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From the general synthetic route we first synthesized
2021-01-26
From the general synthetic route, we first synthesized a directed set of analogues of general formula , keeping the synthesis simple by using a symmetrical pyrazole (R=R=Me). The SAR of a set of 30 compounds in the GTPγS binding assay turned out to be quite tight: only 4 (13%) compounds showed moder
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The aim of the present study was to investigate the
2021-01-26
The aim of the present study was to investigate the acute effects of THC on resting state bupropion hydrochloride neurophysiology, and to examine the impact of COMT genotype on these effects. Thirty-nine healthy volunteers participated in a randomised, placebo-controlled, crossover pharmacological
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Cholesterol homeostasis is maintained through
2021-01-26
Cholesterol homeostasis is maintained through a tight regulation between endogenous de novo synthesis, dietary absorption, utilization and excretion of bile salts. The 7915 of cholesterol from the intestine constitutes the central part of cholesterol homeostasis in the body [41]. In particular, the
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SS is a high grade malignant
2021-01-26
SS is a high-grade malignant soft tissue sarcoma accounting for 5%–10% of soft tissue sarcomas. After RMS, SS is the most common sarcoma in children, adolescents and young adults [9]. SS originates primarily in the lower (62%) and upper (21%) extremities but may occur at any anatomic site [9], [10].
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br Introduction Breast cancer is the most common malignant t
2021-01-26
Introduction Breast cancer is the most common malignant tumor in women and the second leading cause of female death [1]. In recent years, with the improvement of early detection and the emergence of new treatment methods, the mortality rate of breast cancer has been greatly reduced. However, the
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br Discussion The etiology of autoimmune diseases including
2021-01-26
Discussion The etiology of autoimmune diseases including psoriasis is intricate and a composite of environmental and biological factors. There are very limited studies available that report the association analysis of ACE I/D polymorphism with psoriasis risk. In the current study we report on ass
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Here we explored the relative contribution of D like
2021-01-25
Here we explored the relative contribution of D1-like and D2-like receptor subtypes in the control of glutamate release, as well as their pharmacological properties and their interactions modulating the release. The pharmacological parameters (EC50 and Emax) of dopamine for the different types of re
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DNA bound Ku proteins recruit DNA PKcs and thereby transloca
2021-01-25
DNA-bound Ku proteins recruit DNA-PKcs; and thereby translocate into the duplex by one helical turn, leaving DNA-PKcs near the DNA terminus to assist in tethering the broken ends together [25]. In addition to keeping the DSBs in close proximity, DNA-PKcs may prevent exonucleolytic degradation of the
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br Structural and biochemical features of
2021-01-25
Structural and biochemical features of pol X family polymerases The X-family DNA polymerase (polX) is specialized in DNA repair. This family is composed of four different DNA polymerases: pol β, pol λ, pol μ and TdT. Only three members of the polX family possess an N-terminal BRCT (BRCA1 carboxy-
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br Expression and Purification of Atg and Atg
2021-01-25
Expression and Purification of Atg4 and Atg8 Proteins for In Vitro Assays Measurement of Atg4 Activity In Vitro and Ex Vivo Kinetics Analysis of Atg4 Enzymes Summary Atg4 proteases play a crucial role in preparing Atg8 for conjugation to lipid membranes and for the deconjugation of Atg8
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br Conclusions Taken together the
2021-01-25
Conclusions Taken together, the roles of CDK8 and miR-152-3p in the process of HCC likely performed opposite effect completely. Both CDK8 and miR-152-3p could serve as the independent prognostic factors for predicting the OS and DFS in HCC patients. We identified that miR-152-3p as a post-transcr
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Acidic substituents showed moderate biochemical activity
2021-01-25
Acidic substituents () showed moderate biochemical activity, but these compounds showed reduced cellular potency. Additional compounds bearing a carboxylic s6 kinase were also prepared and tested (data not shown). All of acidic compounds showed low cellular potency regardless of their biochemical a
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Apart from neutrophil mediated inflammation the production o
2021-01-25
Apart from neutrophil-mediated inflammation, the production of pro-inflammatory cytokines and chemokines from PGD2/CRTH2 activated macrophages could further aggravate LPS-induced lung injury (Eguchi et al., 2011; Jandl et al., 2016). Interestingly, genetic ablation of CRTH2 diminishes the TNF-α prod
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An intriguing feature of the pre and postsynaptic
2021-01-25
An intriguing feature of the pre and postsynaptic processes at the level of the VTA that have been shown to be mediated by CRF2 receptors [9], [34] is that they are exerted only by agonists with high affinity for both CRF2 receptors and CRF-BP. The four endogenous peptides of the CRF system have hig
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Conversely to the reduction in restraint
2021-01-25
Conversely to the reduction in restraint-evoked HR increase following the blockade of CRF receptors, Nijsen et al. [28] demonstrated that BNST treatment with a nonselective CRF Berbamine hydrochloride mg antagonist enhanced the tachycardia evoked by contextual fear conditioning. Taken together, the
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