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Tetracyclines constitute one of the most important antibioti
2024-03-16
Tetracyclines constitute one of the most important antibiotic groups used as veterinary and human medicine and as feed additives in the agricultural sector (Li et al., 2011a, Simon, 2005). Annual worldwide production of tetracyclines is estimated to be in the thousands of tons (Michalova et al., 200
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raas inhibitors A rate limiting step in
2024-03-15
A rate-limiting step in the generation of kynurenine and xanthurenic raas inhibitors is the oxidation of N-formyl-kynurenine to l-kynurenine via indolamine 2,3-dioxygenase (IDO) or tryptophan dioxygenase (TDO). IDO and/or TDO knockdown decreases and ectopic over-expression increases production of en
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The relatively high concentration of HT
2024-03-15
The relatively high concentration of 5-HT used in this study (100 µM) is consistent with the concentrations used in other published ex vivo studies (Ropert and Guy, 1991, Passani et al., 1994, Shen and Andrade, 1998). In our paradigm 5-HT was focally applied at the surface of the slice via a fast pe
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An alternative approach to the
2024-03-15
An alternative approach to the administration of ADO agonists is to amplify the actions of endogenous ADO by inhibiting the ADO-metabolizing enzyme, ADO kinase (AK). Inhibition of AK has the net effect of potentiating the local concentration and the effects of ADO in the extracellular compartment. T
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BGB-324 Introduction Myasthenia gravis MG is an autoimmune d
2024-03-15
Introduction Myasthenia gravis (MG) is an autoimmune disorder characterized by muscle weakness, which is mainly due to autoantibodies reducing the number or function of postsynaptic BGB-324 receptors (AChRs) [1], [2]. Animal models have been developed to uncover the immunopathogenesis of MG. Exper
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NSAIDs induce gastrointestinal toxicity and evoke asthma
2024-03-15
NSAIDs induce gastrointestinal toxicity and evoke niacin nicotinic acid by decreasing the production of gastroprotective prostanoids and by redirecting the COX substrate AA into LT biosynthesis, thereby causing vasoconstriction in gastric mucosa and airways (Celotti and Laufer, 2001; Koeberle and W
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br Conclusions br Acknowledgments br Introduction To die
2024-03-15
Conclusions Acknowledgments Introduction To die or not to die – that is the question. Christian de Duve created the word “autophagy” in 1960’s for the first time (Klionsky et al., 2016). The word “autophagy” was derived from the Greek roots “auto” (self) and “phagy” (eating) and referred to
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A-674563 The identification of novel kinase inhibitor scaffo
2024-03-15
The identification of novel kinase inhibitor scaffolds is highly desirable in order to develop selective kinase inhibitors. Small-molecule inhibitors of Interleukin-2-inducible T-cell kinase (Itk) that are based on the 3-aminopyridin-2-one fragment 1 have been reported. Despite derivatisation of 1 y
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Maintaining the normal vaginal fluid acidity is important fo
2024-03-15
Maintaining the normal vaginal fluid acidity is important for vaginal functions (Wagner and Levin 1984). Estrogen has been shown essential in maintaining the acidity of vaginal fluid, in which its deficiency could cause vaginal fluid pH to increase (Gorodeski et al. 2005). After menopause, low estro
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We used the lead compound C to demonstrate that
2024-03-15
We used the lead compound C4 to demonstrate that small molecule ACL inhibitors can recapitulate ACL knockdown (KD) in modulation of cancer stemness. We have shown previously that ACL KD reduced the CSC population in multiple cancer cell lines. The E-snail cells are an established CSC model system.
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Investigating these possibilities will illuminate
2024-03-15
Investigating these possibilities will illuminate whether NECA receptor possess mechanisms to differentially detect ACLY-generated versus ACSS2-generated acetyl-CoA as well as define the functional relationship between histone acetylation levels and cellular functions and phenotypes. Given that ACL
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There are several reports providing evidences that functiona
2024-03-14
There are several reports providing evidences that functional and mechanistic connection between Sirt1 and LKB1/AMPK in metabolic regulation [26], [32], [33]. It has been reported that the deacetylation of LKB1 by Sirt1 is one of the determining factors of the subcellular localization of LKB1. In ag
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Interestingly metabolic dysfunction is also
2024-03-14
Interestingly, metabolic dysfunction is also observed in amyotrophic lateral sclerosis (ALS). Patients and mouse models of familial ALS exhibit higher levels of resting N-Methyl-D-aspartic acid expenditure and lower fat-free mass, indicating a hypermetabolic phenotype. Lim et al. (2012) found that
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Analysis of the enzyme activity expressed as rate of
2024-03-14
Analysis of the enzyme activity, expressed as rate of product formation per unit serum volume (20μl), between the diagnostic groups revealed that ApB activity was significantly decreased in the patient group both at recruitment and after 13months when the substrate concentration used was 1.5mM (pCH5
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The decreased AR mediated response has
2024-03-14
The decreased βAR-mediated response has been attributed to different mechanisms, including an attenuation of PKA activation, an impaired generation of cyclic AMP, a reduced receptor density, and a less efficient coupling to adenylyl-cyclase [10]. However, currently there is no single molecular or ce
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