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br Conflict of interest statement br Acknowledgments
2022-02-10
Conflict of interest statement Acknowledgments The authors would like to thank Dr. Linda Console-Bram for her editing of this review, Valentina Lucchesi for help with the figures, and acknowledge funding from NIH/NIDA (DA023204). GPR35 is an orphan G protein-coupled receptor (GPCR) implicat
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Oxidative stress results from the disequilibrium between
2022-02-10
Oxidative stress results from the disequilibrium between levels of prooxidant molecules produced and the ability of a biological system to detoxify and neutralize the reactive molecules [14]. OS is a chronic, self-perpetuating state of damage to cells and increased inflammation resulting from the co
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Introduction The hypoglossal nucleus is the nucleus of the
2022-02-10
Introduction The hypoglossal nucleus is the nucleus of the twelfth cranial nerve and is located on both sides of the mid line in the dorsal medulla oblongata and is situated between the proximal end of the medullary central canal and the beginning of the fourth ventricle (Tomasch and Etemadi, 1962)
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ATP is essential for maintaining the ionic balance of
2022-02-10
ATP is essential for maintaining the ionic balance of the lens (Michael and Bron, 2011). Without sufficient ATP there is an ionic imbalance due to Na+K+ATPase dysfunction. Previous studies have shown that rabbit lenses incubated ex vivo without glucose rapidly lost ATP in their lens epithelium and f
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Hydroxysafflor yellow A sale This GluR A independent mechani
2022-02-10
This GluR-A-independent mechanism, by which the associative strength of spatial locations can be increased (and/or decreased) gradually over many trials, and which presumably underlies spatial reference memory acquisition during tasks such as the Morris watermaze or the radial maze (Zamanillo et al.
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The role of cell to cell interactions in coordinating
2022-02-09
The role of cell-to-cell interactions in coordinating the cells’ behaviour to ensure an appropriate anterior pituitary hormone response is receiving increasing attention. Anterior pituitary Tylosin tartrate interact with neighbouring cells through junctional complexes. As their name implies, the co
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Herein we describe the development of second generation GSM
2022-02-09
Herein, we describe the development of second generation GSM compounds aimed at improving critical physicochemical properties while maintaining the potent activity of the parent AGSM. Ligand design focused on identifying heterocyclic replacements for the hydrophobic D-ring as a means to improve ADME
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In the previous paper we described the
2022-02-09
In the previous paper, we described the design and synthesis of tricyclic thiazoles as FBPase inhibitors, and a series of SAR studies led to the identification of phosphate 3 and difluoromethylenephosphonate 4 exhibiting potent FBPase inhibitory activities (IC50=13, 47nM, respectively) (Fig. 2). In
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br Application of TIRFM to visualizing exocytosis TIRFM
2022-02-09
Application of TIRFM to visualizing exocytosis TIRFM was first used to visualize exocytosis from large secretory granules from chromaffin graphpad molarity (Steyer et al., 1997). Before that, visualization of secretory organelle was strictly limited to a few exceptions, such as mast cell of muta
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The lysine K specific demethylase KDM family is
2022-02-09
The lysine (K)-specific demethylase 4 (KDM4) family is comprised of 4 isoforms, KDM4A to -D, also known as JMJD2A to -D. KDM4A, B, and C encode proteins consisting of a JmjC, a JmjN, two PHD, and two Tudor domains. KDM4D is unique within the KDM4 family in that it has neither PHD nor Tudor domains,
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Anti apoptotic Bcl proteins have become attractive
2022-02-09
Anti-apoptotic Bcl-2 proteins have become attractive targets for anti-cancer agents development, because they are associated with progression of a wide variety of human cancers., , The small-molecular Bcl-2 inhibitor venetoclax (ABT-199) () has been approved recently for the treatment of patients wi
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Considering its role in regulating cytoskeletal dynamics
2022-02-09
Considering its role in regulating cytoskeletal dynamics, the Rho kinase effector ROCK has been particularly implicated in tumor metastasis. The ROCK inhibitors Y27632 and fasudil have been extensively studied in cancer and beneficial effects have been observed in many types of cancers (Kale et al.,
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Recently a G protein coupled receptor GPR a was
2022-02-09
Recently, a G-protein-coupled receptor, GPR109a, was identified as a molecular target for niacin. Mechanistic studies have suggested that the benefits of niacin therapy may result from the activation of GPR109a located on adipocytes. Recent experiments have shown that niacin activation of GPR109a re
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Optimization of the tetrahydroindazole series led to the dis
2022-02-08
Optimization of the tetrahydroindazole series led to the discovery of two moderately potent γ-secretase modulators, 2-cyclobutane and 2-hydroxy-2-methylpropane which were subsequently evaluated in a kinetic aqueous solubility assay. Unfortunately, neither analog demonstrated improved solubility ()
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br Structures of human secretase Before the
2022-02-08
Structures of human γ-secretase Before the near-atomic resolution structures, the highest resolutions achieved for γ-secretase were 15 and 12Å [19, 21]. The 15-Å structure revealed a MG 149 chamber in the transmembrane domain and two pores at the top and bottom of γ-secretase, which were specula
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