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The discovery of acetylsalicylic acid
2024-08-27

The discovery of acetylsalicylic TC 14012 (aspirin) in 1897 paved the way for the development of classical NSAIDs as first-line therapeutics for anti-inflammatory, anti-pyretic and analgesic therapy. Large efforts have been made in the following decades to improve the efficacy and in particular saf
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Autotaxin has been linked to
2024-08-27

Autotaxin has been linked to chemoresistance through its ability to inhibit apoptosis induced by paclitaxel in breast cancer Protease Inhibitor Library [15] and LPA can inhibit cell death induced by cisplatin [40]. Autotaxin was included in the present study because it was identified as being over-
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However there are studies revealing the dark side of autopha
2024-08-27

However, there are studies revealing the “dark side” of autophagy at later stages in cancers, when oncogenes (mainly K-ras and B-raf) are activated and/or tumour suppressors such as PTEN and p53 are inactivated. These studies are based on the use of GEMM and deletions of essential autophagy genes (A
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br Materials and methods br Results
2024-08-27

Materials and methods Results Discussion Japanese encephalitis caused by JEV is characterized by kainic acid sale neuron death. However, the underlying mechanism is not fully understood. We and other researchers have demonstrated that JEV induces apoptosis by ER stress-mediated IRE1/JNK an
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The levels of Mcl and
2024-08-27

The levels of Mcl-1 and FLIP are homeostatically controlled by transcriptional and posttranslational processes. Accumulating evidence suggested that intracellular signaling molecules such as Akt are crucial to the transcription of Mcl-1 and FLIP [30], [31]. The constitutive activation of Akt is dete
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br Mechanism of action In general
2024-08-26

Mechanism of action In general, the main targets for antifungal drug development are cell wall polymer (glucans, chitin, mannoproteins), cell membrane (especially ergosterol) biosynthesis, DNA and protein synthesis (topoisomerases, nucleases, elongation factors and myristoylation), and signal tra
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Glycosylphosphatidylinositol GPI cell wall anchor
2024-08-26

Glycosylphosphatidylinositol (GPI) cftr channel anchor synthesis pathway is another promising antifungal target. Novel inhibitors of Gwt1 and Mcd4, two enzymes in the GPI anchor pathway were identified by the chemical-genomics-based screening platform CaFT (Candida albicans fitness test) [89]. Scre
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br Conclusions br Material and
2024-08-26

Conclusions Material and methods Conflicts of interest Acknowledgements Introduction Currently more than 30 human proteins are implicated in a range of degenerative disorders owing to their misfolding and misassembly into various aggregate structures and leading to at least 20 serious
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ERAP has been crystallized in
2024-08-26

ERAP1 has been crystallized in two different conformations, wherein the C-terminal domain IV is either closely interacting with domains I/II and enclosing the active site (termed ‘closed’), or is rotated away in a hinge motion which exposes the active site (‘open’). This large motion correlates with
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Our studies suggest that AdipoR and
2024-08-26

Our studies suggest that AdipoR1 and AdipoR2 genes are expressed in multiple tissues in the chicken wherein both receptors are likely to mediate the physiological effects of adiponectin. We determined the relative expression of AdipoR1 and AdipoR2 mRNA in various tissues and found that skeletal musc
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In conclusion two novel series of furo pyrimidin
2024-08-26

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 kinase
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Our results using RT PCR confirm
2024-08-26

Our results using RT-PCR confirm earlier findings (Wilisch et al., 1999, Bruno et al., 2004) including the presence of both the P3A+ and P3A− isoforms of the α-subunit (Beeson et al., 1990). The lack of detection of the ε-subunit mRNAs in some thymomas, and lack of α-, β-, δ- and γ-subunit mRNAs by
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Both subcutaneous s c and mucosal administration of s
2024-08-26

Both subcutaneous (s.c.) and mucosal administration of short synthetic peptide derivatives of AChR prevent the onset of EAMG, but do not treat ongoing EAMG [80], [81], [82], [83], [84], [85]. The selection of peptides for treatment is mainly based on the identification of immunodominant T- and B-cel
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Introduction Microdialysis is an in vivo technique which all
2024-08-26

Introduction Microdialysis is an in vivo-technique which allows continuous sampling of small molecular weight substances (such as neurotransmitters, metabolites and neuropeptides) from the extracellular space of different tissues or organs, e.g. brain, muscle or skin. While the implantation of the
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The cellular mechanism underlying the
2024-08-26

The cellular mechanism underlying the CGS12066-mediated inhibition of glutamate release from hippocampal nerve terminals through presynaptic 5-HT1B receptors remains to be elucidated. 5-HT1B receptors are coupled to PTX-sensitive G proteins (Gi or Go) that have been shown to inhibit AC activity as w
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