• Since the cloning of ARs

  2024-10-28

  

  Since the cloning of ARs in the beginning of the 1990s, the efforts to characterize them have led to the accumulation of a substantial amount of experimental data. Decades of site-directed mutagenesis (SDM; Box 1) studies, in combination with pharmacological data and computational modeling, have pav

• Given the powerful and ubiquitous nature

  2024-10-28

  

  Given the powerful and ubiquitous nature of adenosine action within the CNS, basal levels of extracellular adenosine are carefully regulated and are estimated to be in the region of 30–300 nM (Fredholm et al., 2001). The two main pathways for the control of extracellular adenosine involve phosphoryl

• SC-10 receptor Systematic administration of ABT amino bromop

  2024-10-28

  

  Systematic administration of ABT-702 (4-amino-5-(3-bromophenyl)-7-(6-morpholino-pyridin-3-yl) pyrido[2,3-d] pyrimidine), a potent and selective non-nucleoside AK inhibitor, also generates analgesic effects in animal models of pain (Jarvis et al., 2000, Kowaluk et al., 2000, Suzuki et al., 2001), su

• Toxicity is the main reason for the failure at

  2024-10-28

  

  Toxicity is the main reason for the failure at all stages of the new drug development process. The major part of safety-related attrition occurs at preclinical phases while predicting preclinical safety liabilities earlier in the drug development process. This strategy enables the design and/or sele

• In addition to the above mentioned

  2024-10-28

  

  In addition to the above-mentioned synaptic mechanisms, the serotonergic system also has a critical role in the antidepressant effects of mGlu2/3 receptor antagonists. Indeed, we previously reported that mGlu2/3 receptor antagonists increased the firing rate of serotonin neurons in the dorsal raphe

• To date more than different

  2024-10-28

  

  To date, more than 50 different mutations in the gene have been described (Human Gene Mutation Database at the Institute of Medical Genetics in Cardiff: SRD5A2 Gene: http://www.hgmd.cf.ac.uk). Most of them are missense mutations but premature stop codons and deletions leading to non-functional or su

• Using our infection assays we also

  2024-10-28

  

  Using our infection assays, we also explored whether low-pH compartments were required for the entry of ZIKVs in mammalian cells. Lysosomotropic agents such as ammonium chloride, chloroquine and Bafilomycin A1, strongly inhibited the ability of ZIKVs to enter mammalian cells. Our results are in agre

• Roles of Aurora kinases in directly activating multiple

  2024-10-28

  

  Roles of Aurora kinases in directly activating multiple oncogenic pathways and promoting proliferation as well as transformation have also been demonstrated. Aurora-A has been shown to up-regulate telomerase reverse transcriptase mRNA through c-myc [26]. The kinase was also implicated in activating

• Ki16425 br Valsartan It is another ARB with

  2024-10-26

  

  Valsartan It is another ARB, with several reports for its beneficial effects on CV system both in preclinical and clinical studies. Valsartan treatment has reduced the levels of pentraxin 3, a marker for inflammation and is well tolerated in terms of side effects [17]. In BSCORE study, 90-day sec

• br Valsartan It is another ARB with

  2024-10-26

  

  Valsartan It is another ARB, with several reports for its beneficial effects on CV system both in preclinical and clinical studies. Valsartan treatment has reduced the levels of pentraxin 3, a marker for inflammation and is well tolerated in terms of side effects [17]. In BSCORE study, 90-day sec

• AMPK is a cellular energy sensor that is phosphorylated in

  2024-10-26

  

  AMPK is a cellular energy sensor that is phosphorylated in response to high intracellular ADP levels to increase GLUT4 translocation into the cell, and subsequently, increase intracellular glucose levels to provide substrate to replenish ATP levels [25]. In metabolic syndrome, sequestration of plasm

• MMP-2 Inhibitor I In the largest postmortem study of autopsi

  2024-10-26

  

  In the largest postmortem study of 3618 autopsied individuals, almost 75% of the individuals without Aβ pathology already harbored cortical NFT pathology mostly confined to the medial temporal regions (Murray et al., 2015). In Braak's study of 2366 autopsied individuals (Braak and Del Tredici, 2014)

• br Competing interests br Acknowledgments This research was

  2024-10-26

  

  Competing interests Acknowledgments This research was supported by Basic Science Research Program through the National Research Foundation of Korea (NRF) funded by the Ministry of Science and ICT (NRF-2014R1A4A1071040). Introduction Mitochondria occupy an important position as mediators of

• AHR mediated MMP upregulation has been

  2024-10-26

  

  AHR-mediated MMP1 upregulation has been shown in response to tobacco smoke [32]. Tobacco smoke contains various AHR ligands such as benzo[a]pyrene. Both benzo[a]pyrene [15] and FICZ [13] are high-affinity ligands for AHR and upregulate CYP1A1 and CYP1B1. FICZ is rapidly degraded by CYP1A1 [20], [33]

• br ABCA mRNA expression is

  2024-10-26

  

  ABCA2 mRNA expression is elevated in Niemann-Pick type C and familial hypercholesterolemia fibroblasts Niemann-Pick Type C disease is a neurological disorder of adolescents due to autosomal-recessive mutations in either one or both Niemann-Pick-2 (NPC2) and NPC1 genes, which, like ABCA2, are loca

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