• br Phosphorylation of P c Initial studies In addition to

  2023-09-09

  

  Phosphorylation of P450c17 – Initial studies In addition to the molar ratio of POR to P450c17 and the allosteric action of cytochrome b5, a third factor that governs 17,20 lyase activity is the serine/threonine (Ser/Thr) phosphorylation of P450c17 itself. In a search for post-translational factor

• br Expression of autotaxin in cancer Autotaxin ATX is a

  2023-09-09

  

  Expression of autotaxin in cancer Autotaxin (ATX) is a member of the family of NPPs (Nucleotides pyrophosphatases phosphodiesterases (NPP) family with a unique lysophospholipase D (lysoPLD) activity, allowing the synthesis of LPA from lysophospholipid precursors such as the lysophosphatidylcholin

• br ASK in Huntington s

  2023-09-09

  

  ASK1 in Huntington's disease and other polyglutamine diseases The polyglutamine (polyQ) diseases are a group of inherited neurodegenerative disorders caused by the expansion of cytosine-adenine-guanine (CAG) trinucleotide repeats in the coding regions of specific genes, leading to the production

• Acknowledgments br Introduction Pulmonary fibrosis PF is

  2023-09-08

  

  Acknowledgments Introduction Pulmonary fibrosis (PF) is a chronic, fibrosing interstitial pneumonia and a crushing disease that occurs as a result of a variety of lung injuries, including auto-immune, tuberculosis and traumatic insult [1], [2]. PF is characterized by the accumulation of extracel

• br Concluding Remarks and Future Perspectives

  2023-09-08

  

  Concluding Remarks and Future Perspectives The collective evidence from studies detailing the functions of AMPK in the neuromuscular system, combined with those in DMD, SMA, and DM1 surveyed in the present review, strongly suggests that AMPK is a central mediator of neuromuscular determination, m

• AMP activated protein kinase AMPK is a

  2023-09-08

  

  AMP-activated protein kinase (AMPK) is a key cellular energy sensor that maintains energy homeostasis at the cellular and whole-organism level (Hardie et al., 2012). Functionally, the AMPK pathway sustains adenosine triphosphate (ATP) production through activation of fatty SNDX275 oxidation and auto

• br AMPK as a druggable target

  2023-09-08

  

  AMPK as a druggable target AMPK signaling has attracted considerable attention within the past decades, owing to the capacity of pharmacological compounds (e.g., 5-aminoimidazole-4-carboxamide-1-β-D-ribofuranoside [AICAR] and metformin) or natural compounds (e.g., resveratrol) to activate AMPK in

• AMN107 Recently two distinct small molecule inhibitors of PH

  2023-09-08

  

  Recently, two distinct small-molecule inhibitors of PHGDH were identified using high-throughput screens, both of which inhibit de novo serine biosynthesis and show selective toxicity to cancer AMN107 with high SSP flux [50,51]. The inhibitor NCT-503, which has an IC50 of 2.5μM, reduces the growth a

• In conclusion we have shown that mGlu receptors

  2023-09-08

  

  In conclusion, we have shown that mGlu7 receptors negatively regulate α1-adrenergic receptor signalling in heterologous expression systems, parp inhibitors tissue and living animals. This interaction might represent a protective mechanism aimed at restraining an excessive activation of noradrenergi

• G actin has a molecular weight of kD and dimensions

  2023-09-08

  

  G-actin has a molecular weight of 42 kD and dimensions about 55 × 55 × 35 Å3. It consists of 375 amino acids arranged into two individual domains (Alberts et al., 2014). A central cleft bisects the protein into two aforementioned domains which surround a deep cleft containing ATP or ADP and a tightl

• XL-888 In conclusion two novel series of

  2023-09-08

  

  In conclusion, two novel series of furo[2,3-]pyrimidin4-amines and 7-pyrrolo[2,3-]pyrimidin-4-amines which exhibit potent in vitro inhibitor activity against ACK1 have been identified and evaluated. 1,3-Dithiolane-substituted pyrrolopyrimidine displays excellent ACK1 cellular inhibition, good kinas

• Altogether the situations described above clearly impede

  2023-09-08

  

  Altogether, the situations described above clearly impede the critical steps of drug discovery and development and the scientific process in general [14]. In conclusion, it is the opinion of these authors that many exciting lines of drug discovery (which includes those devoted to nAChR ligands) have

• AVE 0991 In addition to the data provided

  2023-09-08

  

  In addition to the data provided by the Ki16425 treatment in the K/BxN arthritis model, new findings from the study of two new LPA receptor antagonists confirm the involvement of the LPA pathway in the pathogenesis of experimental arthritis. In the study by Miyabe et al., the authors reported the tr

• HCC aetiology is multifactorial and

  2023-09-08

  

  HCC aetiology is multifactorial and the disease is often preceded by other conditions including liver fibrosis and cirrhosis that are associated with HCV, HBV, alcoholic and non-alcoholic hepatitis. The discovery of new therapeutic targets will require a greater understanding of the pathogenic mecha

• In our H K ATPase assay Fig and Supplementary Fig

  2023-09-08

  

  In our H+, K+-ATPase assay (Fig. 1 and Supplementary Fig. 1), myricetin (IC50 = 0.58μM) was more potent than acid-activated omeprazole (IC50 = 1.50μM). In contrast, in oral administration in mice (Fig. 3), omeprazole (20mg/kg) more effectively inhibited gastric 3X FLAG sale secretion compared to my

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