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This hypothesis is in line with our phylogenetic
2021-09-26
This hypothesis is in line with our phylogenetic analysis of FBPase sequences which revealed that vertebrate FBP2 evolved significantly faster than FBP1 (Fig. 2). An average distance between FBP2 and ancestral vertebrate FBPase was higher than that for FBP1. Moreover, preliminary study on amphibia
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In the Medicines for Malaria Venture MMV
2021-09-26
In 2011 the Medicines for Malaria Venture (MMV) distributed the Open-Access Malaria Box to accelerate antimalarial drug discovery (Spangenberg et al., 2013). The Malaria Box consists of 400 structurally diverse compounds, curated from >20,000 hits generated from large-scale screens, that inhibit the
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Vicriviroc Malate Sperm capacitation was negatively r p rela
2021-09-26
Sperm capacitation was negatively (r = −0.68; p ive but not significant (r = 0.22). No significant relationship was observed between the expression levels of either CB1 receptor or FAAH and any of the sperm quality parameters studied. The scatter plot distribution of spermatozoa expression of CB1 an
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We have expanded these studies by doing EEG recording in
2021-09-26
We have expanded these studies by doing EEG recording in the ET-1 model. Using this technique, we demonstrated that activation of either the ETA ML-099 or the ETB receptor induces electrical seizures. ET-1 induced electrical seizures occurred in the presence of either the ETA receptor antagonist or
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br Experimental procedures br Conflicts of interests br
2021-09-26
Experimental procedures Conflicts of interests Introduction Here we investigate differences in growth properties and short-term morphological changes in response to ET-1 in Chinese hamster ovary (CHO) cells stably and separately expressing ETA or ETB receptors. A stably transfected CHO syst
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During the course of the development of aminothiazole derive
2021-09-26
During the course of the development of aminothiazole-derived small molecule GSMs, SGSM-36 (Fig. 1A) was discovered and exhibited good activity for suppressing the production of Aβ42 (Aβ42 IC50=63nM) (Rynearson et al., 2016; Wagner et al., 2014). In addition, SGSM-36 exhibited improved physicochemic
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br Discussion br Concluding remarks There are
2021-09-26
Discussion Concluding remarks There are potentially hundreds or thousands of G-quadruplexes which form within promoters, telomeres, RNA transcripts, and even LINEs and SINES [9,11,121,122]. As articulated previously [27], G-quadruplexes are easily targetable with heterocyclic aromatic compound
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GPR which is also known as
2021-09-26
GPR40, which is also known as FFA receptor 1 (FFAR1 or FFA1), was identified as an orphan receptor in the search for novel human galanin receptor (GALR) subtypes in 1997. Using reverse pharmacology approaches measuring calcium transients, GPR40 were deorphanized and characterized as being activated
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Having shown that some of substitutions Cl CF
2021-09-26
Having shown that some of substitutions (Cl, CF) at the 2-position of the thiophene improved rat microsomal stability, and polar groups at the 4-position of the aryl ring had a beneficial effect on stability in both human and rat microsomes, we combined these features in a new set of analogs. Methyl
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OS has a key role
2021-09-26
OS has a key role in the pathogenesis of micro- and macrovascular diabetic complications [3]. There is now convincing evidence that the enzymes that generate ROS and gasotransmitters, such as nitric oxide (NO) and CO, are redox regulated at both the transcription and activity levels, and are also im
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Introduction Histamine Imidazolyl ethylamine is an
2021-09-26
Introduction Histamine [2-(4-Imidazolyl)-ethylamine] is an important mediator of many physiological and pathological processes including inflammation, gastric Bufalin sale secretion, neuromodulation, regulation of immune function, cell proliferation and differentiation, among others. Histamine exer
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In conclusion studies of the
2021-09-26
In conclusion, studies of the regulation of the HO-1/BVR/CO pathway by selective pharmacological approaches may lead to the discovery of novel compounds for the treatment of diverse diseases. Recent results validate the use of advances in targeting HO-1 in various vascular diseases. However, there a
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While phosphorylation site motifs are typically
2021-09-24
While BTB06584 site motifs are typically described in terms of residues that promote phosphorylation, negatively selected residues can also be an important component of substrate recognition. Such ‘forbidden’ resides can act as a filter to prevent phosphorylation of a site by the ‘wrong’ kinase, whi
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In this study using the
2021-09-24
In this study, using the RBD (Byr2)-GST pull-down assay associated with mass spectrometry, we also detected some kinases interacting with Ras-GTP under NO treatment. Among the kinases identified by mass spectrometry, we highlight Ste11 (designated Byr2 in S. pombe), Ste7 (Byr1) and Hog1. Interesting
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br Acknowledgement br Introduction Malignant melanoma is an
2021-09-24
Acknowledgement Introduction Malignant melanoma is an aggressive and highly metastatic cancer. The incidence of malignant melanoma is increasing all over the world, and the population of patients with advanced melanoma is growing [1], [2]. Malignant melanoma is often resistant to conventional
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