• The first rationally designed dual mPGES LO

  2024-06-26

  

  The first rationally designed dual mPGES-1/5-LO inhibitor was reported in 2008 and represents a structural derivative of pirinixic Tirapazamine - a synthetic agonist of PPARα with lipid-lowering properties (Koeberle et al., 2008b). Further α-alkyl- and α-aryl-substituted derivatives have been synth

• The first natural product described as LO inhibitor was the

  2024-06-26

  

  The first natural product described as 5-LO inhibitor was the polyphenol nordihydroguaiaretic death associated protein kinase from the Mexican dessert plant Larrea divaricata in 1981 (Bokoch and Reed, 1981), short after the initial identification of 5-LO in 1979 (Borgeat and Samuelsson, 1979). Long

• Subsequently Palvimaki et al corroborated Ni and Miledi s st

  2024-06-26

  

  Subsequently, Palvimaki et al. (1999) corroborated Ni and Miledi's study by demonstrating that treatment with fluoxetine leads to 43% occupancy of the 5-HT2C receptors. Moreover, the affinity of fluoxetine for 5HT2C receptors (Ki 65 nM) is close to its affinity for 5-HT transporters (Ki 33 nM) (Ni a

• Several tertiary prevention studies are currently underway e

  2024-06-26

  

  Several tertiary prevention studies are currently underway examining the use of dutasteride for prostate cancer treatment: (1) during expectant management of prostate cancer, (2) after radical prostatectomy in men at high risk for relapse, and (3) in men with metastatic disease. The Reduction by Du

• br Concluding remarks Autophagy ensures cell homeostasis and

  2024-06-26

  

  Concluding remarks Autophagy ensures cell homeostasis and survival through the continuous degradation/recycling of intracellular components. It can also represent a conserved, cell-intrinsic, defense mechanism against invading pathogens, including viruses. The autophagy process can be activated r

• Ryoichi et al modified potent clinical candidate VX with

  2024-06-26

  

  Ryoichi et al. modified potent clinical candidate VX-680 (6) with 3-cyano-6-(5-methyl-3-pyrazolamino)pyridine as Aurora kinase inhibitor. Substituted cyano pyridine derivative (7) inhibited proliferation of HCT-116 cells with an IC50 value of 115 nM. It showed tumor inhibition in mice model at a dos

• V ATPase is a complex enzyme that is

  2024-06-26

  

  V-ATPase is a complex enzyme that is composed of several subunits, which are assembled into two domains: trans-membrane (V0) and cytosolic (V1) domains [3,5]. Epididymal epithelial AK-7 of rats has been reported to contain V-ATPase which is distributed at the apical pole of the narrow and clear cell

• Recent studies have supported the existence

  2024-06-26

  

  Recent studies have supported the existence of an inward RAS regulatory mechanism in which AT1 receptors downregulate angiotensin-converting enzyme 2 (ACE2) and subsequently impair angiotensin-(1-7) generation and MAS functionality (Jessup et al., 2006, Gallagher et al., 2008, Xia et al., 2009, Pern

• Evidence from basic science studies suggests that Cd

  2024-06-26

  

  Evidence from basic science studies suggests that Cd may play a role in prostate cancer through disruption of the androgen receptor (AR). AR, a hormone-activated transcription factor, is the key driver of prostate cancer progression [6]. Ironically, the AR is also required for normal prostate growth

• In light of several reports of defects in memory related

  2024-06-26

  

  In light of several reports of defects in memory-related tasks for the dysbindin-deficient mice (Cox et al., 2009, Takao et al., 2008), it was rather unexpected that an enhancement of CA3–CA1 LTP was observed in our investigation as well as in another independent study (T.T. Tang et al., 2009). The

• Accumulating evidence suggest that patients

  2024-06-25

  

  Accumulating evidence suggest that patients with advanced -positive NSCLC are at increased risk of VTE or coagulation disorders during the course of their disease, indicating that cancer genotype might play a role in the occurrence of cancer-related thromboembolism . Here we report the case of a pat

• br Introduction Myasthenia gravis MG

  2024-06-25

  

  Introduction Myasthenia gravis (MG) is an autoimmune disease characterised by failure of transmission at the neuromuscular junction (NMJ). In 80–85% of myasthenia gravis patients, the disease is mediated by antibodies to the nicotinic 3CAI receptor (AChR; (Lindstrom et al., 1976). Many investiga

• Celastrol br Introduction In myasthenia gravis MG autoantibo

  2024-06-25

  

  Introduction In myasthenia gravis (MG), autoantibodies against the native AChR conformation cause loss of AChR at the neuromuscular junction and fatigable muscle weakness (Newsom-Davis et al., 1993). The AChR is a pentameric transmembrane protein, with two splice forms of the α-subunit, P3A− and

• The effect of capital deductions on

  2024-06-25

  

  The effect of capital deductions on equilibrium prices is given by the following comparative statics Thus, equilibrium prices are strictly decreasing in the share of capital cost deduction. The reason is that a higher share of capital cost deduction reduces the effective marginal costs, which makes

• Small kinase inhibitors have been developed to block AXL

  2024-06-25

  

  Small kinase inhibitors have been developed to block AXL by interacting with the kinase cytoplasmic ATP binding site. Up to date, no AXL selective kinase inhibitors are marketed. As depicted in , some marketed kinase inhibitors such as Bosutinib and Cabozantinib or kinase inhibitors in clinical pha

15758 records 128/1051 page Previous Next First page 上5页 126127128129130 下5页 Last page