• The stability and function of the

  2022-04-07

  

  The stability and function of the HIF-1α protein are affected by many post-translational modifications (PTMs), including hydroxylation, acetylation, ubiquitination and SUMOylation [[29], [30], [31]]. It has been shown that HIF-1α stability is regulated by LSD1 [25]; in particular, the Set9 histone m

• Beside its role in NF

  2022-04-06

  

  Beside its role in NF-κB and IL-1β activation, the NRLP3 pathway is closely involved in another essential pathophysiologic mechanism such as the cellular calcium homeostasis. Full activation of the NRLP3 inflammasome requires decreased extracellular K concentrations resulting in decreased osmotic pr

• br GPR a G protein coupled

  2022-04-06

  

  GPR35, a G protein-coupled receptor (GPCR), was discovered and classified as an orphan GPCR in 1998 and deorphanized in 2006 by the discovery of kynurenic α-mangostin as the endogenous agonist. Since its discovery, limited references on the GPR35 receptor have appeared, due in part to a scarcity

• In summary we have designed and optimized a

  2022-04-06

  

  In summary, we have designed and optimized a new series of 1,4-dioxycyclohexane GPR119 agonists. SAR studies led to the discovery of the preferred molecule that has potent and efficacious GPR119 activity across species. This lead compound exhibited an excellent ADME and safety profile, and demonstra

• CD binding to gp causes a

  2022-04-06

  

  CD4 binding to gp120 causes a large scale conformational change of gp120 which involves the gp120 core structure and the transitions of inner-domain layers (layer 1, 2 and 3), but also involves the movement of the major loops (V1, V2 and V3) [16], [17], [18], [19]. For instance, the V2-loop joins th

• However the GPR R H polymorphism

  2022-04-06

  

  However, the GPR40 R211H polymorphism was reported to affect the variation of insulin secretory capacity in other ethnic groups. The allele frequency of H211 in Japanese was 78.4%.102, 103 By comparing clinical and metabolic parameters among Japanese men, Ogawa et al. found that histidine homozygote

• Tail group SAR of the imidazole

  2022-04-06

  

  Tail group SAR of the imidazole derived analogs is shown in . The previous SAR study from the discovery of AMG 837 revealed that a simple un-substituted meta-biphenyl tail group was less favorable in terms of potency. Efforts to introduce polarity to the tail group were not successful. When a methyl

• To further implicate the role of EAAT in morphine

  2022-04-06

  

  To further implicate the role of EAAT3 in morphine-induced place preference, the effects of morphine on EAAT3 gdc-0980 was determined. Interestingly, morphine increased EAAT3 protein expression in the plasma membrane of mPFC, nucleus accumbens and VTA but not in the hippocampus of wild-type mice at

• While TUNEL staining is traditionally thought to be an apopt

  2022-04-06

  

  While TUNEL staining is traditionally thought to be an apoptosis marker, studies have shown that TUNEL can stain necrotic SGC-CBP30 [19], [20], [21]. Furthermore, DNA degradation has also been observed in necrotic cells [22]. TUNEL staining alone is therefore insufficient to distinguish apoptosis fr

• Although GLP has greater insulin releasing effects at

  2022-04-06

  

  Although GLP-1 has greater insulin-releasing effects at pharmacological concentrations [10], it is apparent that the higher circulating concentrations of GIP combined with more pronounced increase in secretion following feeding make GIP the major physiological incretin [7], [11]. The peptide exerts

• In summary the SAR of

  2022-04-06

  

  In summary, the SAR of a series of phenylpropanoic acid-free fatty Stiripentol synthesis receptor agonists is described which resulted in the identification of potent FFA4 agonists. The superior pharmacokinetic properties of compound led to its selection as an in vivo tool compound which afforded

• Earlier we have showed that

  2022-04-02

  

  Earlier we have showed that tumor associated sFas mRNA isoform profile and splicing factors expression levels in solid tumors do not correspond to profiles that are observed in cell lines [45]. In the present study, for the first time we show that Fas but not Rac1 pre-mRNA's alternative splicing is

• br Introduction br Results br Discussion br Experimental

  2022-04-02

  

  Introduction Results Discussion Experimental Acknowledgment Introduction Endocannabinoids, N-arachidonoylethanolamine (AEA) and 2-arachidonoylglycerol (2-AG) have been found in most mammalian tissues and they stimulate cannabinoid CB1 and CB2 receptor activity thereby modulating se

• H O induced astrocyte ATP release through

  2022-04-02

  

  H2O2 induced astrocyte ATP release through lysosome exocytosis. The LDH assay and electric microscope results indicated that the increase of extracellular ATP concentration was not due to the cell rupture, but the alternations in cell activities. In addition, when lysosome exocytosis was blocked by

• Benztropine mesylate australia This crosstalk may be respons

  2022-04-02

  

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

14781 records 456/986 page Previous Next First page 上5页 456457458459460 下5页 Last page