• We have previously reported DAPK inhibitors discovered throu

  2020-07-13

  

  We have previously reported DAPK inhibitors discovered through our structure-based virtual screening (SBVS) research program. In this paper, we describe the general protocol of our in silico approach, and the strategy used to develop hit compounds. In addition, the studies conducted on the structure

• Cot MAP K is the sole MAP

  2020-07-13

  

  Cot (MAP3K8) is the sole MAP3K that activates the MEK1/2-Erk1/2 following the activation of the TLR/IL-1 receptor superfamily as well as some receptors of the TNF receptor family [8], [9], [10] and mediates the production of chemokines and cytokines in different cell systems [reviewed in [11]]. Thu

• Recoverin is a kDa retinal protein that binds to calcium

  2020-07-11

  

  Recoverin is a 23-kDa retinal protein that binds to calcium. It regulates the AZD6738 of rhodopsin during visual transduction within photoreceptor cells. Since the pathogenicity of anti-recoverin antibody is potent, anti-recoverin CAR patients often have progressive visual impairments, characterize

• Nimodipine is an L type calcium

  2020-07-11

  

  Nimodipine is an L-type calcium channel antagonist that reduces excessive calcium influx during pathological conditions, contributing to its neuroprotective properties (Zornow and Prough, 1996; Kobayashi and Mori, 1998). Autophagy can be induced by increased [Ca2+] (Rami et al., 2008). Nimodipine si

• The authentic PPase was purified from B subtilis as

  2020-07-11

  

  The authentic PPase was purified from B. subtilis as described previously [21], whereas the recombinant enzyme was purified to homogeneity from E. coli by a simplified procedure including only phenyl-Sepharose CL-4B column chromatography and DEAE-HPLC [21]. About 26 mg of pure enzyme was obtained fr

• Nociceptive and hyperalgesic actions of ET are produced thro

  2020-07-11

  

  Nociceptive and hyperalgesic actions of ET-1 are produced through ETA and ETB receptors. Previous reports indicate that ETA receptor antagonists in peripheral tissues are effective in inhibiting ET-1 induced hyperalgesia, and attenuation of neuropathic pain in rats [16]. Studies have also shown that

• In addition to vasoconstrictor actions acute effects ET exer

  2020-07-11

  

  In addition to vasoconstrictor actions (acute effects), ET-1 exerts potent mitogenic actions on vascular smooth muscle cells and cardiac myocytes (chronic effects), hence causing vascular and cardiac hypertrophy [19,24,25]. These effects are mediated via stimulation of either ETA or ETB receptors, a

• Our finding that activating DDR

  2020-07-11

  

  Our finding that activating DDR2 variants are a cause of this disease suggested that the ABL inhibitor dasatinib, a leukemia drug that also inhibits DDR2, could be used for treatment of affected individuals.10, 11 To examine the effect of dasatinib on p.Leu610Pro- and p.Tyr740Cys-induced autophospho

• Nimodipine is an L type calcium channel antagonist that redu

  2020-07-11

  

  Nimodipine is an L-type calcium channel antagonist that reduces excessive calcium influx during pathological conditions, contributing to its neuroprotective properties (Zornow and Prough, 1996; Kobayashi and Mori, 1998). Autophagy can be induced by increased [Ca2+] (Rami et al., 2008). Nimodipine si

• Stressful life events are modulators of mood and

  2020-07-10

  

  Stressful life events are modulators of mood and can trigger a variety of destructive behavior, including drug abuse and relapse in addicts (Association, 2013; Chen et al., 2012; Sinha, 2009). Likewise, drug-associated stimuli evoke a negative affective state in abstinent drug users. Compelling evid

• The desire for COTS products and some potential problems

  2020-07-10

  

  The desire for COTS products––and some potential problems There are also technological reasons in support of the use of OTS products. For example, Dawkins and Riddle (2000) point out that the relatively small safety-related systems market cannot sustain the rate of technological advancement stimula

• Several CHK inhibitors have been

  2020-07-10

  

  Several CHK-1 inhibitors have been reported in the literature. Of these, UCN-01 (7-hydroxystaurosporine) is a potent inhibitor of CHK-1 (=5.6nM), , and has modest selectivity among other kinases. UCN-01 is currently in clinical trials. Other CHK-1 inhibitors reported in the literature include indaz

• The ERR gene lacks the typical TATA

  2020-07-10

  

  The ERRα gene lacks the typical TATA and CAAT boxes, but has multiple consensus Sp1 binding elements in the GC-rich promoter (Shi et al., 1997). Previously, our laboratory has shown that ERRα expression is upregulated in the mouse uterus by estrogen (Shigeta et al., 1997) and recently we identified

• br Clinical potential of ET receptor

  2020-07-10

  

  Clinical potential of ET receptor biased ligands Is there a clinical need for ET receptor biased ligands? Evidence is strongest from research in epithelial ovarian cancer demonstrating that ET-1 stimulated ETA-mediated β-arrestin signalling leads to activation of the oncogenic mediator NF-κB [21]

• br Conflict of interest statement br Introduction Endothelin

  2020-07-09

  

  Conflict of interest statement Introduction Endothelins (ETs) are a family of multifunctional, naturally occurring peptides with long-lasting vasoconstrictor and pressor effects (Zhou et al., 2004). They are synthesized as a large protein, the pre-proET-1 or Big ET-1, which is subsequently cle

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