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Several structural classes of ASK inhibitors
2022-11-28
Several structural LGX818 receptor of ASK1 inhibitors, mostly from industry but also from academia, have been identified over the last decade. In 2012, Terao et al. (Takeda) reported imidazo[1,2-α]pyridine () as a potent ASK1 inhibitor derived from structure-based drug design. GSK, Merck and Gilead
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Long term blood pressure regulation is linked to renal
2022-11-24
Long term blood pressure regulation is linked to renal function through the mechanisms of pressure natriuresis (Evans et al., 2005), which has been shown to be modulated by the RAS (Hall et al., 1999). Key components of the RAS are expressed throughout the kidney, and are implicated in renal excreto
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br Introduction Nausea and vomiting are among the most
2022-11-22
Introduction Nausea and vomiting are among the most distressing side effects associated with chemotherapy in cancer patients (Billio et al., 2010). Severe emesis can negatively affect a patient's nutritional state, ability to work and motivation, which can, in turn, interfere with the clinical co
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br Acknowledgement br Introduction There
2022-11-21
Acknowledgement Introduction There has been great progress in the treatment of autoimmune disease during the past several decades. However, the majority of autoimmune diseases have no known cure. B lymphocytes and autoantibodies play important roles in many autoimmune diseases, including rheum
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br Acknowledgement br Introduction There
2022-11-21
Acknowledgement Introduction There has been great progress in the treatment of autoimmune disease during the past several decades. However, the majority of autoimmune diseases have no known cure. B lymphocytes and autoantibodies play important roles in many autoimmune diseases, including rheum
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Whole body loss of ACLY
2022-11-18
Whole-body loss of ACLY is early embryonic lethal, indicating that it serves non-redundant roles during development (Beigneux et al., 2004). Silencing or inhibition of ACLY suppresses the proliferation of many cancer cell lines and impairs tumor growth (Bauer et al., 2005, Hanai et al., 2012, Hatziv
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yutopar br Acknowledgments This work was supported by the Sw
2022-11-18
Acknowledgments This work was supported by the Swiss National Science Foundation. 15-Lipoxygenase 1 (15-LOX-1) is a nonheme, iron-containing enzyme predominantly expressed in reticulocytes, eosinophils, macrophages, mast cells, and bronchial epithelial cells . 15-LOX-1 is a key enzyme involved
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Introduction the DNA damage response important
2022-11-18
Introduction: the DNA damage response — important implications for tumour development and treatment Cells are invariably challenged by tens of thousands of lesions inflicted on their DNA everyday (Lindhal, 1993). This DNA damage can be caused exogenously by exposure to different types of radiation
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Autophagy and apoptosis have a very complex relationship and
2022-11-18
Autophagy and apoptosis have a very complex relationship, and the precise mechanism remains to be determined. At present, a large amount of research has confirmed that autophagy can protect the cell from apoptosis in special conditions such as nutrient deficiency or growth factors deprivation; the e
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AP 18 br HMG proteins mobile modulators
2022-11-18
HMG proteins: mobile modulators of chromatin structure and cellular phenotype The term “High Mobility Group” was originally coined for the HMG proteins because of their unusual solubility properties, their small size and their rapid mobility, relative to other chromatin proteins, during gel elect
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Despite the absence of disulfide bonds
2022-11-18
Despite the absence of disulfide bonds in its linear structure, KT43C displays antifungal and antibacterial activity. Disulfide bonds are determinants of defensins' integrity and have been reported to increase the antimicrobial activity (Jenssen et al., 2006). However, some linear derivatives of AMP
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Introduction AMP activated protein kinase AMPK is
2022-11-18
Introduction AMP-activated protein kinase (AMPK) is mainly known as a highly conserved and ubiquitously expressed energy sensor that is highly sensitive to changes in cellular energy levels (by sensing increases in AMP:ATP and ADP:ATP ratios) and makes appropriate adjustment to balance the consumpt
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In this study we designed and synthesized two ALK PROTACs
2022-11-18
In this study, we designed and synthesized two ALK PROTACs (degraders), 5 (MS4077) and 6 (MS4078), by linking ceritinib and pomalidomide [45] through two different linkers. Using human ALCL and NSCLC cells, we characterized both compounds in a battery of assays to demonstrate their effects on reduci
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To further clarify the vascular cell types expressing
2022-11-18
To further clarify the vascular cell types expressing AR subtypes, double immunofluorescence staining for ARs and vascular endothelial S/GSK1349572 or vascular smooth muscles was performed. As shown in Fig. 3, Fig. 4, overlay images show the expression of all ARs subtypes that we examined in vascul
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Ozone induced innate inflammatory responses in
2022-11-18
Ozone-induced innate inflammatory responses in the lung involve neutrophil extravasation through enhanced trans-endothelial migration (Krishna et al., 1997). Catecholamines and glucocorticoids, which are increased by ozone inhalation (Bass et al., 2013, Miller et al., 2015, Miller et al., 2016a, Mil
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