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According to the literature HER
2021-11-24

According to the literature, HER2 mutations are present in 2–4% of lung adenocarcinoma (ADC) patients. Most HER2 mutations are in-frame insertional mutations occurring at exon 20 in the protein kinase domain [[2], [3], [4], [5]]. Although several small molecules and HER2 GDC-0941 have been tested f
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Norfloxacin hydrochloride Preadipocytes are capable of diffe
2021-11-24

Preadipocytes are capable of differentiating into lipid-laden mature adipocytes. Lipid droplets are a prominent morphological feature of mature adipocytes, which is accumulated and maintained during adipocytes differentiation [26]. In this study, rHhip treatment increased lipid accumulation, as well
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NCSs are helical proteins containing four EF hand motifs
2021-11-23

NCSs are α-helical proteins containing four EF-hand motifs with EF1 being incapable of Ca-binding throughout the family (atomic-resolution structure was firstly resolved for recoverin [5]; for review on NCS structure, see [6]). Some of the NCS proteins (i.e. recoverin and KChIP3) have two while othe
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The stress of accelerated lactate production in cancer cells
2021-11-23

The stress of accelerated lactate production in cancer DHAP receptor is moderated by the overexpression of lactate transporters – symporters for lactate anions and protons called monocarboxylate transporters (MCTs) – that are capable of bidirectional transport depending on the environmental and/or c
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In conclusion GPR inhibits and GPR enhances
2021-11-23

In conclusion, GPR120 inhibits and GPR40 enhances the cell motile activity stimulated by TPA in melanoma cells, while MMP-9 activation was reduced by GPR40. In contrast, GPR40 negatively regulated cellular functions of fibrosarcoma LCL161 [11]. Taken together, it is suggested that opposite effects
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Previously we reported that the inhibition of PKC and PKC
2021-11-23

Previously, we reported that the inhibition of PKC-ζ and PKC-ε activity in hypertrophic adipocytes had deleterious effects on EPA-induced GPR120-mediated VEGF-A production [12]. However, the activation of PKC-θ, -ζ and -λ can also enhance the phosphorylation of IKK and p65, and facilitate the transl
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Typically upon chronic agonist exposure GPCRs
2021-11-23

Typically, upon chronic agonist exposure GPCRs undergo desensitization and internalization resulting in a loss of receptor responsiveness over time (Drake et al., 2006, Kelly et al., 2008). However, not all GPCR systems conform to this model of acute agonist-mediated regulation. Some receptors have
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To investigate if such an
2021-11-23

To investigate if such an effect is observed in native GlyT1, we introduced S605D and S605A mutations into GlyT1 and transfected these DNA constructs into N2a cells. For an internal control of calpain cleavage, we also introduced the first 100 amino-acids of the rat GlyT2N terminus upstream of the m
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Introduction Cancer is known as a
2021-11-23

Introduction Cancer is known as a renegade system of expansion that initiate in human body. It is distinguished, in spite of its category, by one universal characteristic, which is uncontrolled cell division. Cancerous regulator of g protein signaling have the ability to bypass the normal apoptosi
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In insects structural cuticular proteins CPs play important
2021-11-23

In insects, structural cuticular proteins (CPs) play important roles in determining the diverse physical properties of the cuticle, depending on developmental stages, as well as different body regions, as a result of interactions with other CPs and the structural biopolymer chitin [4]. Many studies
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During pain signal transmission glutamate is released into t
2021-11-23

During pain signal transmission, glutamate is released into the synaptic cleft, which, in turn, causes activation of N-methyl-d-aspartate (NMDA) receptors and hence neurotransmission across the synapse occurs. The synaptic concentration and resultant activity of glutamate are controlled by excitator
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During the course of the development of aminothiazole derive
2021-11-23

During the course of the development of aminothiazole-derived small molecule GSMs, SGSM-36 (Fig. 1A) was discovered and exhibited good activity for suppressing the production of Aβ42 (Aβ42 IC50=63nM) (Rynearson et al., 2016; Wagner et al., 2014). In addition, SGSM-36 exhibited improved physicochemic
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The effects of FFAR and FFAR activation in different
2021-11-23

The effects of FFAR1 and FFAR2 activation in different tissues have been reported in several species (Hara et al., 2014). Herein, we report the first evidence for differential expression of FFAR1 and FFAR2 during the peripartal period in the liver of dairy cows that differ in liver metabolism, based
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One effective approach to fine tuning the lipophilicity
2021-11-23

One effective approach to fine-tuning the lipophilicity profile of FFA1 agonists is to ‘decorate’ the 3-phenylpropahoic PRX-08066 receptor scaffold with polar heterocyclic moieties. Alternatively, this scaffold could be replaced with heterocyclic isosteres (as in Takeda’s compounds 1,2 and 3 as wel
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br Introduction The nature of chemotherapies is
2021-11-22

Introduction The nature of chemotherapies is to relieve the tumor burden of the patients by eliminating cancer Temozolomide via inducing cell death, mostly regulated cell death represented by apoptosis [1,2]. Dozens of anticancer agents including clinically used ones kill cancer cells by promoti
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