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Capsaicin A prominent example of such enzyme is the proteaso
2021-01-06

A prominent example of such enzyme is the proteasome, a highly promising target not only in cancer, but also in inflammatory and autoimmune diseases. Circulating proteasomes and respective anti-proteasome autoantibodies were detected in serum samples from patients with autoimmune diseases such as m
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A novel series of DHODH inhibitors was developed
2021-01-06

A novel series of DHODH inhibitors was developed by us based on a lead that was discovered during a docking procedure and medicinal chemistry exploration. The activity of the initial lead was improved by a QSAR method and yielded low nanomolar inhibitors. Introduction The most common metabolic h
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In vitro work by us
2021-01-06

In vitro work by us and others revealed that high affinity interaction with collagen requires dimerization and/or pre-oligomerization of DDR1 (Agarwal et al., 2007, Abdulhussein et al., 2008, Leitinger, 2003). It has also been reported that a significant percentage of the DDR1 population forms ligan
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Instead of receptor interaction or GT activity we focused on
2021-01-06

Instead of receptor interaction or GT activity, we focused on the CPD and autoprocessing. The CPDs from the 2 toxins are highly homologous: each cysteine protease targets an intramolecular substrate and mediates InsP6-induced autoprocessing to release the GTD into host cytosol.40, 41 However, TcdB i
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br Materials and methods br Results Metabolic stability of c
2021-01-06

Materials and methods Results Metabolic stability of compounds was studied by incubation with pooled human liver microsomes. Piperine was the metabolically most stable compound, with a t1/2 of 141min (Fig. 2, and Table 1). SCT-29 and LAU 397 showed t1/2 of approx. 45min, whereas a t1/2 of only
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The selective estrogen receptor modulators SERMs are another
2021-01-05

The selective estrogen receptor modulators (SERMs) are another type of estrogen receptor ligands. The main difference between SERMs and xenoestrogens relies on the fact that SERMs present functional duality and are able to act both as agonists and antagonists of the estrogen receptors in different t
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DMSO River sand was graded in accordance with ASTM C
2021-01-05

River sand was graded in accordance with ASTM C778 [47] (see Table 2). The graded sand had a water DMSO of 1.00%, fineness modulus of 3.49 and specific gravity of 2350kg/m3. A polycarboxylate based superplasticizer called ZP with pH of 7±1 and specific gravity of 1.1±0.02 was also used to adjust t
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S/GSK1349572 Altered brain insulin signaling and CNS
2021-01-05

Altered S/GSK1349572 insulin signaling and CNS hypometabolism are also associated with pathogenesis of neurodegeneration. Insulin receptors are mostly located in the cerebral cortex, hippocampus, cerebellum, hypothalamus and olfactory bulb, possess an effective role in the regulation of central glu
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The key difference between the membrane zymography
2021-01-05

The key difference between the membrane zymography and classical measurements of enzyme activities in soil slurries is the enzyme-substrate accessibility. Classical enzyme assays maximize access of substrate to all potentially reactive enzyme sites by ensuring sample destruction and detachment follo
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Enzyme mimics belong to a
2021-01-05

Enzyme mimics belong to a type of rising catalysts which show the similar function with their corresponding natural enzymes [20], [21], [22], [23], [24], [25], [26], [27], although their structures are different from natural enzymes. In the area of prodrug activation, the widely-used enzyme mimics a
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br Abbreviations br Introduction br Collagen induced DDR act
2021-01-05

Abbreviations Introduction Collagen-induced DDR activation A key feature of DDRs is their ability to bind both fibrillar and non-fibrillar collagens (Shrivastava et al., 1997, Vogel et al., 1997). DDR1 and DDR2 recognize the GVMGVO (O, hydroxyproline) motif within fibrillar collagens I–III
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br Results br Discussion The origin and fate
2021-01-05

Results Discussion The origin and fate of Tfh cells has been intensely studied since their first description 14 years ago (Breitfeld et al., 2000, Schaerli et al., 2000). Although mice engineered to report BCL6 (Kitano et al., 2011, Liu et al., 2012) and interleukin-21 (IL-21) (Lüthje et al.,
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Epiandrosterone sale According to these results the power Ga
2021-01-05

According to these results, the power GaN seems more robust than existing technologies (VDMOS, Superjunction, IGBT,) [5,10] and [11]. Comparing with the SiC technology, the previous works show a low SEE tolerance [[12], [13], [14]] and [15]. The SOA of power GaN devices can be equivalent to the IGBT
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The assessment process is even more difficult
2021-01-05

The assessment process is even more difficult when Commercial-Off-The-Shelf (COTS) components – whose internals are partially or totally unknown – come into play. COTS are being increasingly used by the industry to reduce costs and to shorten development (and possibly deployment) time. However, sinc
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The reference standards methyl difluoro dioxolo benzo imidaz
2021-01-05

The reference standards methyl 3-((2,2-difluoro-5-[1,3]dioxolo[4′,5′:4,5]benzo[1,2-]imidazol-6-yl)carbamoyl)benzoate () and -(2,2-difluoro-5-[1,3]dioxolo[4′,5′:4,5]benzo[1,2-]imidazol-6-yl)-3-methoxybenzamide (), and their corresponding desmethylated precursors 3-((2,2-difluoro-5-[1,3]dioxolo[4′,5′:
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