Frontiers in Pharmacology, 2018 When a small molecule binds to the androgen receptor (AR), a conformational change can occur which impacts subsequent binding of co-regulator proteins and DNA.
Sugunadevi Sakkiah +6 more
doaj +1 more source
Science Translational Medicine, 2018 The small-molecule AT-121 is an agonist of nociceptin and mu opioid peptide receptors and mediates analgesia without opioid-associated side effects in nonhuman primates.
H. Ding +9 more
semanticscholar +1 more source
In vitro and in vivo pharmacological activities of 14-o-phenylpropyloxymorphone, a potent mixed mu/delta/kappa-opioid receptor agonist with reduced constipation in mice [PDF]
, 2018 Pain, particularly chronic pain, is still an unsolved medical condition. Central goals in pain control are to provide analgesia of adequate efficacy and to reduce complications associated with the currently available drugs.
Lattanzi, Roberta +4 more
core +2 more sources
Opioid agonist treatment for pharmaceutical opioid dependent people.
Cochrane Database of Systematic Reviews, 2016 BACKGROUND There are increasing concerns regarding pharmaceutical opioid harms including overdose and dependence, with an associated increase in treatment demand.
S. Nielsen +5 more
semanticscholar +1 more source
Serotonin Type 6 and 7 Receptors as a Novel Therapeutic Target for the Treatment of Schizophrenia
Neuropsychiatric Disease and Treatment, 2020 Etsay Weldekidan Tsegay,1 Desalegn Getnet Demise,1 Nigus Alemu Hailu,2 Zenawi Hagos Gufue3 1Department of Pharmacy, College of Medicine and Health Sciences, Adigrat University, Adigrat, Tigray, Ethiopia; 2Department of Biomedical Science, College of ...
Tsegay EW, Demise DG, Hailu NA, Gufue ZH
doaj
Cannabinoid receptor interacting protein suppresses agonist-driven CB1 receptor internalization and regulates receptor replenishment in an agonist-biased manner [PDF]
, 2016 Cannabinoid receptor interacting protein 1a (CRIP1a) is a CB1 receptor (CB1R) distal C-terminus-associated protein that modulates CB1R signaling via G proteins, and CB1R down-regulation but not desensitization (Blume et al.
Bass, Caroline E. +8 more
core +2 more sources
Agonist-Mediated Activation of STING Induces Apoptosis in Malignant B Cells.
Cancer Research, 2016 Endoplasmic reticulum (ER) stress responses through the IRE-1/XBP-1 pathway are required for the function of STING (TMEM173), an ER-resident transmembrane protein critical for cytoplasmic DNA sensing, IFN production, and cancer control. Here we show that
C. Tang +6 more
semanticscholar +1 more source
Regions of beta 2 and beta 4 responsible for differences between the steady state dose-response relationships of the alpha 3 beta 2 and alpha 3 beta 4 neuronal nicotinic receptors [PDF]
, 1995 We constructed chimeras of the rat beta 2 and beta 4 neuronal nicotinic subunits to locate the regions that contribute to differences between the acetylcholine (ACh) dose-response relationships of the alpha 3 beta 2 and alpha 3 beta 4 receptors ...
Cohen, B. N. +5 more
core +2 more sources
T-Cell activation: a queuing theory analysis at low agonist density [PDF]
, 2006 We analyze a simple linear triggering model of the T-cell receptor (TCR) within the framework of queuing theory, in which TCRs enter the queue upon full activation and exit by downregulation.
Bossi +61 more
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Identification of a Raloxifene Analog That Promotes AhR-Mediated Apoptosis in Cancer Cells
Biology, 2017 We previously reported that raloxifene, an estrogen receptor modulator, is also a ligand for the aryl hydrocarbon receptor (AhR). Raloxifene induces apoptosis in estrogen receptor-negative human cancer cells through the AhR.
Hyo Sang Jang +9 more
doaj +1 more source