• The subnuclear localizations of redox regulators is also lar

  2023-01-30

  

  The subnuclear localizations of redox regulators is also largely unknown. The potential role of thiol reductases as transcription regulators or DNA repair molecules may suggest an association to DNA. In this way, the presence of a zinc finger domain potentially involved in protein/DNA interactions o

• br Acknowledgments br Introduction Alzheimer s disease AD is

  2023-01-29

  

  Acknowledgments Introduction Alzheimer's disease (AD) is a severe neurodegenerative disorder primarily affecting the elderly population. Senile plaques in the brain, one of the pathological hallmarks of AD, are formed by the accumulation of aggregated β-amyloid (Aβ) with an extensive β-sheet s

• In this study we designed and synthesized two ALK

  2023-01-29

  

  In this study, we designed and synthesized two ALK PROTACs (degraders), 5 (MS4077) and 6 (MS4078), by linking ceritinib and pomalidomide [45] through two different linkers. Using human ALCL and NSCLC cells, we characterized both compounds in a battery of assays to demonstrate their effects on reduci

• br Rapid nongenomic effects of corticosterone in an

  2023-01-29

  

  Rapid nongenomic effects of corticosterone in an amphibian model Studies in the model organism, the roughskin newt, Taricha granulosa, over 30 years ago led to the discovery that stress can rapidly (within minutes) suppress sexual behavior (amplectic clasping) of male T. granulosa, an effect that

• br Role of OCT in histamine clearance Histamine is

  2023-01-29

  

  Role of OCT3 in histamine clearance Histamine is a powerful neuromodulator, as well as a regulator of immune processes and vascular tone in the central nervous system (Gross, 1981; Haas et al., 2008; Jutel et al., 2006). In contrast to 5-HT and the catecholamines, a high-affinity transporter for

• The putative physiological meaning of epinephrine

  2023-01-29

  

  The putative physiological meaning of epinephrine-related hepatic drug transporter regulation remains to be established. It is nevertheless noteworthy that the catecholamine rather decreases expression of sinusoidal SLC transporters like NTCP, OAT2, OAT7, OCT1, OATP1B1 and OATP2B1 whereas those of c

• Notably both circulating adiponectin and

  2023-01-29

  

  Notably, both circulating adiponectin and adipsin were equally diminished by about 50% in Arfrp1 mice consistent with several studies reporting overlapping trafficking routes for their secretion from 3T3-L1 Limitations which was strikingly inhibited upon ablation of TfR-positive endosomes [18,26,33

• br Functional consequences of ADK regulation on astrocyte fu

  2023-01-29

  

  Functional consequences of ADK regulation on astrocyte function As outlined above (see introduction), ADK critically regulates the extracellular adenosine levels in Amyloid β-peptide (10-35), amide (Boison, 2006, Etherington et al., 2009). Changes in the levels of adenosine, as a result of the r

• A high throughput small molecule ACK

  2023-01-29

  

  A high-throughput small molecule ACK1 biochemical inhibition screen was performed in-house and led to the identification of 1μM inhibitor furanopyrimidine (). Further binding studies found N-Nonyldeoxynojirimycin to be both ATP-competitive and reversible. Early structure-activity relationship (SAR)

• Tacrine an aminoacridine derivative Fig A was the

  2023-01-29

  

  Tacrine, an aminoacridine derivative (Fig. 1, A), was the first AChE inhibitor approved for treatment of AD [12], [13]. This compound was withdrawn from the market due to its hepatotoxicity [14]. In spite of tacrine's side effects, it is still an attractive lead compound for medicinal chemists due t

• In the present study the alternative splicing of

  2023-01-29

  

  In the present study, the alternative splicing of several nAChR subunits was identified in the oriental migratory locust (Locusta migratoria manilensis Meyen), a serious worldwide pest to agricultural production and also a model insect species [5]. Several α subunits were tried to co-express with ra

• Another significant group of reductase inhibitors is the ste

  2023-01-29

  

  Another significant group of 5α-reductase inhibitors is the steroidal 3-carboxylic ras inhibitor sale derivatives (relevant examples in Fig. 5), which were designed to mimic the putative enzyme-bound enolate intermediate. This was achieved by introducing sp2-hybridized centers at C3 and C4 and an an

• br Materials and methods br Results The clinical characteris

  2023-01-29

  

  Materials and methods Results The clinical characteristics of the two selected groups are shown in Table 1. As shown in Table 1, the enzyme activity of ATX in CSF of MS patients (59.90±3.09nmol/min/ml±SEM) was significantly higher (p Discussion Numerous studies have so far shown that ATX tak

• The acidification of endocytic compartments is

  2023-01-29

  

  The acidification of endocytic compartments is closely related to endocytic activity, although the mechanism linking acidification and membrane dynamics is largely unknown. In a recent RNA interference (RNAi)-based screen, V-ATPase depletion blocked the formation of clathrin-coated vesicles, an effe

• There are in contrast many

  2023-01-29

  

  There are in contrast many studies demonstrating that sex steroids modulate 4-IPP processing of stimuli related to reproduction and this correlates with the observation that steroid receptors and aromatase are expressed in many brain nuclei that are part of the olfactory, visual and auditory pathwa

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