• 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

• KP372-1 mg Analogous to all GPCRs the GLP R transduces signa

  2022-07-21

  

  Analogous to all GPCRs, the GLP-1R transduces signals from the outside of the cell to the inside by allosterically converting a ligand-binding event to activation of intracellular effectors. The GLP-1R couples to several intracellular effectors and this pleiotropic coupling is physiologically releva

• Neither GIP nor GIPR SNPs were associated

  2022-07-21

  

  Neither GIP nor GIPR SNPs were associated with occurrence of fractures in the OPRA cohort (Table 4). Discussion The basis for this study lies in the role of glucose-insulinotropic peptide (GIP) hormone in the regulation of insulin secretion as well as its anabolic effect on osteoblasts and inhib

• br Secretase in inflammatory diseases Secretase appears to p

  2022-07-21

  

  γ-Secretase in inflammatory diseases γ-Secretase appears to play a more important role than previously recognized in inflammatory diseases. Studies have shown that mice partially deficient in PS genes (PS1+/− PS2−/−) develop an immune system deficit in late adulthood, such as ulcerated skin or a

• Inflammasomes are multimeric protein complexes involved

  2022-07-21

  

  Inflammasomes are multimeric protein complexes involved in the host defense protecting activity against invading pathogens and in physiological aberrations such as cancer and auto-inflammatory, metabolic, and neurodegenerative diseases. Inflammasomes induce the inflammatory process by triggering the

• Having shown that some of substitutions Cl

  2022-07-21

  

  Having shown that some of substitutions (Cl, CF) at the 2-position of the thiophene improved rat microsomal stability, and polar groups at the 4-position of the aryl ring had a beneficial effect on stability in both human and rat microsomes, we combined these features in a new set of analogs. Methyl

• Combination inhibitors of FAAH TRPV

  2022-07-21

  

  Combination inhibitors of FAAH, TRPV1, and/or COX2 may have the advantage of effective pain relief with a high therapeutic index. For example, arachidonoyl serotonin (AA-5-HT) inhibits both FAAH (IC=1–12μM) and TRPV1 (IC=37–270nM against 100nM capsaicin in HEK-293 cells)., In mice, AA-5-HT had grea

• Neuropathic pain NP is a chronic pain caused by lesion

  2022-07-21

  

  Neuropathic pain (NP) is a chronic pain caused by lesion or disease affecting any part of the nervous system leading to clinical conditions ranging from painful neuropathy to poststroke central pain. Anticonvulsant drugs, Gabapentin and Pregabalin, acting on αδ subunit-containing voltage-dependent c

• WM-1119 synthesis br The inhibitory effect of ATP B

  2022-07-21

  

  The inhibitory effect of ATP7B knockdown on lysosomal exocytosis is likely mediated by the resulting oxidative stress induced by Cu, as exposure to oxidative stress induced by tert-Butyl hydroperoxide (TBHP) inhibited β-hex exocytosis as well, indicating that oxidative stress inhibits lysosomal ex

• Following the discovery of diketo compounds S and

  2022-07-20

  

  Following the discovery of β-diketo compounds S-1360 [31] and L-731988 [32] as anti-HIV integrase inhibitors, a group of researchers discovered a potent PEG Virus Precipitation Kit based derivative (1) as the inhibitor of HIV integrase functioning at the 3′-processing and strand transfer steps of H

• The molecular mechanism of gliotransmitter release is not fu

  2022-07-20

  

  The molecular mechanism of gliotransmitter release is not fully understood until now, and previous studies have emphasized that the elevation of [Ca2+]i triggers vesicular monensin of glutamate. Parpura et al. reported that the essential role of Ca2+ release from internal stores in glutamate release

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