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SW033291 mg We have previously designed an azobenzene
2021-12-22
We have previously designed an azobenzene-based molecule, Razo, which could switch the conformations of G-quadruplex structures by photoregulation. 12, 13, 14, 15 However, it lacks selectivity to different G-quadruplexes. Therefore, we want to find a way to modify this molecule so that it could be u
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Akt mTOR signaling pathway is a major negative
2021-12-22
Akt/mTOR signaling pathway is a major negative regulator of autophagy, via modulating ULK1 complex. It is well established that Inhibition of mTOR by deprivation of nutrients or growth factors, led to dephosphorylation of ULK1, ULK2, and Atg13 in human cells, which is a key step for ULK1 complex ass
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Syt itself does not catalyze lipid mixing and
2021-12-21
Syt1 itself does not catalyze lipid mixing and membrane fusion. Rather, the pairing of vesicular and target membrane SNAREs into complexes serves to pull bilayers together to drive fusion; Ca•syt1 accelerates these fusion reactions so that they occur on rapid timescales in a manner that is precisel
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br Introduction Over one million people are
2021-12-21
Introduction Over one million people are currently living with HIV in the United States (CDC, 2016). Through advances in HIV medications, the use of antiretroviral therapy has led to people living longer with HIV (Palella et al., 2006). In attempts to mitigate the effects of the psychological and
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Myelination by oligodendrocytes is required for saltatory ne
2021-12-21
Myelination by oligodendrocytes is required for saltatory nerve impulse conduction and proper CNS function (Bercury and Macklin, 2015). Defects in myelination and remyelination impair saltatory nerve conduction and functional connectivity leading to cognitive, behavioral, and motor deficits in neuro
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GSK has also been used as PET radiotracer
2021-12-21
GSK-189254 has also been used as PET radiotracer (in the form of [11C]-GSK-189254, also used as [11C]-AZ12807110 by Jucaite et al. (Jucaite et al., 2013)) to assess H3R occupancy (Ashworth et al., 2010), and is currently used in an image-based phase I clinical trial study for investigating GSK-23951
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br Introduction The coronary vasculature is required
2021-12-21
Introduction The coronary vasculature is required for supplying oxygenated blood to the cardiac muscle. Proper coronary blood circulation is essential for embryonic and adult cardiac tissue homeostasis. Defects associated with the coronary function leads to myocardial ischemia, infarction, and he
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The absolute requirement for substrate prephosphorylation ra
2021-12-21
The absolute requirement for substrate prephosphorylation raised the possibility that short phosphorylated peptides might serve as selective substrate competitive inhibitors. A set of phosphorylated peptides patterned after known GSK-3 substrates was generated and shown to inhibit GSK-3 in vitro in
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It was reported that GPR
2021-12-21
It was reported that GPR120 is expressed on macrophages in adipose tissue (Oh et al., 2010). Whether GPR120-positive SQ 22536 in human and rat pancreas belongs to macrophages was studied. CD68 is a transmembrane glycoprotein that is highly expressed by human monocytes and tissue macrophages (Horika
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Our last area of exploration
2021-12-21
Our last area of exploration was the piperidine core as shown in . We rationalised that the basicity of the nitrogen (measured p=7.0) may be responsible for the affinity for the hERG receptor and we therefore sought to moderate this by incorporation of electronegative groups at the 3-position. To th
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Disrupting the dialog between microbiota and
2021-12-21
Disrupting the dialog between microbiota and the host, especially at the level of mucosal immunology, is expected to have profound effects on disease development. By using the AOM+DSS model of colitis-associated CRC, Singh et al. (2014) showed that development of inflammation and CRC are exacerbated
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br Materials and methods br Results shows
2021-12-21
Materials and methods Results shows serum FSH, LH, oestradiol and progesterone values in the two cycles from day 2 to day 10. Basal values of these hormones on day 2 (before any intervention) were similar in the two cycles. Thereafter, FSH values did not differ significantly between the two c
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Based on work from our labs with mGlu NAMs
2021-12-21
Based on work from our labs with mGlu NAMs, and the ability of [3.3.0] systems, such as the octahydropyrrolo[3,4-]pyrrole, to effectively mimic piperazines, we focused our attention on the potential bioisoteric replacement of the [3.1.0] system of and , as well as the piperidine of , with a [3.3.0]
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It is important to clarify whether the decrease in USV
2021-12-21
It is important to clarify whether the decrease in USV after administration was secondary to the central depressant actions of the test compounds. Several reports have addressed the possibility that central depressant actions such as motor incoordination or changes in body temperature might affect U
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br GR Is a Transcriptional Activator
2021-12-21
GR Is a Transcriptional Activator How GR activates some genes while repressing others remains unsettled after decades of study. While significant controversy exists regarding GR-mediated repression, a consensus model for transcriptional activation has emerged: GR activates transcription through s
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