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RSL3 The androgen receptor AR is a steroid hormone
2021-02-08

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
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Recent data obtained with etifoxine suggest that
2021-02-08

Recent data obtained with etifoxine suggest that facilitation of GABAergic inhibition may be also associated with an indirect mechanism implying activation of the peripheral benzodiazepine receptor with a subsequent increase in neurosteroid production (Schlichter et al., 2000, Verleye et al., 2005).
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Under conditions of energy scarcity or nutritional restricti
2021-02-08

Under conditions of energy scarcity or nutritional restriction, AMPK, a critical energy sensor, is activated in response to the increased ratio of AMP to ATP. Various kinases may phosphorylate AMPK, leading to its activation. For example, AMPK phosphorylation by liver kinase B 1 (LKB1) at Thr172 res
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P H is a nonheme iron II dioxygenase that uses
2021-02-08

P4H is a nonheme iron(II) dioxygenase that uses O2 and α-ketoglutarate as co-substrates (Fig. 1A). The three-dimensional structure of mammalian P4H is unknown. We reasoned that an electrophilic analog of α-ketoglutarate could serve as an irreversible inhibitor of the enzyme and, hence, a useful prob
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Thus the understanding of the various mechanisms
2021-02-08

Thus, the understanding of the various mechanisms of action of estrogen and SERMs is an important medical challenge and could help to develop an “ideal” SERM, preserving the beneficial effects of estrogen in the bone and urogenital system, and reducing the unwanted side effects, mainly increased ris
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Recent studies have shown that the extracellular regulated p
2021-02-08

Recent studies have shown that the extracellular regulated protein kinase 1 and 2 (ERK1 and ERK2), commonly referred to collectively as ERK 1/2, are members of the mitogen-activated protein kinase (MAPK) family. This family of kinases transport signals from the surface of the cell to the nucleus, th
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br Disclosure statement br Acknowledgment This work was supp
2021-02-08

Disclosure statement Acknowledgment This work was supported by the National Natural Science Foundation of China (81270704, 81330018). Background Over-expression of cyclooxygenase-2 (COX-2) is common in many malignancies including non-small cell lung cancer (NSCLC) and is associated with po
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Artificial permutations have also been exploited by protein
2021-02-08

Artificial permutations have also been exploited by protein engineering to manipulate protein scaffolds, in order to improve catalytic activity, alter substrate or ligand binding affinity, reduce proteolytic susceptibility, increase stability, generate different aggregation states and improve fluore
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Introduction Ubiquitylation is a post
2021-02-08

Introduction Ubiquitylation is a post-translational modification which impacts almost every biological process in the cell. Dysregulation of the ubiquitylation pathway is associated with several diseases, including cancer, neurodegenerative disorders, and immunological dysfunctions. Single ubiquiti
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br Methods br Results br Discussion Skin biopsy
2021-02-08

Methods Results Discussion Skin biopsy and microneurography have both been described as useful tools in the diagnosis of PAN, directly identifying peripheral sympathetic fibers without the mediation of specific apiii receptor organs (Donadio et al., 2005, Donadio et al., 2012a, Donadio and
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br Discussion The biochemical separation of
2021-02-08

Discussion The biochemical separation of exonuclease activity from DNA-PK dependent endonuclease activity reported in this manuscript is consistent with genetic separation of Artemis enzymatic activity. Mutations in the protein which result in disruption of endonuclease activity have no effect on
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DGK is not the only
2021-02-08

DGKε is not the only DGK isoform that has been associated with p53. It has been shown that DGKζ binds to p53 and modulates its activity in both the cytoplasm and the nucleus [39]. In the cytosol DGKζ promotes the degradation of p53 through the ubiquitin-proteosome system [39], also a likely mechanis
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Raloxifene HCl Unexpectedly CRF receptor agonist and antagon
2021-02-07

Unexpectedly, CRF2 receptor agonist and antagonist evoked similar effects in the fall in tail skin temperature caused by restraint. However, Ucn3 reduced basal values of tail skin temperature, thus indicating that some degree of basal vasoconstriction caused by BNST treatment with Ucn3 may have cont
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br Advantages of modified proteins over unmodified
2021-02-07

Advantages of modified proteins over unmodified ones In contrast to small-molecule drugs, proteins are readily amenable to site-specific alterations through genetic engineering. In principle, therefore, it is possible to build in features that allow them to remain active for longer in the body an
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HO-3867 receptor The first mammalian mutation linked to CR
2021-02-07

The first mammalian mutation linked to CR was identified in golden hamsters (Mesocricetus auratus). The mutation was an autosomal allele first described in the late 1980s [8] and was identified using positional cloning [9]. These animals displayed a shortened period length (20h in homozygous animals
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