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In contrast to sGC stimulators sGC activators promote enzyma
2021-11-30
In contrast to sGC stimulators, sGC activators promote enzymatic activity of sGC containing oxidized heme iron (Fe3+) or missing the heme group. A-350619 is one of the oldest activators of sGC to be discovered. A-350619 increased sGC activation in a non-additive manner with respect to YC-1, leading
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Introduction Epigenetic alterations play an
2021-11-30
Introduction Epigenetic alterations play an important role in carcinogenesis. Aberrant promoter CpG island hypermethylation causes transcriptional gene silencing [1], and has been documented for a number of genes in prostate cancer (PCA) [2]. Histone modifications are also important regulators of t
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FR 180204 mg GPR has been implicated in
2021-11-30
GPR55 has been implicated in neuropathic and inflammatory pain (Staton et al., 2008) and bone remodeling (Whyte et al., 2009). Thus delineating the pharmacology of this receptor and the discovery of selective agonists and antagonists merits further study and could lead to new therapeutics. Acknow
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br Introduction The amino acid
2021-11-29
Introduction The amino Doripenem receptor glycine functions as a neurotransmitter in the vertebrate central nervous system: as an inhibitory neurotransmitter and as a co-agonist of the NMDA-subtype of excitatory glutamatergic receptors (Eulenburg et al., 2005). Under a current hypothesis that sc
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br Restart of Stalled Replication Forks By
2021-11-29
Restart of Stalled Replication Forks By preventing the replisome from unwinding duplex DNA, ICLs stall progression of the replication fork, which in turn results in genomic instability 41., 42.. As in prokaryotes, the conventional mechanism of ICL repair in eukaryotes involves the combined activi
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The GlyR is pentameric with each subunit consisting of an
2021-11-29
The GlyR is pentameric, with each subunit consisting of an extracellular ligand binding domain (LBD), four transmembrane (TM) segments, and a large intracellular loop between TM3 and TM4. Binding of neurotransmitter produces conformational changes that are rapidly transmitted to the membrane-spannin
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C steroids and their glycosylation products distribute widel
2021-11-29
C21 steroids and their glycosylation products distribute widely in Asclepiadaceae plants. Their anticancer activities have been shown in different human cell lines and in vivo animal experiments [[27], [28], [29], [30], [31], [32]]. However, the mechanisms of their anticancer activities are still un
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Our initial lead optimization started with the modification
2021-11-29
Our initial lead optimization started with the modification of the indole head group as summarized in . Extensive exploration indicated that there was limited tolerance of structural change in this region of the molecule. All of the modifications to the indole moiety, including N-substitution (), li
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Two intermediate compounds A and B in
2021-11-29
Two intermediate compounds (A and B in Fig. 1) were tested for both Aβ40 and CYP3A4 inhibition activity. Potential hydrolysis of structures I and IIin vivo may produce A which is a strong CYP3A4 inhibitor. Cyclopropanol group is a suspected liability, because Tubacin australia B without it has a cl
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Reports described a range of synthetic GPR agonists
2021-11-29
Reports described a range of synthetic GPR40 agonists with desirable safety and efficacy profiles, compared with existing antidiabetic therapies such as insulin and sulfonylureas [[20], [21], [22], [23], [24], [25], [26], [27], [28]]. Among them, several small molecules were tested in the clinical t
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Our results are consistent with the
2021-11-29
Our results are consistent with the hypothesis that reduced Fas-mediated apoptosis in maternally activated T-lymphocytes could result in insufficient trophoblast invasion of the spiral ion channels as the activated T-lymphocytes become able to enhance the destruction of the cytotrophoblasts. A redu
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In our cohort each patient had
2021-11-29
In our cohort, each patient had a median of 2 Anti-FXa measurements performed daily and a median of 1 infusion rate change daily to maintain therapeutic unfractionated heparin levels. Previously, several studies have documented that APTT-based protocols lead to more fluctuations in comparison with A
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Hexa His tag While considering the molecular pathogenesis of
2021-11-29
While considering the molecular pathogenesis of an MPNST, the Ras/Raf/MEK/ERK, mTOR/AKT, p53, and PTEN pathways associated with tumor growth have been described (McCubrey et al., 2012). The involvement of receptor tyrosine kinases such as EGFR and TAM receptor families, and its associated molecular
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br Conflict of interest br Introduction Endometriosis is
2021-11-29
Conflict of interest Introduction Endometriosis is defined as the presence of endometrial glands and stroma outside the uterus, most often in the pelvic peritoneum and ovaries. This disorder affects an estimated 10% of women in the reproductive age group and is basically an estrogen-dependent
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br Competing interests br Funding br
2021-11-29
Competing interests Funding Ethical approval Acknowledgement Introduction Hepatitis C is a disease that infects the liver through transmission of the hepatitis C virus (HCV). Because the symptoms of this infection are not pronounced, the infected individuals may not even be aware of t
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