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Previous research has suggested that the acetylcholine
2021-06-17

Previous research has suggested that the acetylcholine-gated chloride channels (ACCs) in Caenorhabditis elegans (Putrenko et al., 2005) exhibit the characteristics of promising drug targets. The genes that encode the various subunits of this family are present across the nematode phylum and appear t
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To develop antagonists selective for the
2021-06-17

To develop antagonists selective for the mouse EP1 receptor, we started with compound (), synthesized as previously described (). Diethyl dipicolinic Nicotine Difartrate () was reduced with NaBH to . Parikh–Doering oxidation of with sulfur trioxide–pyridine complex and DMSO produced the unstable
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Ultrasound is an acoustic wave with
2021-06-17

Ultrasound is an acoustic wave with a frequency >20 kHz that needs a medium to propagate [20]. Accompanied by the spread of an ultrasonic wave, a series of alternating cycles of compression and rarefaction emerge in the liquid medium. During the rarefaction cycle, microbubbles are formed because of
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The discoidin domain receptors DDR and DDR are
2021-06-17

The discoidin domain receptors, DDR1 and DDR2, are receptor tyrosine kinases (RTKs) that are stimulated by collagen in the extracellular matrix (ECM). Unlike most other RTKs, they form ligand-independent stable dimers that are non-covalently linked. This ECM activation induces receptor phosphorylati
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br A brief introduction to DUBs The reversal
2021-06-16

A brief introduction to DUBs The reversal of ubiquitin conjugation of targeted proteins relies on deubiquitinating gaba b receptor (DUBs), which catalytically cleave single Ub or poly-ubiquitin chains from proteins. The human genome encodes approximately 100 potential DUBs which can be classifie
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The aniline R group was extensively
2021-06-16

The aniline R2 group was extensively explored and a large variety of substitution was tolerated at several positions on the aryl ring (). Notably, substitution at the 3-position often gave increased potency. Increasing lipophilic bulk at this position gave increasing potency within an ether series (
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Two key enzymes play important
2021-06-16

Two key enzymes play important roles in the bioconversion of xylitol from d-arabitol, namely d-arabitol dehydrogenase (ArDH) and NADH-dependent xylitol dehydrogenase (XDH), respectively (Qi et al., 2014). In an earlier study, we developed a high xylitol yield strain by expressing xdh in E. coli BL21
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There exists a glucose residue in the
2021-06-16

There exists a glucose residue in the structure of 5. Acid hydrolysis (Supplementary data) followed by TLC comparison with the reference compound as well as GC–MS analysis (l-cysteine methyl ester hydrochloride derivative: tR=22.22min for glucose residue of 5 and 22.46min for the reference compound)
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br Material and methods br Results br
2021-06-16

Material and methods Results Discussion In the present study, twenty strains of Y. enterocolitica were analyzed for their inhibitory potential on cysteine proteases. Five of these strains belonged to bioserotype 4/O:3, which is distinguished for its pathogenicity towards humans. The rest of
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In a study on the time
2021-06-16

In a study on the time course of a mechanism-based inactivation of CYP3A by HIV protease inhibitors, Katzenmaier et al. [37] reported that the suppression of CYP3A activity continued for threedays after the discontinuation of ritonavir. In the present study, the CYP3A activity on day 28 after a seve
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Introduction Cytochrome P CYP A is the most important enzyme
2021-06-16

Introduction Cytochrome P450 (CYP)3A is the most important enzyme involved in the metabolism of 30–40% of currently prescribed drugs [1]. The KW-6002 receptor level and activity of CYP3A show large intra- and inter-individual variability, which contributes to unpredictable drug response and toxici
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Investigations of mice lacking up to three CDKs identified t
2021-06-16

Investigations of mice lacking up to three CDKs identified the mitosis-regulating kinase CDK1 as the main essential component for the cell cycle, whereas ablation of other trilithium regulators such as CDK2, CDK4, or CDK6 did not result in defective proliferation 12, 13. Mouse models and specific CD
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Palliative surgeries for refractory epilepsy
2021-06-16

Palliative surgeries for refractory epilepsy include vagus nerve stimulation and corpus callosotomy. Among 220 individuals with CDD with parent-entered data, 17% had a vagus nerve stimulation implanted and 69% of parents reported reduced seizure frequency. These data are consistent with a case repor
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Nitazoxanide receptor br Discussion In depression an activat
2021-06-16

Discussion In depression, an activation of the inflammation process and production of cytokines (including chemotactic cytokines – chemokines) and their receptors may occur due to the stimulation of the immune system. One of the earliest studied and described cytokines in depression is interleuki
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Apart from its high affinity the selection of GW as
2021-06-16

Apart from its high affinity, the selection of GW2580 as Fmoc-Cl mg lead in our radiotracer development program was motivated by its exceptional selectivity. The observed profound impact of small structural modifications on the selected panel of four kinases tested prompted us to conduct comprehensi
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