• Another milestone in the field is the de

  2021-04-22

  

  Another milestone in the field is the de novo discovery of EPAC2 and EPAC1 specific inhibitors through fluorescence-based HTS assays. Due to the excellent EPAC/PKA selectivity of TKI258 , it has been widely applied as a useful chemical probe to discriminate EPAC related signaling pathways and biolo

• br Mechanisms of acquired resistance to st and

  2021-04-21

  

  Mechanisms of acquired resistance to 1st and 2nd generation EGFR inhibitors After treatment with first or second generation EGFR TKIs, virtually all patients after approximately 12 months develop acquired resistance (AR). Different mechanisms of AR to EGFR TKIs have been reported to date and may

• ATP dependent DNA ligases in vertebrates

  2021-04-21

  

  ATP-dependent DNA ligases in vertebrates are divided in three families [7]. Family I DNA ligases are responsible for sealing the nicks during DNA replication and in long-patch base excision repair (BER). Family III DNA ligases are involved in short-patch BER. Lastly, family IV DNA ligases are involv

• Arsenic could cause apoptosis in both benign and

  2021-04-21

  

  Arsenic could cause apoptosis in both benign and malignant cells (Akao et al., 2000, Gupta et al., 2003, Namgung and Xia, 2001). However, at present, little is known about the consequences of arsenic-treated urothelial cells in autophagy and expression of its related proteins. In addition, the alter

• Conoidin A We report here that DAPK

  2021-04-21

  

  We report here that DAPK signaling pathways play significant roles in OGD-induced neuronal death. Exposure of the Conoidin A to OGD led to DAPK activation, which then promoted cell death through BimEL overexpression. Furthermore, DAPK-induced BimEL overexpression was mediated by inactivating ERK1/2

• A surprising second functional effect was found in culture e

  2021-04-21

  

  A surprising second functional effect was found in culture experiments. Inclusion of LTD4 reduced the frequency of Fas receptor (CD95) expression. Once again, this effect, although modest, was reversed by a cysLT1 receptor antagonist. The biologic significance of this effect or its mechanism remaine

• A series of monocarboxylated chalcones e g

  2021-04-21

  

  A series of monocarboxylated chalcones (e.g. compounds 7 and 8, Fig. 2A) was previously identified as good CysLT1 antagonists [20], and none of them exhibited CysLT2 antagonistic activities (Supplementary Table S1). This study was consistent with reported result that CysLT2 LY3039478 was not sensit

• Next we evaluated the therapeutic potential of compound

  2021-04-21

  

  Next, we evaluated the therapeutic potential of compound () using the mouse model of collagen-induced arthritis (CIA model), which is the pathological model for RA. Consequently, oral once-daily dosing of 3 mg/kg reduced the overall progression of the clinical score, including inflammation and bone

• br Materials and methods br Results br Discussion

  2021-04-21

  

  Materials and methods Results Discussion We confirmed the published cDNA and protein sequence of feline CSF-1R and stably cloned the cat receptor into the Ba/F3 cell line. Activation of feline CSF-1R by recombinant human CSF-1 was previously tested by Woolford et al. [14]. Expression of onc

• br Acknowledgments Denise Fernandes acknowledges a

  2021-04-21

  

  Acknowledgments Denise Fernandes acknowledges a postdoc fellowship (SFRH/BPD/34289/2006) from the Portuguese Fundação para a Ciência e Tecnologia (FCT) of the Ministry of Science and Technology of Portugal. This work was supported by the Spanish National Plan for Research (Project Ref. CGL2011-24

• br Diverse functions of ERK pathway Same as the other

  2021-04-20

  

  Diverse functions of ERK pathway Same as the other MAPK cascades, the ERK pathway is activated by several extracellular stimuli and different internal routes. ERK vitally tunes the function of various substrates in all cellular components; the nucleus, cytoplasm, membranes and the cytoskeleton. E

• br Introduction Prostaglandins are important local mediators

  2021-04-20

  

  Introduction Prostaglandins are important local mediators in a host of reproductive processes including ovulation, fertilization, embryonic development, luteal regression, and parturition (Ushikubi et al., 2000). Prostaglandin E2 (PGE2) is among the more versatile prostanoids, and its effects app

• To study systemic potential of the selected compounds as

  2021-04-20

  

  To study systemic potential of the selected compounds as EP1 receptor antagonist, they were evaluated with regard to the sulprostane-induced increase of intravesical bladder pressure in rats. Some of the analogs, 13 and 15–17, which were selected on the basis of their in vitro EP1 receptor affinity,

• As a co factor CIITA

  2021-04-20

  

  As a co-factor, CIITA lacks the ability to recognize and directly bind to specific DNA elements to regulate transcription; instead, it relies on interaction with sequence-specific transcription factors (TFs) to be recruited to the chromatin. Therefore, the observation that CIITA binds to a specific

• br Methods br Results br Discussion Here we have shown

  2021-04-20

  

  Methods Results Discussion Here we have shown that two GPCR subtypes thought to trigger similar signalling events by coupling to Gαq in fact regulate different signalling networks via coupling to distinct G proteins. Thus global effects regulated by both receptors in events such as cardiac

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