• This crosstalk may be responsible for the

  2021-11-02

  

  This crosstalk may be responsible for the beneficial effects of histamine H2 receptor inverse agonists on bifonazole receptor pathologies and may also explain unwanted effects of these drugs on other tissues. In this way, Allen et al. reported an anaphylactoid reaction following cessation of high-d

• A similar symbiotic relationship has been reported in

  2021-11-02

  

  A similar symbiotic relationship has been reported in the brain, where increased gradients of lactate secreted by astrocytes enables neurons to import and use this nutrient, a process referred to the ‘neuron–astrocyte lactate shuttle’ [16]. Similarly, lactate-based metabolic coupling established b

• Recently a G protein coupled receptor GPR a was

  2021-11-02

  

  Recently, a G-protein-coupled receptor, GPR109a, was identified as a molecular target for niacin. Following this breakthrough, our group initiated a drug discovery program focused on the development of a high affinity ‘flush-free’ niacin-like agonist. Previously, we reported on the identification of

• br Significant efforts are currently focused

  2021-11-02

  

  Significant efforts are currently focused on non-dopaminergic strategies to address the unmet medical needs in schizophrenia, and targeting -methyl--aspartate (NMDA) article source hypofunction has garnered a great deal of attention., , Elevation of synaptic glycine levels near NMDA-containing syn

• Next we investigated the accumulation of

  2021-11-02

  

  Next, we investigated the accumulation of [3H]-ribavirin in fresh villous fragments of human placenta, which provide a physiologically relevant, well-described and validated model for assessing drug interactions with ENTs [32], [35], [69], [70]. The uptake of [3H]-ribavirin was time-dependent and si

• br Acknowledgements This work was financed by the projects M

  2021-11-02

  

  Acknowledgements This work was financed by the projects “Mejora Genética del Almendro” (MINECO-Spain, AGL2017-85042-R), “The molecular mechanisms to break flower bud dormancy in fruit trees” to RS-P within the Villum Young Investigator Program and by the VILLUM Research Center for Plant Plasticit

• A main finding of this study

  2021-11-02

  

  A main finding of this study was that the impact of exogenous insulin on hippocampal memory and glucose utilization was GluT4-dependent. Although insulin was administered directly to the hippocampus, it is important to point out that such administration does indeed have physiological relevance; that

• Nevertheless in the brain we found that trehalose phosphoryl

  2021-11-02

  

  Nevertheless, in the brain, we found that trehalose phosphorylates AMPK, which is a metabolic sensor. AMPK is known to be transiently activated in muscle by acute exercise [21,22]. Bayod et al. also reported that AMPK was significantly activated in both the cerebral cortex and hippocampus in exercis

• Sequences of hexokinases were initially deduced and predicte

  2021-11-02

  

  Sequences of hexokinases were initially deduced and predicted based on cDNA clones (Andreone et al., 1989, Schwab and Wilson, 1989, Schwab and Wilson, 1991, Griffin et al., 1991, Thelen and Wilson, 1991). Analysis of genome sequence data identified, in Ethacrynic Acid to the 4 expected known hexoki

• GOAT belongs to the super family of membrane bound

  2021-11-02

  

  GOAT belongs to the super family of membrane-bound O-acyltransferases (MBOATs). It is encoded by the gene MBOAT4 in human. The protein GOAT is highly conserved from zebrafish to human (Yanagi et al., 2018). GOAT is ubiquitously expressed with abundant expression in the stomach and intestine (Sakata

• 7112 mg Two excellent GSMs with clear pharmacological effect

  2021-11-02

  

  Two excellent GSMs with clear pharmacological effect across rats, dogs, monkeys, and human subjects are BMS-932481 and BMS-986133 with IC50 at 6.6 and 3.5 nM to reduce Aβ42, respectively. Both GSMs exhibit dose- and time-dependent activity in vivo by decreasing Aβ1-42 and Aβ1-40 levels while increas

• Trifluoromethyl ketones and fluorophosphates were the first

  2021-11-02

  

  Trifluoromethyl ketones and fluorophosphates were the first generation FAAH inhibitors identified. They showed good in vitro FAAH inhibition potency, but most of them exhibited poor selectivity for FAAH over other serine hydrolases (such as the triacylglycerol hydrolase and the membrane-associated h

• In addition to Rabs several proteins have been shown

  2021-11-01

  

  In addition to Rabs, several proteins have been shown to interact with Rabphilin3a, for instance the GluN2A subunit of the NMDA receptor, PSD-95 ([56,57] and references therein), Rabaptin-5, α-actinin [16] and SNAP-25 [21,23,41,61]. Only the latter has been reported to participate in the AR. Explori

• Aurora kinase B AURKB and

  2021-11-01

  

  Aurora kinase B (AURKB) and haploid cell-specific protein kinase (Haspin) are two well-known participants in N-terminal histone H3 phosphorylations during mitosis. A related role played by these kinases relates to the fact that AURKB is activated by Haspin promoted phosphorylation at T3. Irrespectiv

• GPR agonistic activity was evaluated for the human

  2021-11-01

  

  GPR119 agonistic activity was evaluated for the human GPR119 receptor in a cell-based cAMP assay. The results expressed the potency as EC values and the inherent activity (IA) as percentages which were compared to the test compound with oleoylethanolamide (OEA), an endogenous ligand of GPR119 (defin

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