• In the case of DIA CN the docking

  2024-01-13

  

  In the case of DIA-4CN the docking results do not show any interaction between the iron atom and the inhibitor, presumably due to the reduced ability to form a complex involving the -CONN- moiety versus the bidentate -CONHNH- central group of HYD-4Me. This results in a considerable gap between the i

• A high throughput screening campaign led to the discovery

  2024-01-13

  

  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

• The class C receptors also share a

  2024-01-13

  

  The class C receptors also share a common agonist-binding mode. In all cases, an agonist induces VFT closure by forming intermolecular bonds with surface residues in both the LB1 and LB2 domains (Geng et al., 2013, Geng et al., 2016, Kunishima et al., 2000, Muto et al., 2007, Nuemket et al., 2017, T

• Furthermore we also found that the basic

  2024-01-13

  

  Furthermore, we also found that the basic level of ROS was markedly lower in mtDNA-reduced SW480 ticarcillin synthesis than that in the parent cells. Endogenous ROS is most notably produced at the sites of complex I and complex III [5], it might be plausible that the decreased quantity of ROS obser

• Negative regulation of AR expression by NF B

  2024-01-12

  

  Negative regulation of AR expression by NFκB was also correlated with the ‘age-dependent desensitisation’ of androgen action in the rat liver (Supakar et al., 1995). In this case the binding site was mapped upstream of the gene to sequences −555 to −565 bp, that binds heterodimers of p65 and p50, as

• The specific functions of ERs and AR

  2024-01-12

  

  The specific functions of ERs and AR underline their crucial roles during different phases of spermatogenesis. Their deregulation could affect numerous downstream targets, thereby, disrupting spermatogenesis and male fertility. Various studies have shown that estrogen-like chemicals in the environme

• Immunohistochemistry in tissue samples showed the expression

  2024-01-12

  

  Immunohistochemistry in tissue samples showed the expression of several nuclear receptor co-activators, including NCOA1, NCOA2, NCOA3, CREBBP, and EP300, in 85–100% of induced pluripotent stem cell tumors even some of which lacked AR expression (Boorjian et al., 2009). Knockdown of each co-activato

• This evidence suggests the strong clinical relevance of the

  2024-01-12

  

  This evidence suggests the strong clinical relevance of the identification of acquired resistance mechanisms for a proper therapeutic decision in patients with ALK-rearranged NSCLC. When the tissue is not available, the analysis of circulating tumor DNA (cfDNA) can be a valid alternative for the det

• Bupivacaine HCl br Conflict of interest br Introduction The

  2024-01-12

  

  Conflict of interest Introduction The Piezo proteins, Piezo1/FAM38A and Piezo2/FAM38B, are multi-pass transmembrane proteins that have been identified as mechanically-activated (MA) homomultimeric, pore-forming ion channels [1,2]. Piezo1 is broadly expressed with its highest expression in blad

• The cavity volume of the binding pocket may differ not

  2024-01-12

  

  The cavity volume of the binding pocket may differ not only between species but also among various AhR/ARNT isoforms within a single species. It is noteworthy that even a single amino ep4 receptor substitution within a binding pocket may result in a change in the cavity volume. This, in turn, may a

• br ABCA modulates intracellular sphingolipid metabolism

  2024-01-12

  

  ABCA2 modulates intracellular sphingolipid metabolism in the LE/LY Recycling of plasma membrane lipids that occurs by constitutive endocytosis and vesicularization of complex glycolipids, complex sphingolipids and cholesterol as well as free cholesterol liberated from LDL after receptor-mediated

• Young et al described the role of adenine

  2024-01-12

  

  Young et al. [40] described the role of adenine monophosphate-activated protein kinase (AMPK) in the translocation of GLUT4 in the heart. The AMPK is activated during muscle contraction [74] by converting AMP to ATP. The adenosine analog, 5-aminoimidazole-4-carboxamide ribonucleotide (AICAR), is a c

• An alternative approach to the administration of ADO agonist

  2024-01-12

  

  An alternative approach to the administration of ADO agonists is to amplify the actions of endogenous ADO by inhibiting the ADO-metabolizing enzyme, ADO kinase (AK). Inhibition of AK has the net effect of potentiating the local concentration and the effects of ADO in the extracellular compartment. T

• Based on the improved characteristics

  2024-01-12

  

  Based on the improved characteristics of the mutant ECDs we proceeded to crystallization trials, starting with the β1-BPloop as the most promising. We obtained rod shaped hexagonal crystals reproducibly, but with moderate diffraction ability (Fig. 5). Furthermore, the crystals were sensitive in moun

• The present work has implications for our

  2024-01-12

  

  The present work has implications for our thinking about the effects of antidepressant (e.g. SSRIs) use on maternal care in depressed mothers which consist of approximately 10–20% of all mothers (Gjerdingen and Yawn, 2007, Susser et al., 2016), and more than 40% of depressed mothers are prescribed w

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