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Furan analogs and N methylpyrrole analogs had completely dif
2021-01-27
Furan analogs and N-methylpyrrole analogs had completely different SARs. For example, replacement of the furan-2-sulfonyl moiety of 6 with the furan-3-sulfonyl moiety resulted in 8 with a decreased EP1 LRRK2-IN-1 affinity and an increased antagonist activity, while the corresponding chemical modifi
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br Materials and methods br Results br Discussion Schistosom
2021-01-27
Materials and methods Results Discussion Schistosome cercarial elastase secreted from the acetabular glands of cercariae is recognized to play a critical role in mammalian host skin penetration upon infection. The present study extends the understanding of biochemical and immunological prop
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Modulating protein stability specifically inhibiting ubiquit
2021-01-27
Modulating protein stability, specifically inhibiting ubiquitin E3 ligases, provides potential advantages over other druggable targets given the presence of biochemically multiple, unique pharmacophores within complexes that can bind a variety of small molecules [12]. The FBXO3 inhibitors used here
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Like compound substitution on compound contains
2021-01-27
Like compound substitution on compound () contains amino and carboxamide groups attached to adjacent ring positions. These groups have similar interactions as compound with the protein backbone and Glu114. The triazole core is coordinated with Lys291. The triazole ring core π-stacks with Tyr226.
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While these previous correlative studies
2021-01-27
While these previous correlative studies have measured tDDR1 protein by IHC, these studies have not considered that pDDR1 could also be an important marker of cancer prognosis. A phosphoproteomic survey of lung cancer tissues did identify pDDR1 as one of the most commonly phosphorylated receptor kin
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br Pre clinical combination studies using
2021-01-27
Pre-clinical combination studies using CSF-1/CSF-1R inhibitors In preclinical models, the CSF-1R pathway can be blocked by using either small molecule kinase inhibitors (GW2580 [30], PLX3397 [31], Ki20227 [32], BLZ945 [33] and CYC11645 [34]), antibody-mediated inhibition of CSF-1 using 5A1 [35] o
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The CYP D inferred metabolizer phenotype describes
2021-01-27
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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COMT expression protein level and activity are down regulate
2021-01-27
COMT expression, protein level and activity are down regulated by E2. Using estrogen receptor (ER) positive MCF-7 cells, Xie et al. demonstrated an E2 dose dependent (1, 10 and 100 nM) decrease in S-COMT 1.3 kb mRNA that was maximum after 48 h (Xie et al., 1999). A similar decrease was not observed
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Our study demonstrates that the
2021-01-27
Our study demonstrates that the duration of storage under the conditions analysed did not have a major effect on the recovery efficiency for any of the swabs (Fig. 1). However, up to 4-fold differences in the recovery efficiencies were observed between the different swabs tested (Fig. 2). Using the
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HA activates its receptor channels to cause an inward
2021-01-27
HA activates its receptor channels to cause an inward chloride flux in the insect nervous system (Hardie, 1989). Two genes encoding the subunits of these channels were first identified in D. melanogaster: one previously known as ort (also differently named as hclA, DM-HisCl-α1, hisCl2 and Dm HA-Cl I
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Polymorphism of the CD gene also
2021-01-26
Polymorphism of the CD226 gene also affected the progression rate without any significant effect on autoantibody formation. This gene has been reported to be a common genetic factor in multiple autoimmune diseases such as SLE, systemic sclerosis and type 1 diabetes [43]. CD226 is an immunoglobulin s
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br Introduction O Methylguanine DNA methyltransferase MGMT
2021-01-26
Introduction O6-Methylguanine-DNA methyltransferase (MGMT) is a DNA-repair enzyme that specifically transfers alkyl adducts from the O6 position of guanine to the cysteine residue (Cys145) in its active site. In cancer cells, this ability of MGMT disrupts the cytotoxic actions of alkylating antic
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C PHNO has been described
2021-01-26
[11C]-(+)-PHNO has been described as a full agonist at both D2 and D3 receptors [54,55]. [11C]-(+)-PHNO was initially developed as a PET radiotracer for imaging the high affinity state of the D2 receptor (i.e., highD2) as a means of measuring synaptic dopamine changes in response to pharmacologic ch
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br Conclusion Our objective is to
2021-01-26
Conclusion Our objective is to promote cell activity on biomaterials, especially for use in regenerative medicine, by grafting THPs containing collagen-binding sites onto inert substrates. We have previously reported a methodology to derivatize EDC/NHS crosslinked films with photoreactive THPs. T
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It was recently reported that a functional single nucleotide
2021-01-26
It was recently reported that a functional single nucleotide polymorphism (rs75932628) within Triggering receptor expressed on myeloid 2-Methoxyestradiol australia 2 (TREM2) is associated with AD (Guerreiro et al., 2013). Homozygous loss of function mutations in TREM2 are also associated with an au
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