• Here we report discovery of highly selective

  2024-09-03

  

  Here we report discovery of highly selective pan-Aurora kinase inhibitors through phenotypic screening. The co-crystal structure of C527 bound in the ATP binding site of Aurora A is described, and provides insight into the possible structural basis for the selectivity of the interaction. To ident

• As cytosolic acetyl CoA levels in hepatocytes descend cellul

  2024-09-03

  

  As cytosolic acetyl-CoA levels in hepatocytes descend, cellular production and concentration of cholesterol go down, a change that is known to be sensed by the Sterol response element binding protein (SREBP)/Cleavage-Activating Protein system, leading to SREBP escort to the Golgi apparatus, cleavage

• The mitogen activated protein kinase MAPK

  2024-09-03

  

  The mitogen-activated protein kinase (MAPK) plays an important role in a variety of cell processes by controlling transcriptional or translational regulation [14]. There are three major MAPK family members that have been well characterized: extracellular signal-regulated kinase (ERK), c-Jun N-termin

• Recently competitive inhibitors of arginase have been develo

  2024-09-03

  

  Recently, competitive inhibitors of arginase have been developed which have greater specificity for the enzyme. Initial development of these compounds involved determination of the crystal structure of arginase. Christianson and colleagues found that a binuclear manganese cluster was required for ca

• However one should keep in mind that

  2024-09-02

  

  However, one should keep in mind that these results may not reflect exactly in vivo antioxidant activity. Many other issues such as absorption, metabolism and physicochemical properties of different antioxidants must also be considered (Prior et al., 2007, Wu et al., 2004). Some research groups are

• In order to further explore whether

  2024-09-02

  

  In order to further explore whether the cytoprotective effect of isogarcinol against oxidative stress in H2O2-induced HepG2 hpdp australia is a consequence of the breakdown of the endogenous antioxidant defence mechanism, we measured the LDH release, MDA levels, GSH levels and SOD activity. A large

• Treatment of RAW cells with

  2024-09-02

  

  Treatment of RAW264.7 CGS 35066 mg with AP(+)-exosomes caused an increase in their phagocytic activity. In the presence of amastatin, phagocytic activity was not completely suppressed, suggesting that at least two components were responsible for the activity; one of which is aminopeptidase(s). When

• Our results add to previously published

  2024-09-02

  

  Our results add to previously published data on the contribution of ALDH3A1 to the optical properties of the cornea. Specifically, the study by Nees et al. (2002) was among the first to examine whether ALDH3A1 serves as a structural component in the cornea and similarly to lens crystallins. Their ex

• The direction of glutamate transport by

  2024-09-02

  

  The direction of glutamate transport by the cell membrane transporter is reversible. As mentioned above, glutamate transport is an electrogenic process associated with a transmembrane ion gradient established by the Na+-K+ pump through hydrolysis of adenosine triphosphate. Under conditions of energy

• Lithium Citrate synthesis To examine whether the interaction

  2024-09-02

  

  To examine whether the interaction between mGlu7 and α1-adrenergic receptors could be confirmed at a behavioural level, we performed the FST in mice. This test has value in predicting the antidepressant-like effect of drugs or environmental manipulations (Krishnan and Nestler, 2008, Krishnan and Nes

• The obtained results indicate that even

  2024-08-31

  

  The obtained results indicate that even when the impairment of the same forms of memory are present, amnesia can develop in different ways. Impairment of memory reconsolidation in the conditioned food aversion model through both the serotonin receptor antagonist and the antagonist of NMDA glutamate

• In the late s Solvay Pharmaceuticals discontinued the Phase

  2024-08-31

  

  In the late ‘90s, Solvay Pharmaceuticals discontinued the Phase 2 development of a promising potent and highly selective A1AR antagonist based on the pyrrolopyrimidine scaffold, SLV320 [43] (2, Chart 1, also named derenofylline; Ki hA1AR = 1 nM), for the treatment of acute heart failure [24]. In the

• br Introduction Adenosine deaminase ADA also

  2024-08-31

  

  Introduction Adenosine deaminase (ADA), also known as adenosine aminohydrolase, is a key enzyme involved in the purine metabolism that converts adenosine to inosine irreversibly (Lupidi et al., 1997). It is a zinc containing metalloenzyme present in both prokaryotes and eukaryotes. In humans ADA

• Targeting the BCR is the ideal strategy to identify

  2024-08-31

  

  Targeting the BCR is the ideal strategy to identify the antigen reactive B cells. However, there is concern that B cells could be activated when BCR are bound and cross-linked by antigens, a possibility that is obviously negative for the treatment of autoimmune disease. Proby et al. (2000) tried to

• Introduction Myasthenia gravis MG is an

  2024-08-31

  

  Introduction Myasthenia gravis (MG) is an autoimmune disorder characterized by muscle weakness, which is mainly due to autoantibodies reducing the number or function of postsynaptic tak1 inhibitor receptors (AChRs) [1], [2]. Animal models have been developed to uncover the immunopathogenesis of MG

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