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br Next we explored the SAR around the
2021-11-24
Next, we explored the SAR around the aryl ring attached to the pyrrole nitrogen in the presence of the 3-CF and the 2,6-difluorophenylpropionic selinexor sidechain (). The EC value of the unsubstituted phenyl was about 100 nM. The 4-methyl was 2-fold more potent, however ethyl and bromo did n
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RVX-208 Fig summarizes the underlying mechanism of SB on inh
2021-11-24
Fig. 7 summarizes the underlying mechanism of SB on inhibiting inflammation and maintaining epithelium barrier integrity in the TNBS-induced colitis model. Our findings not only explained the protective effect of SB on colon health, but also provided evidence that GPR109A likely constitutes a valid
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NEIL interacts with many DNA replication proteins
2021-11-24
NEIL1 interacts with many DNA replication proteins including flap-endonuclease 1 (FEN-1), proliferating cell nuclear antigen (PCNA), and Werner RecQ helicase (WRN) through its disordered C-terminal part. One study showed that in in vitro condition, NEIL1 binds to the damaged Ro 48-8071 in an RPA-co
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The unique mechanism of EAAT anion channel gating
2021-11-24
The unique mechanism of EAAT anion channel gating results in neuronal or glial anion conductances that follow changes in substrate concentrations and thus allow feedback control of glutamate release (Wersinger et al., 2006) or modification of GABAergic postsynaptic currents by glutamatergic signals
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br Materials and methods br Results br
2021-11-24
Materials and methods Results Discussion In this study, we discover that Sufu stabilizes Gli1 protein levels by antagonizing Numb/Itch-mediated protein degradation. Together with previous work that demonstrates control of Gli2/3 protein levels by Sufu (Chen et al., 2009, Jia et al., 2009, W
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Gap junction intercellular communication GJIC facilitates th
2021-11-24
Gap junction intercellular communication (GJIC) facilitates the exchange of ions, metabolites, Ca2+, inositol phosphates, and/or cyclic nucleotides of up to 1.8 kD in size between 8-Hydroxy-DPAT hydrobromide through contact-dependent mechanisms [3,4]. Oocyte growth and development (as depicted in F
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Hypertriglyceridemia is associated with an overproduction an
2021-11-24
Hypertriglyceridemia is associated with an overproduction and secretion of triglyceride-rich lipoproteins (TRLs), due to increased liver lipid substrate availability (Adiels et al., 2005, Choi and Ginsberg, 2011), and/or reduced catabolism of TRLs and their remnants, due to reduced lipoprotein lipas
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A way to identify what subunit interfaces contribute
2021-11-24
A way to identify what subunit interfaces contribute to the pharmacology of agents is to utilise binary GABAARs as tool receptors to ascertain possible binding sites for particular ligands. These receptors can help identify subunits and subunit interfaces that contribute to receptor pharmacology. In
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In recent years it was discovered in animals
2021-11-24
In recent years, it was discovered in animals that certain types of non-apoptotic cell death are strictly dependent on iron and ROS. The term ‘ferroptosis’, derived from the Greek word ‘ptosis’ (falling) and the Latin word ‘ferrum’ (iron), is coined to describe such cell death phenomena. Cytoplasmic
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Here we employ a genetic approach to examine the potential
2021-11-24
Here we employ a genetic approach to examine the potential interaction of Gli3 and Ezh2 with respect to anteroposterior limb bud polarity. Loss of Ezh2 in a Gli3 mutant background leads to synergistic loss of anterior identity, although the double mutant phenotype more closely resembles that of Ezh2
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Introduction Breast cancer is the most common
2021-11-24
Introduction Breast cancer is the most common cancer among women worldwide, representing 30% of new cancer diagnoses. In addition, it is the second leading cause of cancer deaths among women [1]. With regard to the risk of breast cancer, proper diagnosis and stratification of tumors for individuali
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The Hedgehog signaling pathway HH
2021-11-24
The Hedgehog signaling pathway (HH pathway hereafter) is vital for development and tissue homeostasis. [4] In recent years, studying the role of the HH pathway in carcinogenesis and cancer stemness has highlighted the HH inhibitors as putative cancer therapeutics [5]. However, clinical application o
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Glycogen synthase kinase GSK is an evolutionarily conserved
2021-11-23
Glycogen synthase kinase-3β (GSK-3β) is an evolutionarily conserved serine/threonine kinase that plays multifaceted role in diverse cellular and neurophysiological processes [8]. GSK-3β is regulated by inhibitory serine and stimulatory tyrosine phosphorylation on Ser9 and Tyr216 respectively [9]. Dy
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br Materials and methods br Results In this study
2021-11-23
Materials and methods Results In this study we re-examined the kinetics of ET transport and tested the ability of various suggested substrates of OCNT1 to inhibit ET uptake. Using a native ET transporter expressed in the human HeLa cell line ET was found to be taken up with a Km of 51 μM and V
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br Materials and methods br Results
2021-11-23
Materials and methods Results Discussion To the best of our knowledge, the current study presented the first evidence that GPR40, also named FFAR1, played an essential role in bone formation and mediated AZD1208 induced osteogenic effect via Wnt/β-catenin signaling. We found that dose–resp
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