
dopa) therapy for Parkinson's disease (PD). L-dopa-induced dyskinesia (LID) are ultimately …
dopa) therapy for Parkinson's disease (PD). L-dopa-induced dyskinesia (LID) are ultimately …
GPCR drug discovery: integrating solution NMR data with crystal and cryo-EM structures
I Shimada, T Ueda, Y Kofuku, MT Eddy… - Nature Reviews Drug …, 2019 - nature.com
The 826 G protein-coupled receptors (GPCRs) in the human proteome regulate key
physiological processes and thus have long been attractive drug targets. With the crystal …
physiological processes and thus have long been attractive drug targets. With the crystal …