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Although the ramifications of non additive SAR are context d
2022-02-14

Although the ramifications of non-additive SAR are context-dependent, the knowledge that perturbations in one region of a chemical series are not synergistic with perturbations in another region of the same chemical series is clearly pertinent to any medicinal chemistry effort. In our experience, no
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Target regulated the formation of G quadruplex was used here
2022-02-14

Target-regulated the formation of G-quadruplex was used here to “kill two methylphenidate hcl with one stone” for the detection of melamine and I− with one probe DNA. G-quadruplexes are higher-order structures formed from G-rich oligonucleotides through the stacking of planar G-tetrads [43,44]. The
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Growing evidence supporting the anti inflammatory and tissue
2022-02-14

Growing evidence supporting the anti-inflammatory and tissue-protective effects of FPR antagonists led to the screening of commercial libraries for novel small-molecule FPR antagonists. As result of these screening efforts and/or structure–activity relationship (SAR)-directed design and synthesis, a
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Apoptosis via Fas FasL system has been evidenced to play
2022-02-14

Apoptosis via Fas/FasL system has been evidenced to play a role in the pathogenesis of many diseases [26], [27], [28], [29], [30], [31], [32], [33], [34]. Along with these, Fas/FasL system has an important role in progressive renal disease and organ rejection in renal, cardiac and liver transplanta
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po1 HCC metastasis is a multistep multifactorial process inc
2022-02-14

HCC metastasis is a multistep, multifactorial process, including adhesion of tumor po1 to the extracellular matrix (ECM), remodeling and degradation of ECM, invasion through local tissue, intravasation into blood or lymph vessels, and forming new tumors at distant sites [6,7]. Loss of adhesion or ad
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Our present data together with other studies have shown
2022-02-14

Our present data together with other studies have shown that the communication of stroma and cancer cells via ECM-cell interaction led to the primary activation of FAK [41]. Here we propose a model depicting an important role of ADAM12-L in the regulation of ESCC invasion and metastasis. ADAM12-L ov
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The first wave of cells infiltrating
2022-02-12

The first wave of gsk products infiltrating heart shortly after MI is composed mainly of neutrophils, with the highest number on the first day after ischemic episode [101]. These cells are recruited via C-X-C motif chemokine ligand-2 (CXCL-2)- and CXCL-5-mediated chemotaxis. Both chemokines are pro
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br Pathophysiology of glaucoma Glaucoma is a
2022-02-12

Pathophysiology of glaucoma Glaucoma is a group of optic neuropathies defined by progressive degeneration of RGCs and their monensin in the optic nerve, which leads to irreversible loss of vision [3,8,9]. RGC degeneration is often significantly advanced before changes in visual acuity and evidenc
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GPR is present primarily in
2022-02-12

GPR119 is present primarily in the pancreas and the intestine. Activation of GPR119 increases insulin, GLP-1, GIP and PYY secretion. GPR119 agonists stimulate insulin release in a glucose-dependent manner. The glucose dependent insulin secretion (GIDS) mechanism makes GPR119 an attractive target for
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In glioma or glial derived primary brain
2022-02-12

In glioma, or glial-derived primary ace inhibitor tumors, as in other cancers, glutathione is an important survival mechanism. Glioma cells are dependent upon SXC-mediated cystine uptake for viability, as they require intracellular cystine/cysteine for GSH synthesis (Ogunrinu and Sontheimer, 2010,
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Glucose uptake a critical metabolic control point in
2022-02-12

Glucose uptake, a critical metabolic control point in glycolysis, is mediated by the GLUT (SLC2) family of integral membrane transporters (Mueckler and Thorens, 2013). GLUT1 (SLC2A1), one of the most well-studied members of the SLC2 family, exhibits a wide tissue distribution; cell surface expressio
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Ketamine has recently been found to exert rapid and sustaine
2022-02-12

Ketamine has recently been found to exert rapid and sustained antidepressant effect. Single dose ketamine can have an efficacy of up to 1 week [20]. Furthermore, ketamine is an effective drug against refractory depression [21,22]. The antidepressant mechanism of ketamine is still unclear. Whether CO
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br Introduction The glucagon receptor GCGR is a G protein
2022-02-12

Introduction The glucagon receptor (GCGR) is a G-protein-coupled receptor expressed mainly in the liver and kidney. Upon glucagon binding, it activates the stimulatory G protein (Gs) and increases cAMP level, subsequently transducing glucagon signaling involved in glucose, amino acids and lipid m
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br Acknowledgments The research leading to these results
2022-02-12

Acknowledgments The research leading to these results was funded by European Community’s Seventh Framework Programme (FP7/2007-2013) under grant agreement No. 222719 – LIFECYCLE and by the Foundation for Science and Technology of Portugal (FCT), through projects PTDC/MAR-BIO/3890/2012 and PEst-C/
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Combination inhibitors of FAAH TRPV and or COX
2022-02-11

Combination inhibitors of FAAH, TRPV1, and/or COX2 may have the advantage of effective pain relief with a high therapeutic index. For example, arachidonoyl serotonin (AA-5-HT) inhibits both FAAH (IC=1–12μM) and TRPV1 (IC=37–270nM against 100nM capsaicin in HEK-293 cells)., In mice, AA-5-HT had grea
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