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br Conclusion The histamine H receptor has been
2022-04-13
Conclusion The histamine H3 receptor has been the focus of a great deal of research over the past four decades and in this context, substantial progress has been made in developing H3R-related ligands. The involvement of H3Rs in many neurological disorders has been documented by several lines of
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740 Y-P Tylophora atrofolliculata is a centuries used folk m
2022-04-13
Tylophora atrofolliculata is a centuries-used folk medicine for the treatment of rheumatism in China (Jiangsu New Medical College, 1977). One group of its bioactive components is phenanthroindolizidine alkaloids, which have been demonstrated as lead compounds of anti-tumor agents in our previous stu
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However despite medicinal chemistry efforts lead to consider
2022-04-13
However, despite medicinal chemistry efforts lead to considerable improvement in potency and selectivity of new HO-1 inhibitors, still have not identified inhibitors in the low nanomolar range. Therefore, due to the possible in vivo non-specific effects at high dosage, novel strategies should be dev
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In first wave first generation drugs
2022-04-13
In 2013, first-wave, first-generation drugs telaprevir and boceprevir was the first protease inhibitors (PIs) incorporated in Brazilian Clinical Guidelines for the treatment of patients infected with HCV JNJ-26854165 1. Based on this 2013 Clinical Guideline, telaprevir could be used for both naïve a
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Organisms can adapt to increasing ROS
2022-04-13
Organisms can adapt to increasing ROS production by up-regulating antioxidant defences, such as the activities of antioxidant enzymes (Livingstone, 2003). Failure of antioxidant defences to detoxify excess ROS production can lead to significant oxidative damage including enzyme inactivation, protein
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etretinate DNA methylation is a kind of epigenetic modificat
2022-04-12
DNA methylation is a kind of epigenetic modifications that can be described as a heritable alteration in gene expression, without any changes in the DNA sequence. Recent evidences suggest that the regulation of DNA methylation status is a frequent and early event in prostate carcinogenesis. For exam
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br Conflict of Interest Both GM
2022-04-12
Conflict of Interest Both GM and BDH are shareholders in Caldan Therapeutics, a company exploring potential novel treatments for type 2 diabetes. Acknowledgments Work described herein was supported by Biotechnology and Biological Sciences Research Council [grant BB/K019864/1)] (to GM) and [gr
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Here we performed TEM and AFM imaging to study APE
2022-04-12
Here, we performed TEM and AFM imaging to study APE1–DNA interactions. The results showed that APE1 can dynamically polymerize on DNA in an apparently sequence-independent manner. We propose that this protein polymerization allows for scanning of the structural properties of DNA with short residence
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Introduction Adaptations in the metabolism of cancers contri
2022-04-12
Introduction Adaptations in the metabolism of cancers contribute to tumor survival and growth and present opportunities to develop novel therapeutic strategies (Kelloff et al., 2005, Som et al., 1980). In particular, glutamine metabolism plays such an important role in cancer growth that a phenome
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Next the effects of a phenyl group at the and
2022-04-12
Next, the effects of a phenyl group at the 3- and 4-positions of the furan on GCGR affinity were investigated (). Surprisingly, despite the lack of a 4-phenyl group at the furan, compound exhibited almost the same GCGR affinity as compound . On the other hand, when the phenyl group at the 3-positio
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Some of the key aspects of the
2022-04-12
Some of the key aspects of the myofibroblasts’ biology, including their signaling sensitivity and residual regenerative potential, are shaped by their origin. In this respect, lineage studies on myofibroblast precursors are critical for increasing our understanding of the natural history of fibrosis
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Ulimorelin also known as TPZ is a macrocyclic molecule that
2022-04-12
Ulimorelin, also known as TPZ101, is a macrocyclic molecule that is a potent agonist of the ghrelin receptor (Hoveyda et al., 2011). Due to its ability to stimulate gastrointestinal motility, ulimorelin has been evaluated as a possible treatment in gastroparesis (Ejskjaer et al., 2010), ileus (Frase
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br Ethics approval br Availability of data and
2022-04-12
Ethics approval Availability of data and materials Consent for publication Competing interests Authors contributions Introduction Glucose supply to tissues is maintained through a complex regulatory network mostly driven by the pancreatic hormones insulin and glucagon which control
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Three main mechanisms have been
2022-04-11
Three main mechanisms have been proposed for the secretion of active forms of hedgehog ligands: first, construction of a multimeric molecule with lipid moieties placed on the inside, making a soluble Hh protein which can diffuse from the membrane; second, function of dispatched proteins through pack
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br Intracellular trafficking with concurrent signaling of NP
2022-04-11
Intracellular trafficking with concurrent signaling of NPRA Our recent studies have shown internalization and concurrent signaling of NPRA in subcellular compartments; this had not been previously demonstrated [26,42]. Preparation of the enhanced GFP (eGFP)-tagged NPRA (eGFP-NPRA) construct has g
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