• Phagosomes acquire some hydrolases early during

  2024-10-09

  

  Phagosomes acquire some hydrolases early during their journey from the cell surface to lysosomes. An example for such hydrolase is cathepsin H which is most concentrated in the early phagosome at a pH of approximately 6.3 (Claus et al., 1998), the pH optimum of enzyme activity (Schwartz and Barrett,

• Whole body loss of ACLY is early embryonic lethal indicating

  2024-10-09

  

  Whole-body loss of ACLY is early embryonic lethal, indicating that it serves non-redundant roles during development (Beigneux et al., 2004). Silencing or inhibition of ACLY suppresses the proliferation of many cancer cell lines and impairs tumor growth (Bauer et al., 2005, Hanai et al., 2012, Hatziv

• A high throughput screening campaign led to the discovery

  2024-10-09

  

  A high-throughput screening campaign led to the discovery of the first series of both potent and selective ATR kinase inhibitors by Vertex Pharmaceuticals (Charrier et al., 2011). One of these compounds, VE-821, was shown to be a potent ATP-competitive inhibitor of ATR with minimal cross-reactivity

• br Aromatase the key enzyme for

  2024-10-09

  

  Aromatase: the key enzyme for estrogen formation in adipose tissue Estrogens are synthesized from androgens by aromatase, a member of the cytochrome P450 superfamily, which is the rate-limiting enzyme in estrogen biosynthesis (Santen et al, 2009, Simpson et al, 1994). At the cellular level, aroma

• Torin1 br Materials and methods br Results br

  2024-10-09

  

  Materials and methods Results Discussion Pulmonary fibrosis is a progressive and chronic lung disease and its typical features include Torin1 proliferation, epithelial injury, chronic interstitial inflammation, increased extracellular matrix (ECM) production, and collapse of alveoli, all of

• br Introduction Sustained over activation of neurohormonal s

  2024-10-09

  

  Introduction Sustained over-activation of neurohormonal systems is a hallmark in the pathophysiology of cardiac dysfunction following myocardial infarction (MI) and heart failure (HF). Inhibitors of the renin-angiotensin mrna protein synthesis system (RAAS) constitute cornerstones of pharmacothe

• br Materials and Methods br Results

  2024-10-08

  

  Materials and Methods Results In the Base Analysis (53% of patients having access to the ALK test in both Current and Alternative Scenarios), a total of 16,583 patients were tested of whom 1,252 were assumed to be ALK-positive. A more extensive use of Ventana in the Alternative Scenario determ

• Since natural and recombinant glycoprotein hormones exhibit

  2024-10-08

  

  Since natural and recombinant glycoprotein hormones exhibit some differences in their carbohydrate structures, we checked whether this could affect the permissive effect on FSK-induced cyclic AMP response in MLTC-1 cells. Fig. 6 shows that the same sensitizing effect to FSK is observed with pituitar

• ADORs accomplish a variety of physiological effects

  2024-10-08

  

  ADORs accomplish a variety of physiological effects in different tissues. In neurons, ADORs regulate the release of neurotransmitters such as dopamine and glutamate (Ferré et al., 1992; Fredholm and Dunwiddie, 1988; Ginsborg and Hirst, 1972; Gonçalves et al., 2015; Quarta et al., 2004; Stella et al.

• br Materials and methods br Results The determination of

  2024-10-08

  

  Materials and methods Results The determination of the intrinsic inhibitory potential of the oximes HI-6 and MMB-4 with human and guinea pig AChE revealed marked differences between both oximes (Table 1). MMB-4 had an only marginal effect on both AChE species, calculated IC50 of >1000μM, while

• The geometry of two three four and

  2024-10-08

  

  The geometry of two, three, four and five Cy7.5 maleimide(non-sulfonated) neutral radical ACh molecule complexes with various electronic configurations, i.e. with various multiplicities equal to 1, 2 and 4 (for ACh trimer) were determined using DFT with the unrestricted B97d/SVP potential/basis set

• Although effects of low concentrations of agonist were not a

  2024-10-08

  

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

• br lipoxygenase pathway in brain aging

  2024-10-08

  

  5-lipoxygenase pathway in histamine receptors aging and alzheimer’s disease 5LO is found throughout the central nervous system, in both neuron and glia cells (Farias et al., 2007). However, its expression levels are highest in the cortex and hippocampus areas, two regions that are particularly vu

• Receptors containing an x y subunit interface

  2024-10-08

  

  Receptors containing an αx/γy subunit interface, where x=1, 2, 3, 5 and y=1–3, form a high-affinity binding site for benzodiazepines (Figure 1A), for the later developed Z-drugs of different chemotypes, and for a large number of chemically distinct research compounds 17, 18 (Box 1 for examples). For

• Fourth non canonical sites may be targeted Classical benzodi

  2024-10-08

  

  Fourth, non-canonical sites may be targeted. Classical benzodiazepines require the presence of a γ subunit for high-affinity binding, which limits their activity to a specific large pool of receptor isoforms, leaving other isoforms unaffected. In particular, δ subunit-containing receptors, as well a

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