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br Materials and methods br Results
2021-02-08
Materials and methods Results Discussion The oestrogen agonist properties and androgen antagonist activities of parabens have been well documented by a variety of in vitro and in vivo assay systems over the past decade (Chen et al., 2007, Darbre and Harvey, 2008, Golden et al., 2005). To th
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br Material and methods br Results
2021-02-08
Material and methods Results and discussion Conclusions Prostanoid-E receptor selective antagonists that inhibit EP2 or EP4 receptor activities may be used as a pharmacological strategy to limit cyst formation and ADPKD progression. Our study follows on from our previous observations of the
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br Iterative design approach overview An
2021-02-08
Iterative design approach overview An iterative design strategy is used to identify a peptidase-resistant reporter that acts as an efficient substrate for kinases in cell lysates as well as intact cells (Fig. 1). In this process, small-scale, rationally designed libraries are used to screen pepti
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The development of novel approaches to
2021-02-08
The development of novel approaches to study GPCR-mediated transactivation in live Luciferase Reporter Assay Kit receptor is important, and this study describes a unique BRET-based quantification of Grb2 recruitment to the EGFR as a direct readout of GPCR-mediated transactivation. We have previously
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In the context of E ligase
2021-02-08
In the context of E3 ligase drug discovery, it is critical to identify the appropriate E2/E3 substrate pairing to ensure the development and use of the most physiologically relevant screening assay. There have been many reports of limited E2/E3 activity profiling with a small number of E2 and E3 LY
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iso 1 sale br Acknowledgement br Introduction Human dihydroo
2021-02-08
Acknowledgement Introduction Human dihydroorotate dehydrogenase (hDHODH), a flavin-dependent mitochondrial enzyme involved in de novo iso 1 sale biosynthesis, is a validated therapeutic target for the treatment of autoimmune diseases such as rheumatoid arthritis and cancer [1], [2], [3]. Leflu
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As shown in Fig there are two
2021-02-08
As shown in Fig. 9, there are two mechanisms for the removal of the Va-acyl group from PC to make it available for incorporation into TAG with DGATs' acting at the final acylation step. ①: Transfer of Va from PC to the acyl-CoA pool. This process can be driven by the reverse action of acyl- CoA:lyso
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Endothelins ETs are peptides expressed in both the
2021-02-07
Endothelins (ETs) are peptides expressed in both the peripheral and the central nervous systems, which can contribute to sensory changes seen in animal models of inflammatory, cancer and neuropathic pain [10], [11]. All three mammalian isoforms (ET-1, ET-2 and ET-3) activate specific G protein-coupl
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The mechanism by which OC use leads to
2021-02-07
The mechanism by which OC use leads to impaired glucose tolerance is yet to be fully clarified. Decreased insulin sensitivity appears to be mainly accounted for by estrogenic component and this effect may be modified by progestogenic component [14], [15]. Estrogenic effect on glucose tolerance has b
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br Conflicts of interest br Author
2021-02-07
Conflicts of interest Author contributions Acknowledgements This work was supported by the University of Brescia (ex 60%) and Siderurgica Leonessa research funds to AF. RR was supported by Associazione Italiana per la Ricerca sul Cancro - AIRC (MFAG 18459 grant). We are grateful to Umberto
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Introduction Psoriasis is a chronic recurrent and inflammato
2021-02-07
Introduction Psoriasis is a chronic, recurrent and inflammatory skin disease, and it is characterized by erythema, skin hyperplasia, scales, and hyperproliferation of keratinocyte [1]. It is reported that the psoriasis occurrences are about 3% worldwide [2], but the number varies depending on ethni
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In the present study it was
2021-02-07
In the present study, it was particularly of interest that intravesical administration of PGE2 evoked ONO-8130-reversible rapid phosphorylation of ERK in the L6 spinal cord. Detection of phosphorylated ERK is now often used as a marker for somatic and visceral nociception, including read full post
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What are the molecular signals that guide
2021-02-07
What are the molecular signals that guide Tfh cells as they navigate around the lymph node in the course of the immune response? It was recently reported that Tfh cells inside GCs have high expression of SIPR2, which acts to repel them from the S1P-rich lymph in the SCS and promote their retention i
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In humans several different small ubiquitin related modifier
2021-02-07
In humans, several different small ubiquitin-related modifier (SUMO) paralogs can be conjugated to cellular proteins. The human genome codes for five SUMO paralogs (SUMO1–5); of these, SUMO1 and the almost identical SUMO2 and SUMO3 are ubiquitously expressed. Sumoylation is executed by an enzymatic
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We next focused our design building
2021-02-07
We next focused our design building into the ribose binding site, which had not been yet utilized in this effort. Compounds bearing a series of five-membered aromatic heterocycles (compound , ) showed reduced inhibition of the Gram-positive isozymes compared with compound , but a 20-fold improved po
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