• To function as Ub ligases E proteins must

  2019-10-14

  

  To function as Ub-ligases, E3 proteins must interact with E2s. As compared to the extensive studies on E3s, functional studies on E2s are relatively rudimentary in higher plants. We previously reported that there are 48 genes encoding Ub-conjugating (UBC) fold-containing putative E2 proteins in the

• The human serotonin hydroxytryptamine HT receptor

  2019-10-14

  

  The human serotonin (5-hydroxytryptamine; 5-HT) receptor family consists of 14 receptor subtypes to date, which are primarily G protein-coupled receptors (GPCRs) with 5-HT3 being the sole ligand-gated ion channel (Alexander et al., 2017). These receptors are widely distributed in the central and per

• br Acknowledgments br The design

  2019-10-14

  

  Acknowledgments The design of polyaromatic molecules able to bind to DNA is of significant importance for the development of anticancer and fluorescent imaging agents. Among them, 1,8-naphthalimide derivatives have received significant attention and have been extensively investigated for their

• The preferences for source of FAs for DGAT and DGAT

  2019-10-14

  

  The preferences for source of FAs for DGAT1 and DGAT2 are related to their membrane topologies, subcellular locations, interactions with other proteins or organelles (discussed in the former section), and their differential expression, substrate specificities, and enzyme kinetics. According to UniPr

• DDR expression is upregulated in the glomeruli

  2019-10-14

  

  DDR1 expression is upregulated in the glomeruli and tubules of injured kidneys [7], [8], [19]; however, what role this receptor plays in kidney resident Ginsenoside Rb1 and is unclear. A plausible hypothesis is that DDR1 might contribute to kidney injury by directly exerting a pro-fibrotic action. I

• In our model CSF R blockade with PLX mainly targeted

  2019-10-14

  

  In our model, CSF-1R blockade with PLX647 mainly targeted the more abundant MDSCs instead of macrophages, suggesting that the role of CSF-1 may be tumor model-dependent. Different tumor models, genetic backgrounds, or treatments may induce different growth factors or cytokines in the tumor microenvi

• Another breakthrough towards the understanding of

  2019-10-14

  

  Another breakthrough towards the understanding of the mechanisms responsible for stress-induced relapse to drug seeking behaviour is the evidence published by the group of Wise [34] in which they show that the activation of VTA CRF2 and not CRF1 receptors is responsible for stress-mediated relapse t

• We further correlated OPRK and OPRM methylation levels with

  2019-10-14

  

  We further correlated OPRK1 and OPRM1 methylation levels with individual characteristics in Xinjiang Han and Uygur controls. Partial correlation analyses showed that OPRK1 methylation was positively correlated with age in Uygur male controls (r=0.72, p=0.001, adjusted by body mass index (BMI), gluco

• br Results br Discussion The ubiquitin system has in recent

  2019-10-12

  

  Results Discussion The ubiquitin system has in recent years become an exciting area for drug discovery (Cohen and Tcherpakov, 2010), as multiple enzymatic steps within the ubiquitylation process are druggable. The potential of targeting the ubiquitin-proteasome pathway was first demonstrated i

• br Results This study was carried out with a

  2019-10-12

  

  Results This study was carried out with a series of engineered extracellular matrix films of collagen assembled at hydrophobic surfaces, which allow for independent control of supramolecular structure, mechanical stiffness, and receptor recognition sites [17], [21]. Vascular smooth muscle alltran

• Recently a sandwich cultured hepatocyte model has been prove

  2019-10-12

  

  Recently, a sandwich-cultured hepatocyte model has been proved to be a valuable in vitro system that maintains specific hepatic cytomorphology and function relevant to drug metabolism, disposition and toxicity, and thus, closely resembles the in vivo setting. This hepatocyte model was recognized as

• The androgen receptor AR is a steroid hormone receptor

  2019-10-12

  

  The androgen receptor (AR) is a steroid hormone receptor that plays a crucial role in the normal development of male reproductive tissues, and its high expression and/or relaxation of its regulation are strongly implicated in prostate cancer (PCa) [11]. Androgen binding induces conformational change

• Estrogen receptors ERs belong to the third class

  2019-10-12

  

  Estrogen receptors (ERs) belong to the third class of nuclear receptors (NR3) [23]. Two different forms of ER have been described, ERα and ERβ. They are coded by two distinct genes (ESR1 and ESR2, respectively) containing 8 transcribed exons that give rise to six conserved protein domains: domains A

• Raloxifene is a second generation

  2019-10-12

  

  Raloxifene is a second generation SERM that has tissue-specific effects that differ from those of tamoxifen. Raloxifene was marketed for prevention and treatment of osteoporosis in postmenopausal women in the US and Europe. In a phase II randomized double-blind study, tamoxifen and raloxifene were e

• The AURA trial was a phase I II study evaluating

  2019-10-12

  

  The AURA trial was a phase I/II study evaluating the safety, tolerability and activity of Osimertinib in patients with EGFR-mutated NSCLC progressing after a previous EGFR TKI. The phase I component of the study included a dose escalation part (Osimertinib 20mg to 240mg), using a rolling six design,

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