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6,716 results
  • Opioid signaling and design of analgesics. [Journal Article]
    Prog Mol Biol Transl Sci. 2023; 195:153-176.Paul B, Sribhashyam S, Majumdar S
  • Clinical treatment of acute to severe pain relies on the use of opioids. While their potency is significant, there are considerable side effects that can negatively affect patients. Their rise in usage has correlated with the current opioid epidemic in the United States, which has led to more than 70,000 deaths per year (Volkow and Blanco, 2021). Opioid-related drug development aims to make targe…
  • Ciliary signaling proteins are mislocalized in the brains of Bardet-Biedl syndrome 1-null mice. [Journal Article]
    Front Cell Dev Biol. 2022; 10:1092161.Stubbs T, Bingman JI, … Mykytyn K
  • In the brain, primary cilia are found on most, if not all, central neurons. The importance of neuronal cilia is underscored by the fact that human diseases caused by primary cilia dysfunction, which are known as ciliopathies, are associated with neuropathologies, including neuropsychiatric disorders and learning and memory deficits. Neuronal cilia are enriched for certain G protein-coupled recept…
  • Cannabinoid tolerance in S426A/S430A x beta-arrestin 2 knock-out double mutant mice. [Journal Article]
    J Pharmacol Exp Ther. 2023 Jan 20 [Online ahead of print]Piscura MK, Sepulveda DE, … Morgan DJ
  • Tolerance to compounds that target G protein-coupled receptors (GPCR), such as the cannabinoid type-1 receptor (CB1R), is in part facilitated by receptor desensitization. Processes that mediate CB1R desensitization include phosphorylation of CB1R residues S426 and S430 by a GPCR kinase (GRK), and subsequent recruitment of the b-arrestin2 scaffolding protein. Tolerance to cannabinoid drugs is redu…
  • New simulation insights on the structural transition mechanism of bovine rhodopsin activation. [Journal Article]
    Proteins. 2023 Jan 11 [Online ahead of print]Damodaran K, Khan T, … Sudandiradoss C
  • Inactive rhodopsin can absorb photons, which induces different structural transitions that finally activate rhodopsin. We have examined the change in spatial configurations and physicochemical factors that result during the transition mechanism from the inactive to the active rhodopsin state via intermediates. During the activation process, many existing atomic contacts are disrupted, and new one…
  • Using canavanine resistance to measure mutation rates in Schizosaccharomyces pombe. [Journal Article]
    PLoS One. 2023; 18(1):e0271016.Pai CC, Heitzer E, … Kearsey SE
  • We constructed a panel of S. pombe strains expressing DNA polymerase ε variants associated with cancer, specifically POLES297F, POLEV411L, POLEL424V, POLES459F, and used these to compare mutation rates determined by canavanine resistance with other selective methods. Canavanine-resistance mutation rates are broadly similar to those seen with reversion of the ade-485 mutation to adenine prototroph…
  • Impact of membrane lipid polyunsaturation on dopamine D2 receptor ligand binding and signaling. [Journal Article]
    Mol Psychiatry. 2023 Jan 06 [Online ahead of print]Jobin ML, De Smedt-Peyrusse V, … Trifilieff P
  • Increasing evidence supports a relationship between lipid metabolism and mental health. In particular, the biostatus of polyunsaturated fatty acids (PUFAs) correlates with some symptoms of psychiatric disorders, as well as the efficacy of pharmacological treatments. Recent findings highlight a direct association between brain PUFA levels and dopamine transmission, a major neuromodulatory system i…
  • [β-arrestin2 recruitment by β-adrenergic receptor agonists and antagonists]. [Journal Article]
    Sheng Li Xue Bao. 2022 Dec 25; 74(6):993-1004.Wang YR, Cheng DQ, … Liu X
  • A large number of β-adrenergic receptor (β-AR) agonists and antagonists are widely used in the treatment of cardiovascular diseases and other diseases. Nonetheless, it remains unclear whether these commonly used β-AR drugs can activate downstream β- arrestin-biased signaling pathways. The objective of this study was to investigate β-arrestin2 recruitment effects of β-AR agonists and antagonists t…
  • Structural basis for Y2 receptor-mediated neuropeptide Y and peptide YY signaling. [Journal Article]
    Structure. 2023 Jan 05; 31(1):44-57.e6.Kang H, Park C, … Choi HJ
  • Neuropeptide Y (NPY) and its receptors are expressed in various human tissues including the brain where they regulate appetite and emotion. Upon NPY stimulation, the neuropeptide Y1 and Y2 receptors (Y1R and Y2R, respectively) activate GI signaling, but their physiological responses to food intake are different. In addition, deletion of the two N-terminal amino acids of peptide YY (PYY(3-36)), th…
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