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In untreated rodent or human hepatocytes PXR or CAR
2020-01-21
In untreated rodent or human hepatocytes, PXR or CAR is stabilized by cytoplasmic co-chaperone partners like heat shock protein 90 (HSP90, Fig. 1). Upon ligand binding, the nuclear receptors are freed and translocated into the nucleus, identified as a pivotal step in PXR- or CAR-mediated transactiva
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Considering the protumoral functions of TAMs new therapies a
2020-01-21
Considering the protumoral functions of TAMs, new therapies against TAMs have recently gained interest. Such treatments, particularly inhibitors of the colony stimulating factor 1 receptor (CSF-1R), are currently evaluated in several clinical trials [19]. CSF-1R inhibitors may also be of interest in
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Another option is to use the
2020-01-21
Another option is to use the thiol groups of cysteine residues, which can be modified by use of PEG-maleimide and vinyl sulfone. However, changes in PEGylation interactions or reaction conditions can result in changes in the functional properties of the therapeutic proteins [[50], [51], [52]]. A st
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The first mammalian mutation linked to CR
2020-01-21
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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The nucleus accumbens is a critical locus for ER
2020-01-21
The nucleus accumbens is a critical locus for ER/mGluR signaling in the context of addiction ER/mGluR signaling is regulated by caveolin proteins and palmitoylation Because of the vast implications of ER/mGluR association, it is important to understand what regulates their interaction. Such regu
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Otherwise ES cells express high level of histone lysine
2020-01-21
Otherwise, ES Voreloxin express high level of histone lysine specific demethylase 1 (LSD1) expression. In this context, it is proposed that LSD1 inhibition may block the function of EWS-ETS proteins [70]. Furthermore, checkpoint kinase 1 (CHK1), a modulator of cell survival under the condition of i
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Cytochromes P CYP are a superfamily of
2020-01-20
Cytochromes P450 (CYP 450) are a superfamily of hemoproteins containing a heme cofactor, which are widely distributed in animals, plants and microbes (Hannemann et al., 2007). CYP450 exhibits a variety of biological functions including biotransformation of drugs, detoxification of endogenous and xen
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guanylate cyclase The CYP D inferred metabolizer phenotype
2020-01-20
The CYP2D6-inferred metabolizer phenotype describes only one phase of the tramadol (T) ADME (absorption, distribution, metabolism, and excretion) and response process and does not explain all genotypic contribution of an individual’s phenotypic expression [11]. Numerous polymorphisms in the downstre
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br Disclaimer Statement br Introduction The erythropoietin p
2020-01-20
Disclaimer Statement Introduction The erythropoietin-producing hepatoma (Eph) receptors represent the largest class of receptor tyrosine kinases (RTKs). They are type I transmembrane proteins that interact with their membrane-bound ligands the ephrins and facilitate cell-to-cell contacts resul
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Enzyme mimics belong to a type of rising catalysts which
2020-01-20
Enzyme mimics belong to a type of rising catalysts which show the similar function with their corresponding natural enzymes [20], [21], [22], [23], [24], [25], [26], [27], although their structures are different from natural enzymes. In the area of prodrug activation, the widely-used enzyme mimics a
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Introduction CYP is a superfamily of heme
2020-01-20
Introduction CYP450 is a superfamily of heme-containing monooxygenases, many of which are expressed in the liver, and they are significant phase-I Lesinurad in drug metabolism and detoxification. There are three subfamilies (CYP1, CYP2 and CYP3) that are mainly involved in the metabolism of drugs
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ApicomplexansApicomplexans are unicellular and spore forming
2020-01-20
ApicomplexansApicomplexans are unicellular and spore-forming obligate intracellular parasites that occupy diverse host niches (Mogi and Kita 2010). They have remodeled mitochondrial carbon and energy metabolism through reductive evolution. The development of novel drugs is now a very serious challen
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AMPK is a master regulator of metabolic homeostasis
2020-01-20
AMPK is a master regulator of metabolic homeostasis, its broad spectrum of metabolic activities makes it an attractive target for treatment of metabolic and related disorders including Diabetes and Obesity (Madhavi et al., 2018). It controls lipid metabolism through its target genes PPAR-γ, C/EBP-α
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The aim of the present
2020-01-20
The aim of the present study was to investigate the acute effects of THC on resting state 740 Y-P neurophysiology, and to examine the impact of COMT genotype on these effects. Thirty-nine healthy volunteers participated in a randomised, placebo-controlled, crossover pharmacological MRI study. Acute
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br Results br Discussion Here
2020-01-20
Results Discussion Here we establish a key kinase cascade that acts at PCs to promote homolog pairing and synapsis. CHK-2 phosphorylates the zinc finger proteins that specify PCs, which, in turn, primes their recruitment of PLK-2 (Figure 7D). By recruiting these two kinases, PCs serve as signa
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