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In summary through medicinal chemistry design and computer a
2022-01-24
In summary, through medicinal chemistry design and computer-assisted conformational modeling, the initial lead was evolved into a series of dihydrobenzofuran derivatives, , as potent GPR119 agonists. Optimization of general structure at various regions of the molecule, including the substituent on d
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br Acknowledgments br Introduction Manipulating target
2022-01-21
Acknowledgments Introduction Manipulating target protein expression via either induction or suppression of gene expression is a powerful technology that has been widely used in the recent past in the field of neurobiology, both to study the pathophysiological significance of a target gene and
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MAPK are involved in a large
2022-01-21
MAPK are involved in a large variety of solid and hematolgical neoplasms and, indeed, several components of the MAPK network have already been proposed as targets in cancer therapy, such as p38, JNK, ERK1/2, MEK1/2, RAF, RAS, DUSP1 and ERK5 [11], [12]. Among them, alteration of the RAS-RAF-MEK1/2-ER
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glatiramer acetate australia br Preclinical development of G
2022-01-21
Preclinical development of GIP agonists Since the action of DPP IV is not limited to GIP, the most specific pharmacological approach for GIP would be modification at the N-terminus to disrupt DPP IV-mediated degradation. Indeed, it has been shown that GIP analogues with N-terminal modifications
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We and others have previously reported that neurons
2022-01-21
We and others have previously reported that neurons generated from iPSCs with genetic forms of AD recapitulate aspects of the disease, including increased Aβ peptide production in trisomy 21 and APP duplication neurons (Moore et al., 2015, Israel et al., 2012) and increased production of longer form
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Inhibitors against the proteasome a component of
2022-01-21
Inhibitors against the proteasome, a component of the ubiquitin-proteasome pathway that degrades cellular proteins, provide a new strategy for targeting the 26S proteasome [25]. Proteasome inhibitors can exhibit potent anti-cancer effects against different tumor Caspase-1, mouse recombinant protein
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Prion diseases are transmissible and result in
2022-01-21
Prion diseases are transmissible and result in fatal neurodegenerative disorders, which, similar to AD, also involve the infiltration and activation of mononuclear phagocytes in INCB-024360 lesions (reviewed in [61]). A 21 amino-acid fragment of the aberrant human prion protein, Prp106–126, can for
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Murine models of AML were used to
2022-01-21
Murine models of AML were used to identify differentially expressed proteins following treatment with the EZH2 inhibitor, DZnep. Sandow and coworkers demonstrated that inhibition of EZH2 induces leukemia AZ20 arrest through regulation of cyclin-dependent kinases and increased expression of p53, a c
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Acknowledgements br Introduction Histamine mediates various
2022-01-21
Acknowledgements Introduction Histamine mediates various physiological functions and pathological actions through its interactions with histamine receptors that belong to the superfamily of seven transmembrane G-protein-coupled receptors (GPCRs) (Haas et al., 2008). Four histamine receptor subty
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br Hippo Signaling in Autoimmunity An imbalance of T cell
2022-01-21
Hippo Signaling in Autoimmunity An imbalance of T cell subsets, such as immunosuppressive regulatory T jnk inhibitor (Treg) and inflammatory TH17, has a key role in autoimmune diseases. Recently, investigations found that TAZ but not YAP enhances TH17 differentiation but attenuates Treg different
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ap-1 br HO and cerebral malaria In a
2022-01-21
HO-1 and cerebral malaria In a post-mortem evaluation of human cerebral (falciparum) malaria, strong HO-1 immunostaining was consistently noted in microglia/macrophages within and surrounding the pathognomonic Durck’s granulomas (Schluesener et al., 2001). As witnessed in cerebral trauma specimen
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The primary physiological role of the HO system
2022-01-21
The primary physiological role of the HO system is the protection of Pazopanib Hydrochloride from oxidative stress. These cytoprotective effects are attributable both to the degradation of the pro-oxidant heme and to the positive contribution of the metabolites produced during this degradation, nam
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br Acknowledgements br Funding This work
2022-01-21
Acknowledgements Funding: This work was supported by the Instituto Nacional de Biomedicina do Semiárido (INCT-IBISAB-CNPq), Edital MCT/CNPq N° 014/2010 - Universal and Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES). Introduction Guanylin and uroguanylin are small, heat-
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Two different genes encode GSK isoforms and that
2022-01-21
Two different genes encode GSK-3 isoforms α and β that have very similar catalytic domains but significantly differ in their N- and C-termini. The α and β isoforms split from a common precursor approximately at the emergence of vertebrates, suggesting that at least one of the isoforms took on a new
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br Materials and methods br Results br Discussion
2022-01-20
Materials and methods Results Discussion Disclosures Author contributions Acknowledgements Introduction Diabetes mellitus is one of the fastest growing chronic diseases worldwide, with an estimated prevalence of 382 million patients, of which about 90% have type 2 diabetes melli
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