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Adenosine receptors activate a number of signalling pathways
2023-02-08
Adenosine receptors activate a number of signalling pathways involved in tissue survival including several mitogen-activated protein kinases (Fredholm et al., 2001). The common feature of all adenosine receptors is the positive coupling to ERK1/2, whilst A2B and A3 receptors can also activate the st
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The theoretical calculations of ADME parameters molecular we
2023-02-08
The theoretical calculations of ADME parameters (molecular weight (MW), log P, topological polar surface are (tPSA), number of hydrogen donors (nON) and acceptors (nOHNH), and volume) and DLS are presented in along with the violations of Lipinski’s rule. According to these data, all compounds (–) c
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The nAChR has been considered an interesting
2023-02-08
The α7 nAChR has been considered an interesting potential target for numerous therapeutic indications over the last two decades, with GTS-21 one of the first candidates proposed for Alzheimer's disease [2], [3], [23]. Unfortunately, although many α7-selective agonists have been developed [21], none
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Even within the context of evidence based
2023-02-08
Even within the context of evidence-based interventions for tobacco screening, the science is imperfect. For example, patients who screen positive for current smoking should receive cessation counseling and prescribed known effective nicotine replacement therapy based on the Public Health Services G
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Anti LT therapy by LO
2023-02-08
Anti-LT therapy by 5-LO inhibition has been hampered by occurring liver toxicities by Zileuton or the clinical phase II compound Atreleuton [36], [37] However both compounds possess a thiophene as well as an N-hydroxyurea moiety. These features could be linked with reactive thiophene intermediates [
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The first rationally designed dual mPGES LO inhibitor was re
2023-02-08
The first rationally designed dual mPGES-1/5-LO inhibitor was reported in 2008 and represents a structural derivative of pirinixic NBI 27914 hydrochloride - a synthetic agonist of PPARα with lipid-lowering properties (Koeberle et al., 2008b). Further α-alkyl- and α-aryl-substituted derivatives have
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br Viral manipulation of host factors to
2023-02-08
Viral manipulation of host factors to oppose anti-viral autophagy To escape or manipulate autophagy, some viruses developed strategies that are based on the recruitment of host-cell endogenous factors. The non-enveloped double-stranded DNA virus adenovirus is rapidly endocytosed after attachment.
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Based on currently available knowledge autophagy supports ad
2023-02-08
Based on currently available knowledge, autophagy supports adipocytes development and differentiation. In animals with specific skeletal muscle JP 1302 dihydrochloride of Atg7, reduced adipogenesis was shown. In rodents, autophagy was decreased in adipose tissue of animals fed with high-fat diet (H
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br Acknowledgments br Introduction Human innate immune syste
2023-02-08
Acknowledgments Introduction Human innate immune system provides first line of defense against multiple viral or bacterial attacks, and provides critical surveillance against oncogenic development. Evidences show that individuals with primary immunodeficiency or induced immunosuppression durin
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br Materials and methods br Results and discussion During re
2023-02-08
Materials and methods Results and discussion During recent years, recombinant ASK1 has been obtained by expensive baculovirus-insect cell ER 50891 synthesis systems [20], [27]. In the present study, we constructed recombinant ASK1 and expressed in active form at high level in E. coli. Human
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To further evaluate the influence of antibiotics on
2023-02-08
To further evaluate the influence of Trehalose receptor on allergy, Russel et al. initiated vancomycin treatment during pregnancy in mice and continued it for several weeks after birth. This resulted in exaggerated OVA-induced allergic inflammation, characterized by higher numbers of lung eosinophi
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Fish aminopeptidases from Alaska Pollack roe and tuna
2023-02-08
Fish aminopeptidases from Alaska Pollack roe and tuna pyloric caeca have been reported on [12,13]. More recently, we described the purification of a leucine aminopeptidase from the skeletal muscle of the common carp [14], red sea bream [15] and a lysine aminopeptidases from Japanese flounder [16]. T
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Several ceritinib resistant mutations following
2023-02-08
Several ceritinib-resistant mutations following the second-line treatment of ALK+-NSCLC have been discovered [64]. These mutations include C1156Y, F1174L, and L1152R, which were first observed in crizotinib-resistant tumor samples. The G1202R ceritinib-resistant mutation occurs within the hinge and
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Various compounds have been designed to
2023-02-08
Various compounds have been designed to inhibit aldose reductase (AR) [12]. These compounds can be classified into two main categories, the first category comprises those containing a carboxylic N6022 moiety, for example, 3-thiazolidineacetic acid derivative, which has been reported to be a potent A
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To guide our attempts at
2023-02-08
To guide our attempts at achieving AKT potency and selectivity against p70S6K and other kinases from (p70 S6K IC: 0.004 μM) and , we took advantage of exploiting the subtle sequence differences in the active sites of the AGC family kinases, we utilized the information around crystal structure of AK
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