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pde inhibitors br Introduction O Dowd et al identified a
2024-04-27
Introduction O’Dowd et al. identified a gene very similar to angiotensin type-1 receptor in 1993 (O’Dowd et al., 1993). The specific selective ligand of this receptor called APJ receptor was determined by Tatemoto et al. in 1998 as apelin (Tatemoto et al., 1998). The high expression of apelin and
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Apelin is a bioactive peptide and endogenous
2024-04-27
Apelin is a bioactive peptide and endogenous ligand for the APJ receptor (APLNR), a member of the G protein coupled receptor family that shares a similar sequence as the angiotensin type-1 receptor (AT1) [5]. Early studies demonstrated that the apelin/APLNR receptor axis plays a significant role in
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Breast Cancer Although androgens have been considered to be
2024-04-27
Breast Cancer: Although androgens have been considered to be a risk factor in prostate cancer they have been recommended to treat breast cancers. Even before the discovery of SERMs and aromatase inhibitors, steroidal androgens such as medroxyprogesterone and fluoxymesterone were used to treat breast
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As noted above yeasts particularly
2024-04-27
As noted above, yeasts, particularly S. cerevisiae (Frey and Röhm 1978; Trumbly and Bradley 1983), produce APs, but these are intracellular enzymes located in the vacuolar compartment, with the exception of aminopeptidase II. About 40% of aminopeptidase II activity is detected as external enzyme, li
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Epidermal growth factor EGF has been shown to increase
2024-04-27
Epidermal growth factor (EGF) has been shown to increase the 12S-lipoxygenase mRNA level by about two-fold in human epidermoid carcinoma A431 cells [71]. This enzyme was shown to be of the platelet-type and associated with the microsomal fraction of the cells [71], [72]. A requirement for EGF recept
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Preclinical models indicate roles for
2024-04-27
Preclinical models indicate roles for adiponectin in the maintenance of hepatic lipid metabolism. Adiponectin overexpression prevents accumulation of triglycerides or the deleterious lipid metabolites diacylglycerols or ceramides [5,8]. Direct manipulation of adiponectin expression demonstrates a po
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However although in vitro studies in heterologous systems
2024-04-27
However, although in vitro studies in heterologous systems have provided very important indications of potential novel pharmacology, the studies with endogenous receptors in native tissues are essential to provide evidence for GPCR heteromerization in vivo and to confirm its physiological relevance.
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Two patients developed diffuse mesangio proliferative glomer
2024-04-26
Two patients developed diffuse mesangio-proliferative glomerulonephritis (DMPG) postoperatively, presenting as nephrotic syndrome and benign haematuria, respectively. DMPG has been reported in an adult patient with thymomatous MG following thymectomy [35], and various types of glomerulonephritis hav
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The pathogenesis of d penicillamine induced
2024-04-26
The pathogenesis of d-penicillamine-induced MG is not clear. The repertoire of anti-AChR PP121 mg in d-penicillamine-induced MG has been shown to be similar to that in idiopathic MG in terms of AChR antigenic regions, suggesting a common immune mechanism (Tzartos et al., 1988). About 20% of d-penic
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Altogether the situations described above clearly impede the
2024-04-26
Altogether, the situations described above clearly impede the critical steps of drug discovery and development and the scientific process in general [14]. In conclusion, it is the opinion of these authors that many exciting lines of drug discovery (which includes those devoted to nAChR ligands) have
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On the contrary evidence also suggests
2024-04-26
On the contrary, evidence also suggests that autophagy plays a striking protective role in cancer cells. Highly burgeoning cancer AS-703026 require cellular building blocks for their metabolism and energy production. At this stage of cancer development, autophagy acts as a friend providing all the e
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mgmt inhibitor br Conflicts of interest br Acknowledgments T
2024-04-26
Conflicts of interest Acknowledgments The authors acknowledge National Institute for Medical Research Development (NIMAD) project no. 940943 and National Research Institute for Science Policy (NRISP) no. 1456 for financial support of this work. AM appreciates National Institute for Genetic Eng
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The identification of novel kinase inhibitor scaffolds is
2024-04-26
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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br Current limitations and future directions There
2024-04-26
Current limitations and future directions There are several limitations associated with PET imaging of aromatase using carbon-11 labeled aromatase inhibitors. Due to the very short half-life of carbon 11 (20min), PET studies with currently available, validated tracers can only be performed in med
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br Experimental Section br Results and
2024-04-26
Experimental Section Results and Discussion Conclusions The advantages of the novel enzymo-chemical method for Mn and Co assay are simplicity of analytical procedure and economic effect due to the usage of only one enzyme in the form of apo-enzyme. An effectiveness of the apo-arginase-based
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