Search Results - "Bohn, Laura M"
-
1
Crystal Structure of the Human Cannabinoid Receptor CB1
Published in Cell (20-10-2016)“…Cannabinoid receptor 1 (CB1) is the principal target of Δ9-tetrahydrocannabinol (THC), a psychoactive chemical from Cannabis sativa with a wide range of…”
Get full text
Journal Article -
2
Fulfilling the Promise of "Biased" G Protein-Coupled Receptor Agonism
Published in Molecular pharmacology (01-09-2015)“…The fact that over 30% of current pharmaceuticals target heptahelical G protein-coupled receptors (GPCRs) attests to their tractability as drug targets…”
Get more information
Journal Article -
3
Toward Directing Opioid Receptor Signaling to Refine Opioid Therapeutics
Published in Biological psychiatry (1969) (01-01-2020)“…The mu opioid receptor (MOR) is a diversely regulated target for the alleviation of pain in the clinical setting. However, untoward side effects such as…”
Get full text
Journal Article -
4
Bias Factor and Therapeutic Window Correlate to Predict Safer Opioid Analgesics
Published in Cell (16-11-2017)“…Biased agonism has been proposed as a means to separate desirable and adverse drug responses downstream of G protein-coupled receptor (GPCR) targets. Herein,…”
Get full text
Journal Article -
5
Crystal structures of agonist-bound human cannabinoid receptor CB1
Published in Nature (London) (27-07-2017)“…Crystal structures of the human cannabinoid receptor 1 (CB 1 ) bound to the agonists AM11542 and AM841 reveal notable structural rearrangements upon receptor…”
Get full text
Journal Article -
6
Activation and Signaling Mechanism Revealed by Cannabinoid Receptor-Gi Complex Structures
Published in Cell (20-02-2020)“…Human endocannabinoid systems modulate multiple physiological processes mainly through the activation of cannabinoid receptors CB1 and CB2. Their high sequence…”
Get full text
Journal Article -
7
Crystal Structure of the Human Cannabinoid Receptor CB2
Published in Cell (24-01-2019)“…The cannabinoid receptor CB2 is predominately expressed in the immune system, and selective modulation of CB2 without the psychoactivity of CB1 has therapeutic…”
Get full text
Journal Article -
8
Community guidelines for GPCR ligand bias: IUPHAR review 32
Published in British journal of pharmacology (01-07-2022)“…GPCRs modulate a plethora of physiological processes and mediate the effects of one‐third of FDA‐approved drugs. Depending on which ligand activates a…”
Get full text
Journal Article -
9
Functional selectivity of GPCR signaling in animals
Published in Current opinion in cell biology (01-04-2014)“…Graphical abstract…”
Get full text
Journal Article -
10
The role of beta-arrestin2 in the severity of antinociceptive tolerance and physical dependence induced by different opioid pain therapeutics
Published in Neuropharmacology (01-01-2011)“…Ligands acting at the same receptor can differentially activate distinct signal transduction pathways, which in turn, can have diverse functional consequences…”
Get full text
Journal Article -
11
Biased agonists of the kappa opioid receptor suppress pain and itch without causing sedation or dysphoria
Published in Science signaling (29-11-2016)“…Agonists targeting the kappa opioid receptor (KOR) have been promising therapeutic candidates because of their efficacy for treating intractable itch and…”
Get more information
Journal Article -
12
Agonist-directed signaling of the serotonin 2A receptor depends on β-arrestin-2 interactions in vivo
Published in Proceedings of the National Academy of Sciences - PNAS (22-01-2008)“…Visual and auditory hallucinations accompany certain neuropsychiatric disorders, such as schizophrenia, and they also can be induced by the use or abuse of…”
Get full text
Journal Article -
13
Comparison of morphine, oxycodone and the biased MOR agonist SR-17018 for tolerance and efficacy in mouse models of pain
Published in Neuropharmacology (01-03-2021)“…The mu opioid receptor-selective agonist, SR-17018, preferentially activates GTPγS binding over βarrestin2 recruitment in cellular assays, thereby…”
Get full text
Journal Article -
14
Development of Functionally Selective, Small Molecule Agonists at Kappa Opioid Receptors
Published in The Journal of biological chemistry (20-12-2013)“…The kappa opioid receptor (KOR) is widely expressed in the CNS and can serve as a means to modulate pain perception, stress responses, and affective reward…”
Get full text
Journal Article -
15
5-HT1A Autoreceptors in the Dorsal Raphe Nucleus Convey Vulnerability to Compulsive Cocaine Seeking
Published in Neuropsychopharmacology (New York, N.Y.) (01-04-2016)“…Cocaine addiction and depression are comorbid disorders. Although it is well recognized that 5-hydroxytryptamine (5-HT; serotonin) plays a central role in…”
Get full text
Journal Article -
16
Desensitization of G protein-coupled receptors and neuronal functions
Published in Annual review of neuroscience (01-01-2004)“…G protein-coupled receptors (GPCRs) have proven to be the most highly favorable class of drug targets in modern pharmacology. Over 90% of nonsensory GPCRs are…”
Get full text
Journal Article -
17
A Route to Potent, Selective, and Biased Salvinorin Chemical Space
Published in ACS central science (23-08-2023)“…The salvinorins serve as templates for next generation analgesics, antipruritics, and dissociative hallucinogens via selective and potent agonism of the…”
Get full text
Journal Article -
18
Hyperactivity in Mice Induced by Opioid Agonists with Partial Intrinsic Efficacy and Biased Agonism Administered Alone and in Combination with Morphine
Published in Biomolecules (Basel, Switzerland) (01-06-2023)“…Opioid analgesics such as morphine and fentanyl induce mu-opioid receptor (MOR)-mediated hyperactivity in mice. Herein, we show that morphine, fentanyl,…”
Get full text
Journal Article -
19
GIRK channel modulation by assembly with allosterically regulated RGS proteins
Published in Proceedings of the National Academy of Sciences - PNAS (04-12-2012)“…G-protein–activated inward-rectifying K ⁺ (GIRK) channels hyperpolarize neurons to inhibit synaptic transmission throughout the nervous system. By accelerating…”
Get full text
Journal Article -
20
Opioid receptor homo- and heterodimerization in living cells by quantitative bioluminescence resonance energy transfer
Published in Molecular pharmacology (01-06-2005)“…Opioid receptors have been shown to dimerize or oligomerize among themselves and each other, affecting their functional properties. This study used…”
Get more information
Journal Article