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PI-3065 synthesis br Secretase modulators a loss of pharmaco
2022-07-04
γ-Secretase modulators: a loss of pharmacology? A lack of translation from in vitro to in vivo pharmacology is an unresolved issue among most GSMs. R-flurbiprofen was tested in clinical trials, however, it did not achieve statistical significance on either of its primary endpoints – cognition or
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br The bile acid farnesoid X
2022-07-04
The “bile acid” farnesoid X receptor (FXR) The Farnesoid X Receptor (FXR) is a ligand-activated nuclear receptor belonging to the Nuclear Receptor superfamily of transcription factors exploiting various crucial functions in mammalian physiology, including reproduction, development and metabolism
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Glucose induced nuclear translocation of several enzymes inc
2022-07-02
Glucose-induced nuclear translocation of several enzymes, including GK, glyceraldehyde-3-phosphate dehydrogenase (GAPDH), muscle GS, aldolase, lactate dehydrogenase (LDH) and phosphoglycerate kinase (PGK) is a well-known phenomenon. Additional functions have been proposed for these enzymes in the nu
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br Experimental br Acknowledgments br Human immunodeficiency
2022-07-02
Experimental Acknowledgments Human immunodeficiency virus-1 (HIV-1) is the causative agent of acquired immunodeficiency syndrome (AIDS), and without treatment results in a debilitating disease that cripples the immune system of the patient, increasing susceptibility to opportunistic diseases
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The finding that a peptide consisting of d amino acids
2022-07-02
The finding that a peptide consisting of d-amino acids binds to LSD1-CoREST1 with equal affinity as the l-amino SBI-0206965 receptor ligand indicates that the assays detect a generally non-specific association between two highly charged molecules. Nonetheless, p53-CTD is an effective inhibitor of LS
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Recently the toxicity of TBT was demonstrated at the vascula
2022-07-02
Recently, the toxicity of TBT was demonstrated at the vascular level in animal models (Nath, 2008), and the results obtained so far suggest that TBT may be a potential risk factor for cardiovascular diseases. TBT is capable to alter the coronary vascular reactivity to estradiol (dos Santos et al., 2
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In our study we found that
2022-07-01
In our study, we found that HER2-mutant lung cancers occurred commonly in female patients with an advanced stage at time of diagnosis and in a relatively younger age group. Previously, Mazières et al. [8] obtained comparable epidemiological findings, including a median age of 60 years, a high propor
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br Introduction Chronic hepatitis C CHC
2022-07-01
Introduction Chronic hepatitis C (CHC) caused by hepatitis C virus (HCV) infection affects approximately 170 million individuals worldwide [1]. HCV and human immunodeficiency virus (HIV) have similar routes of transmission, including blood-to-blood contact, sharing of injection equipment, and sex
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The majority of HCV unaware individuals
2022-07-01
The majority of HCV-unaware individuals, for which HCV RNA was obtainable, had active HCV infection and overall almost one-fifth of them had advanced liver disease according to the FIB-4 score; these persons can be classified as having a late HCV diagnosis and are in immediate need of HCV treatment
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Several compounds have been described
2022-07-01
Several compounds have been described in the literature as inhibitors of the sGC. Among them, methylene blue and LY83583 () are not direct sGC inhibitors, but rather block cGMP formation by generating superoxide anion radicals that deactivate NO. Despite their extensive use in plethora of research s
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GPR has been implicated in neuropathic and inflammatory pain
2022-07-01
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 Next we explored the SAR
2022-07-01
Next, we explored the SAR around the aryl ring attached to the pyrrole nitrogen in the presence of the 3-CF and the 2,6-difluorophenylpropionic GS-9620 synthesis sidechain (). The EC value of the unsubstituted phenyl was about 100 nM. The 4-methyl was 2-fold more potent, however ethyl and bromo d
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For a long time the mechanism for the
2022-07-01
For a long time, the mechanism for the TG-lowering effect of nicotinic RG2833 has been thought that the lowered NEFA substrate from adipose tissue limits TG production from the liver (so-called NEFA hypothesis) [[1], [2], [3], [4]]. However, recent emerging evidences have suggested the involvement
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br Functional organization of postsynaptic glutamate recepto
2022-07-01
Functional organization of postsynaptic glutamate receptors Downstream effects of glutamate receptor positioning Mechanisms underlying the subsynaptic positioning of glutamate receptors Conclusions and future prospects The molecular organization of synapses is undoubtedly a critical dete
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Cytarabine br Materials and methods br
2022-07-01
Materials and methods Results Discussion Quercetin is a relatively abundant bioactive flavonoid with a wide variety of documented physiological effects, which has gained popularity as a nutritional supplement [40]. There is increasing interest in quercetin's anticancer properties (for recen
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