Results 51 to 60 of about 31,985 (308)
Allosteric optical control of a class B G-protein-coupled receptor [PDF]
, 2016 Allosteric regulation promises to open up new therapeutic avenues by increasing drug specificity at G‐protein‐coupled receptors (GPCRs). However, drug discovery efforts are at present hampered by an inability to precisely control the allosteric site ...
Broichhagen +20 more
core +1 more source
De Novo Design of Peptidic Positive Allosteric Modulators Targeting TRPV1 with Analgesic Effects
Advanced Science, 2021 Transient receptor potential vanilloid 1 (TRPV1) ion channel is a nociceptor critically involved in pain sensation. Direct blockade of TRPV1 exhibits significant analgesic effects but also incurs severe side effects such as hyperthermia, causing failures
Lizhen Xu +10 more
doaj +1 more source
Understanding the Allosteric Modulation of PTH1R by a Negative Allosteric Modulator
Cells, 2022 The parathyroid hormone type 1 receptor (PTH1R) acts as a canonical class B G protein-coupled receptor, regulating crucial functions including calcium homeostasis and bone formation.
Mengrong Li +5 more
doaj +1 more source
GABAB receptor ligands for the treatment of alcohol use disorder: preclinical and clinical evidence. [PDF]
, 2014 The present paper summarizes the preclinical and clinical studies conducted to define the "anti-alcohol" pharmacological profile of the prototypic GABAB receptor agonist, baclofen, and its therapeutic potential for treatment of alcohol use disorder (AUD).
Agabio R, Colombo G
core +2 more sources
eLife, 2020 Pentameric ligand-gated ion channels (pLGICs) or Cys-loop receptors are involved in fast synaptic signaling in the nervous system. Allosteric modulators bind to sites that are remote from the neurotransmitter binding site, but modify coupling of ligand ...
Marijke Brams +12 more
doaj +1 more source
Novel positive allosteric modulators of GABAA receptors with anesthetic activity [PDF]
Scientific Reports, 2016 AbstractGABAAreceptors are the main inhibitory neurotransmitter receptors in the brain and are targets for numerous clinically important drugs such as benzodiazepines, anxiolytics and anesthetics. We previously identified novel ligands of the classical benzodiazepine binding pocket in α1β2γ2GABAAreceptors using an experiment-guided virtual screening ...
Maldifassi, Maria Constanza +5 more
openaire +3 more sources
Saudi Pharmaceutical Journal, 2023 Chemotherapy-induced peripheral neuropathy (CIPN) is one of chemotherapies’ most often documented side effects. Patients with CIPN experience spontaneous burning, numbness, tingling, and neuropathic pain in their feet and hands.
Amina M. Bagher +3 more
doaj +1 more source
Flavonoids as positive allosteric modulators of α7 nicotinic receptors
Neuropharmacology, 2019 The use of positive allosteric modulators (PAM) of α7 nicotinic receptors is a promising therapy for neurodegenerative, inflammatory and cognitive disorders. Flavonoids are polyphenolic compounds showing neuroprotective, anti-inflammatory and pro-cognitive actions. Besides their well-known antioxidant activity, flavonoids trigger intracellular pathways
Beatriz Elizabeth Nielsen +2 more
openaire +4 more sources
Positive allosteric modulation of indoleamine 2,3-dioxygenase 1 restrains neuroinflammation [PDF]
Proceedings of the National Academy of Sciences, 2020 Significance Indoleamine 2,3-dioxygenase 1 (IDO1) is an immunoregulatory enzyme that transforms tryptophan into kynurenine, an endogenous agonist of the aryl hydrocarbon receptor (AhR) whose activation sustains IDO1 expression and activity over the long term in dendritic cells (DCs).
Giada Mondanelli +30 more
openaire +3 more sources
The pharmacology and function of receptors for short-chain fatty acids [PDF]
, 2015 Despite some blockbuster G protein–coupled receptor (GPCR) drugs, only a small fraction (∼15%) of the more than 390 nonodorant GPCRs have been successfully targeted by the pharmaceutical industry.
Bolognini, Daniele +3 more
core +1 more source