• As an alternative to chronic receptor blockade we have been

  2024-01-23

  

  As an alternative to chronic receptor blockade, we have been targeting adenosine kinase (ADK) – an astrocyte-based enzyme that catalyses the phosphorylation of adenosine, as a means to modify 873 adenosinergic signalling (Boison, 2006, Etherington et al., 2009). Up-regulating ADK facilitates the cle

• The physiological effect of adenosine is

  2024-01-23

  

  The physiological effect of adenosine is now considered a new direction in halting the progression of organ damage in cardiovascular disease [24], [25], [26]. Adenosine has diverse functions, depending on its interaction with different receptor subtypes: A1, A2A, A2B, and A3[24], [25], [26]. Stimula

• Ten strains of lactobacilli TMW isogenic with strain

  2024-01-23

  

  Ten strains of lactobacilli: TMW 1.1434 (isogenic with strain F19 ), TMW 1.1733 (isolated from fermented food), TMW 1.1628 (isolated from baby feces), TMW 1.1609 (isolated from baby feces), TMW 1.1734 (isolated from fermented food), TMW 1.313 (isolated from non-pasteurized Heineken beer), TMW

• Although effects of low concentrations of agonist were not

  2024-01-23

  

  Although effects of low concentrations of agonist were not as thoroughly documented for heteromeric receptors such as the major Senexin B α4β2 nAChR, a similar mechanism of action was described to explain the potentiation of these receptors with low concentrations of acetylcholine-esterase-inhibiti

• br Experimental procedure br Introduction Migraine is a debi

  2024-01-23

  

  Experimental procedure Introduction Migraine is a debilitating neurovascular disorder characterized by recurring unilateral pulsating headaches of moderate to severe intensity, associated with nausea, photophobia and/or phonophobia, lasting from 4 to 72 h (Headache Classification Committee of

• The most potent compounds within the current series of

  2024-01-23

  

  The most potent compounds within the current series of compounds were therefore , , , , and , with Cyclophosphamide mg possessing the best selectivity towards the lyase reaction in comparison to the hydroxylase reaction, indeed, this compound was found to possess an IC value of 1210nM against the 17

• The introduction of a pyrazole moiety into any position

  2024-01-23

  

  The introduction of a pyrazole moiety into any position of the sterane core by cross-coupling reactions [13] or by Knorr construction from a CCC bis-electrophilic sterane precursor and an N,N binucleophile building block [17], [19] may serve as an example. Very few reports are to be found, however,

• At present drugs that specifically inhibit YAP

  2024-01-23

  

  At present, drugs that specifically inhibit YAP activity are not available. In fact, verteporfin, which was originally described as a specific inhibitor of YAP-TEAD interaction, has been recently shown to exert its activity through selective induction of proteotoxicity rather than through YAP inhibi

• br Conflict of interest br

  2024-01-23

  

  Conflict of interest Acknowledgements We thank Ann Jackman, Mike Ormerod and members of Julian Downward's and Alan Ashworth's groups for helpful discussions. This work was supported by grant number PEM/GME/D391/40 from the Kidani Trust (S. Kaye) and by Keele University. Introduction Autota

• Elevated expression of Aurora A and B

  2024-01-23

  

  Elevated expression of Aurora-A and -B frequently detected in a wide variety of human cancers strongly indicate that high expression of these kinases play roles in the development of cancer associated phenotypes. While Aurora-A has been shown to function as an oncogene when over expressed in mammali

• Aurora kinases are a conserved family of serine threonine ki

  2024-01-23

  

  Aurora kinases are a conserved family of serine/threonine kinases that are important for the transition through mitosis and amplification and overexpression of Aurora kinases have been implicated in Carmustine synthesis and transformation. Aurora B is located at the centromere and controls aspects

• Several structural classes of ASK

  2024-01-23

  

  Several structural trifluoperazine of ASK1 inhibitors, mostly from industry but also from academia, have been identified over the last decade. In 2012, Terao et al. (Takeda) reported imidazo[1,2-α]pyridine () as a potent ASK1 inhibitor derived from structure-based drug design. GSK, Merck and Gilea

• br Introduction Arginase deficiency is a rare

  2024-01-23

  

  Introduction Arginase deficiency is a rare metabolic disorder resulting from a loss of arginase 1 (ARG1), the final enzyme in the urea cycle, which is the major pathway for the detoxification of ammonia in terrestrial mammals. ARG1 is expressed most prevalently in hepatocytes and red blood cells.

• Similar studies in Swedish Mutation of

  2024-01-23

  

  Similar studies in Swedish Mutation of APP AD transgenic mice revealed reduced dynamin 1, AP180, and synaptophysin expression in the hippocampus, particularly prominent in the CA1 and CA4 subfields [19]. These findings imply that Aβ can act not only as a modulator of exocytosis but is a potent regul

• In this study an in vitro AChE

  2024-01-22

  

  In this study, an in vitro AChE inhibition assay combined with UF-HPLC-ESI-Q-TOF/MS method was developed for rapid screening and identification of AChEI from the roots of C. chinensis Franch. Five compounds was found with AChE inhibitory activity and identified by the on-line DAD-ESI-Q-TOF/MS compar

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