• Sumatriptan Our previous high throughput screening HTS campa

  2020-08-26

  

  Our previous high-throughput screening (HTS) campaign using automated, robust, and sensitive fluorescence based Sumatriptan assay [10], [11] led to the identification of several EPAC specific inhibitors (ESIs), and was subsequently followed by extensive hit-to-lead optimizations [20], [21], [22], [2

• Results are expressed as mean

  2020-08-26

  

  Results are expressed as mean±s.e.m. Paired or unpaired Student\'s t test was used for comparisons between 2 groups and one-way ANOVA followed by Bonferroni\'s post-test for more groups. Statistical significance was assigned if p Results and discussion Variations in [Ca2+]i in cardiomyocytes loade

• Given the molecular pharmacology and in

  2020-08-26

  

  Given the molecular pharmacology and in vitro metabolism data, we proceeded to evaluate the in vivo pharmacokinetics of . Mice (=3) were subsequently administered a subcutaneous dose (5mg/kg) with intermittent plasma collections to measure systemic levels of (). Compound achieved a maximum plasma

• ICT is a product of icariin via the metabolism of

  2020-08-26

  

  ICT is a product of icariin via the metabolism of intestinal bacteria with estrogen-like activities [33]. ICT as a bone-protecting agent can enhance osteoblast differentiation while suppressing osteoclastic differentiation in vitro [19], and stimulate osteogenic differentiation and inhibit adipogene

• The human serotonin hydroxytryptamine HT receptor

  2020-08-26

  

  The human serotonin (5-hydroxytryptamine; 5-HT) receptor family consists of 14 receptor subtypes to date, which are primarily G protein-coupled receptors (GPCRs) with 5-HT3 being the sole ligand-gated ion channel (Alexander et al., 2017). These receptors are widely distributed in the central and per

• Addressing whether impaired activation of

  2020-08-26

  

  Addressing whether impaired activation of D1 and D2 receptors regulates memory capacity is relevant for all human pathologies that lead to reduced activation of these Kartogenin australia pathways, such as ageing [39], certain genetic polymorphisms [40] and neurodegenerative disorders. In this study

• br Results br Discussion C is related

  2020-08-26

  

  Results Discussion C4 is related to another VACV protein, C16, and the C-terminal domain of C16 also inhibits DNA-PK-mediated DNA sensing via the same mechanism and to a similar level as C4. Moreover, mutagenesis of C16 at the CYC residues equivalent to those in C4 abrogated the C16-Ku interac

• Several authors have been pursuing the aim of finding good

  2020-08-26

  

  Several authors have been pursuing the aim of finding good performing organic solvent compatible adsorbers useful in the context of API purification [[10], [11], [12], [13], 22, 23]. For sulfonate GTIs, scavenging nucleophilic resins [22, 23] or molecular imprinted polymers (MIPs) [10] have been exp

• br Introduction The development of non melanoma skin

  2020-08-24

  

  Introduction The development of non-melanoma skin cancer (NMSC) is a complex process characterized by the acquisition of altered proliferation and invasiveness. These changes are classically defined as occurring in stages, i.e., initiation, promotion, and progression. In the two-stage model of in

• br Introduction Cerebral stroke causes an efflux of various

  2020-08-24

  

  Introduction Cerebral stroke causes an efflux of various groups of progenitor and stem cells from bone marrow to bloodstream and the levels of these cells correlate with neurological status of stroke patients (Gójska-Grymajło et al., 2012, 2018). It is thought that paracrine factors produced by t

• As an endogenous negative modulator CRBN inhibits

  2020-08-24

  

  As an endogenous negative modulator, CRBN inhibits AMPK’s activation (phosphorylation of Thr172) by directly binding to the α-subunit of AMPK, disrupting γ-subunit recruitment to the AMPK complex (Lee et al., 2011, Lee et al., 2013). In our study, we did not focus on AMPK activation, since only a si

• The question arises as to how the massive

  2020-08-24

  

  The question arises as to how the massive conformational changes determining whether APC/CCDC20–MCC is inhibited or able to catalyze MCC ubiquitylation are naturally controlled? This transition likely involves APC/C regions near the subunit APC15, because reducing cellular APC15 levels stabilizes MC

• Db model cells showed various aberrant phenotypes that seeme

  2020-08-24

  

  Db model cells showed various aberrant phenotypes that seemed to reflect the pathological abnormalities found under diabetic conditions. First, in Db model cells after insulin stimulation, we found the inhibition of the transcriptional repression of the gluconeogenic genes, PCK1 and G6PC, and aberra

• Although the formation and toxicity of DPC is

  2020-08-24

  

  Although the formation and toxicity of DPC is theoretically acceptable, it is difficult to evaluate the specific role of DPC and its repair enzyme MGMT in the cytotoxic and mutagenic effects because DPCs are estimated to constitute only 1%–3% of total DNA damage when membrane transport are exposed

• Various domains of DDR have been shown

  2020-08-24

  

  Various domains of DDR1 have been shown to be important for receptor clustering and its oligomeric status. It is now understood that (i) dimerization [7] and higher-order oligomerization [12], [18] of the DDR1 extracellular domain (ECD) enhance its binding to collagen; (ii) DDR1 exists as non-covale

15906 records 787/1061 page Previous Next First page 上5页 786787788789790 下5页 Last page