• br Conflict of interest br Supplementary methods and materia

  2020-08-14

  

  Conflict of interest Supplementary methods and materials Acknowledgments This work was supported by an Early Career Researcher grant awarded by the Institute of Health and Biomedical Innovation to IMW and Queensland University of Technology, and grants awarded to SS by the Prostate Cancer F

• br Halogenases Enzymatic C H activation leading to

  2020-08-14

  

  Halogenases Enzymatic C–H activation leading to halogenation is another emerging area in biocatalysis [55,56]. Incorporation of halogen atoms during medicinal chemistry eff ;orts is a well-established practice, presenting an effective means to control the molecule’s bioactivity and physicochemical

• A growing number of other post translational modifications a

  2020-08-14

  

  A growing number of other post-translational modifications are implicated in regulation of the ubiquitin system, including substrate modification by hydroxylation, glycosylation, acetylation, methylation, modification by poly(ADP-ribose) (PAR), and attachment of ubiquitin-like modifiers. The HIF1-α

• Similarly synthetic analogs of Alogliptin by replacing the

  2020-08-14

  

  Similarly synthetic analogs of Alogliptin by replacing the cyanobenzyl group with the butynyl group have been synthesized and tested as selective DPP-4 inhibitors [7], [8]. Additionally, quinazolines [9], [10], pyridopyrimidinediones [11], pyrazolopyrimidinones [12] and pyrimidines [13] as DPP-IV in

• Since both the Ub and ISG systems are crucial for

  2020-08-14

  

  Since both the Ub and ISG15 systems are crucial for the innate immune response, many prokaryotic and viral pathogens have evolved ways to hijack them in order to create a “window-of-opportunity” for efficient replication. Several viral and bacterial proteins have been found to directly target these

• br Methods br Results br Discussion MEN is a

  2020-08-14

  

  Methods Results Discussion MEN91507 is a potent and selective CysLT1 receptor antagonist. Guinea-pig lung membranes have been widely used for the detection and characterization of CysLT1 receptor antagonists: in this assay the high affinity (subnanomolar) binding of [3H[leukotriene D4 or [3

• In a study on the time course of

  2020-08-14

  

  In a study on the time course of a mechanism-based inactivation of CYP3A by HIV protease inhibitors, Katzenmaier et al. [37] reported that the suppression of CYP3A activity continued for threedays after the discontinuation of ritonavir. In the present study, the CYP3A activity on day 28 after a seve

• 132 6 br Materials and methods br Results

  2020-08-13

  

  Materials and methods Results and discussion Conclusions Data about the ability of non-conventional ligands to operate class-A GPCRs have been accumulating. Specifically, increasing evidence indicates that oxysterols, oxidized derivatives of cholesterol, are involved in many activities that

• Proof of concept studies with disulfiram suggest the potenti

  2020-08-13

  

  Proof-of-concept studies with disulfiram suggest the potential utility of DβH inhibitors for treatment of cocaine use disorder. In a study of 74 subjects stabilized on methadone and randomized into disulfiram and placebo groups for 10weeks, disulfiram treatment reduced cocaine-positive urines, and d

• br Introduction br Sphingolipid metabolism Sphingolipids are

  2020-08-13

  

  Introduction Sphingolipid metabolism Sphingolipids, are fundamental constituents of all eukaryotic membranes and their metabolism is carried out by a broad array of anabolic and DL-Dithiothreitol with ceramide as their hub (for a review, (Hannun and Obeid, 2018)). Ceramide can be formed by mu

• br Experimental procedures br Introduction Protein kinases r

  2020-08-13

  

  Experimental procedures Introduction Protein kinases represent one of the largest enzyme XMD8-92 in the human genome and act as signaling mediators in a variety of cellular processes (Manning et al., 2002). Because many diseases are associated with aberrant protein kinase activity, targeted k

• br Results br Discussion br Experimental Procedures br Ackno

  2020-08-13

  

  Results Discussion Experimental Procedures Acknowledgments In the preceding paper, we reported 3-amido-4-anilinoquinolines as highly selective inhibitors of CSF-1R kinase, along with our initial efforts to optimize the series. Examples from the 6,7-dimethoxyquinoline series were very p

• br Results br Discussion GPCRs recognize a

  2020-08-13

  

  Results Discussion GPCRs recognize a broad range of molecules with a vast chemical boc boc through different mechanisms. Our understanding of the recognition of lipid mediators by GPCRs primarily comes from the structural studies of receptors for lysophospholipids and endocannabinoids includi

• br Role of CRF receptors in the BNST in stress

  2020-08-13

  

  Role of CRF1 receptors in the BNST in stress-induced relapse to cocaine seeking The seminal work of Stewart and co-workers [19] showed that rats that have extinguished their auto-administration of different drugs of abuse relapse to drug-seeking behaviour when exposed to footshock, even after a 4

• Based on the ability of CRF to modulate nociception

  2020-08-13

  

  Based on the ability of CRF to modulate nociception, we hypothesized that stress leads to hyperalgesia by the activation of CRF1 and/or CRF2 receptors in the spinal cord. We tested this hypothesis using an acute forced swim as a widely used and easily reproducible stressor and grip force as a measur

16148 records 806/1077 page Previous Next First page 上5页 806807808809810 下5页 Last page