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Finally worth of mention are few papers that
2021-09-11
Finally, worth of mention are few papers that report on the discovery of HO-2 selective inhibitors. In 2013, starting from the screening of a Safingol australia library, the above-mentioned Canadian research group identified Clemizole (Table 6) as a new hit compound for the development of the first
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br Mechanisms of HDAC inhibition dependent cardioprotection
2021-09-11
Mechanisms of HDAC inhibition-dependent cardioprotection Multiple preclinical studies have demonstrated potent cardioprotective benefits of HDAC inhibition in murine models of myocardial stress, including I/R [19,25,29,30]. TSA reduces myocardial infarct size by up to 50% [19,25]. In addition, tr
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It has been proposed that HCA may be
2021-09-11
It has been proposed that HCA1 may be a better target than HCA2 to treat dyslipidemia and to prevent progression of atherosclerosis, because HCA1 is less widely expressed, and HCA1 activation does not result in flushing. However, since the antilipolytic effects mediated by HCA2 appear to be not the
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The dramatic increase in the development of EAAT inhibitors
2021-09-11
The dramatic increase in the development of EAAT inhibitors and substrates over the last several years can likely be attributed to a number of experimental advances. Firstly, the isolation of the individual EAAT clones allowed each subtype to be selectively examined in well-characterized expression
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As a part of our continuing efforts
2021-09-11
As a part of our continuing efforts towards discovery of new class of compounds against different therapeutic areas and based on the literature reports, we designed a dual pharmacophore which possess a long aliphatic chain of free fatty acids and a phenyl propanoid part of known GPR40 agonists. Here
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Since stroke and cerebrovascular diseases were considered se
2021-09-11
Since stroke and cerebrovascular diseases were considered serious AEs following vaccination, we performed manual chart review to confirm the diagnosis and symptom onset date for all stroke and cerebrovascular disease cases identified by ICD-9 codes. Chart review of 131 presumptive cases confirmed 82
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For further understanding of the interaction between these
2021-09-11
For further understanding of the interaction between these inhibitors and proteins (BRafV600E and HDAC1) for guiding the SAR, compound 10e, the most potent compound of this series, was chosen as a representative for docking into the BRafV600E (PDB code: 1UWJ) and HDAC1 (PDB code: 1C3R), revealing ex
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Interestingly the virulence of HBV may adaptively
2021-09-11
Interestingly, the virulence of HBV may adaptively evolve, thus affecting the macroscopic propagation of hepatitis B. Higher virulence in vivo may result in a higher transmission rate and mortality. By assuming that the transmission rate is a monotonically increasing function of virulence, , we prop
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On the basis of the foregoing set of considerations
2021-09-11
On the basis of the foregoing set of considerations, L1 could exert three possible actions on sGC determining its deactivation, schematically depicted in Fig. 6: i) oxidation of Fe2+ to Fe3+; ii) coordination to sGC, conjecturably, via the pyridyl nitrogen of the canthin-6-one; iii) coordinating and
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br Conflict of interest statements
2021-09-11
Conflict of interest statements Acknowledgements Introduction Oral squamous cell carcinoma (OSCC) is the sixth most common cancer worldwide and is the major cause for cancer morbidity and mortality in developing countries. Age standardized incidence rate in India is 12.6 per 100 000 populat
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Previous studies showed that pregnancy
2021-09-11
Previous studies showed that pregnancy rate improves when ewes have a BCS that exceeds a minimum threshold [43]. The pregnancy rate is increased in sheep with BCS ≥2.5 [44] and >2 [45]. In this work, pregnancy rate was higher in the GnRH group with low BCS compared to the hCG and Control groups. Des
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br Treatment KD is currently the
2021-09-11
Treatment KD is currently the treatment of choice for GLUT1-DS. It is a high-fat, carbohydrate-restricted diet that mimics the metabolic state of fasting; so, the KD relies an exogenous rather than body fat for ketone production, thus maintaining ketosis without weight loss. As the developing br
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Ionotropic glutamate receptors GluRs are ligand gated ion
2021-09-11
Ionotropic glutamate receptors (GluRs) are ligand-gated ion channels that mediate information processing at the majority of excitatory synapses in the brain and participate in such physiological processes as learning and memory, development and maintenance of cellular connections, and pain perceptio
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Cy5.5 hydrazide Seizures in turn selectively modulate the ex
2021-09-11
Seizures, in turn, selectively modulate the Cy5.5 hydrazide of GalR in the hippocampus. Thus, pilocarpine-induced SE led to a 30% downregulation of GalR2 without affecting GalR1 (personal communication with T. Bartfai, Scripps Research Institute). Therefore, despite the fact that GalR2 could have b
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br Conclusions In this study
2021-09-10
Conclusions In this study, we discovered that the G-quadruplex (Q1) formed by S1 sequence in the upstream region of the transcription start site of c-Myb gene functioned as a positive transcriptional regulator, which was different from the most cases that G-rich sequences functioned to impair the
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