• br Acknowledgments br Introduction Non

  2022-07-22

  

  Acknowledgments Introduction Non-steroidal anti-inflammatory drugs (NSAIDs) are a common treatment for a number of disease states involving an inflammatory reaction. This group of drugs mediate their anti-inflammatory effects mainly by inhibition of cyclooxygenase (COX), an enzyme of prime imp

• Tail group SAR of the imidazole derived analogs is shown

  2022-07-22

  

  Tail group SAR of the imidazole derived analogs is shown in . The previous SAR study from the discovery of AMG 837 revealed that a simple un-substituted meta-biphenyl tail group was less favorable in terms of potency. Efforts to introduce polarity to the tail group were not successful. When a methy

• In the Medicines for Malaria Venture MMV

  2022-07-22

  

  In 2011 the Medicines for Malaria Venture (MMV) distributed the Open-Access Malaria Box to accelerate antimalarial drug discovery (Spangenberg et al., 2013). The Malaria Box consists of 400 structurally diverse compounds, curated from >20,000 hits generated from large-scale screens, that inhibit the

• Sperm exocytosis or acrosome reaction AR is a regulated

  2022-07-22

  

  Sperm exocytosis or acrosome reaction (AR) is a regulated secretion with special characteristics essential for fertilization. The AR relies on the same highly conserved molecules that drive intracellular membrane fusion and exocytosis in all other hyPerFUsion™ high-fidelity DNA polymerase (see [59]

• The lysine K specific demethylase KDM family is comprised

  2022-07-22

  

  The lysine (K)-specific demethylase 4 (KDM4) family is comprised of 4 isoforms, KDM4A to -D, also known as JMJD2A to -D. KDM4A, B, and C encode proteins consisting of a JmjC, a JmjN, two PHD, and two Tudor domains. KDM4D is unique within the KDM4 family in that it has neither PHD nor Tudor domains,

• br Mechanisms of HDAC inhibition dependent cardioprotection

  2022-07-22

  

  Mechanisms of HDAC inhibition-dependent cardioprotection Multiple preclinical studies have demonstrated potent cardioprotective benefits of HDAC inhibition in murine models of myocardial stress, including I/R [19,25,29,30]. TSA reduces myocardial infarct size by up to 50% [19,25]. In addition, tr

• XEN445 receptor br Materials and methods br Results br Discu

  2022-07-22

  

  Materials and methods Results Discussion Directly modulating specific target proteins and signaling pathways with small-molecule drugs or agonistic XEN445 receptor is widely used for cancer metastasis therapies [[39], [40], [41]]. ANXA7 acts as a metastasis suppressor in prostate cancer. H

• As part of our discovery efforts searching

  2022-07-21

  

  As part of our discovery efforts searching for small molecule GPR119 agonists, we analyzed active pharmacophores of known agonists from the literature, and found that -methylsulfonylphenyl and substituted 4-hydroxyl piperidine are common fragments. In our initial efforts, we linked these two fragme

• Finally we investigated if calpain truncation affects GlyT t

  2022-07-21

  

  Finally, we investigated if calpain truncation affects GlyT1 turnover and trafficking. To simulate calpain cleavage at the T602/T603 and G626/S627 sites we constructed GlyT1 transporters missing the last 12 and 36 amino acids. Since the 36 amino epigenetics disease truncation also removes all C-ter

• IL-10, human recombinant protein br Materials and methods br

  2022-07-21

  

  Materials and methods Results Discussion In this study, the supF forward mutation assay showed that 5OHU induced mutations in human cells and that a C→T mutation was the predominant mutation among 5OHU-induced mutations. In addition, the DNA cleavage activity assay revealed that 5OHU was ex

• The occurrence of MDR in cancer patients undergoing

  2022-07-21

  

  The occurrence of MDR in cancer patients undergoing chemotherapy can be mimicked in the laboratory by culturing cancer ARCA Cy3 EGFP mRNA in the presence of chemotherapeutic drugs, thereby enforcing the evolution of acquired drug resistance. This has been described in multiple model systems includin

• br Discussion The GlyR is

  2022-07-21

  

  Discussion The GlyR is responsible for mediating much of the neuronal inhibition in the brainstem and spinal cord, although these receptors are also found in a number of higher brain regions (Baer et al., 2009, Jonsson et al., 2012, Jonsson et al., 2009, Lynch, 2004). A variety of structurally-di

• caspofungin br Materials and methods br Results br Discussio

  2022-07-21

  

  Materials and methods Results Discussion Quercetin is a relatively abundant bioactive flavonoid with a wide variety of documented physiological effects, which has gained popularity as a nutritional supplement [40]. There is increasing interest in quercetin's anticancer properties (for recen

• Young et al described the

  2022-07-21

  

  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

• br Material and methods br Results br Discussion Functional

  2022-07-21

  

  Material and methods Results Discussion Functional characterization of naturally occurring GCK mutations in patients with impaired glucose homeostasis has widened our knowledge of the catalytic and regulatory mechanisms of this enzyme [3]. In this work, we have biochemically characterized a

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