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br Introduction Cell motility is fundamentally important in
2024-06-19
Introduction Cell motility is fundamentally important in morphogenesis, wound healing, and the immune response. One of the best-studied basic types of cell movement is lamellipodial motility [1, 2], characterized by a thin (∼0.1–0.2 μm), broad (∼10–40 μm) motile appendage containing a dynamic Ber
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G actin has a molecular
2024-06-19
G-actin has a molecular weight of 42 kD and dimensions about 55 × 55 × 35 Å3. It consists of 375 amino acids arranged into two individual domains (Alberts et al., 2014). A central cleft bisects the protein into two aforementioned domains which surround a deep cleft containing ATP or ADP and a tightl
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Molecular docking simulations were carried
2024-06-19
Molecular docking simulations were carried out for ligands – in the ACE crystal structure (1O86) and DPP4 crystal structure (2G5P). Comparison of the binding mode of – () with enalaprilat (a) in ACE shows that the phenethyl group (–, enalaprilat) occupies the S1 pocket and the adjacent carboxylic My
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Introduction Chronic inflammation is increasingly known as o
2024-06-19
Introduction Chronic inflammation is increasingly known as one of the most critical etiological factors in gastrointestinal (GI) cancers (Lee et al., 2016; Wang and Cho, 2015). Overexpression of 5-lipoxygenase (5-LOX), 5-LOX-activating protein (FLAP), as well as other leukotriene (LT) biosynthetic
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GSK2194069 The synthetic route to M developed by Rice was ut
2024-06-19
The synthetic route to M100907 developed by Rice was utilized, however, the chiral resolution was carried out at an earlier stage to provide the possibility of introducing different substituents onto the piperidinyl group. The conditions for this resolution were different from previously reported.
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As mentioned above variation of the A ring was
2024-06-18
As mentioned above, variation of the A-ring was undertaken in order to improve microsomal stability and kinase selectivity relative to neurotensin receptor (). 1-Imidazole-2-carboxamides with substitution at the 4-position (–) were mostly tolerated with 4-cyano-imidazole-2-carboxamide () having comp
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Nowadays more than kinases have been
2024-06-18
Nowadays, more than 500 kinases have been identified of human genome [2]. Imatinib (Gleevec) was the first tyrosine kinase inhibitor approved by the US Food and Drug Administration (FDA) for the treatment of chronic myeloid leukemia [3], and kinases have become an attractive target for the developme
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br Regulation of V ATPase assembly in
2024-06-18
Regulation of V-ATPase assembly in response to changes in amino 5823 levels A central regulator of cell growth and metabolism is mTORC1 [38]. mTORC1 integrates signals from nutrient availability and growth factor receptors to control such processes as protein and lipid synthesis and autophagy. A
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ATP citrate lyase ACLY is a cytosolic enzyme
2024-06-18
ATP citrate lyase (ACLY) is a cytosolic enzyme that catalyzes the generation of acetyl-CoA from citrate [15]. Acetyl-CoA is the building block for the biosynthesis of fatty acids and cholesterol, and also serves as a substrate of the acetylation reaction of various molecules, including histones and
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The downstream targets of ATR involved in mediating human te
2024-06-18
The downstream targets of ATR involved in mediating human telomerase recruitment have not yet been identified. Under stalled fork conditions, activated ATR is able to phosphorylate and activate ATM (Stiff et al., 2006, and Figures 4C and 4D); whether this FAUC-365 of ATM participates in a positive f
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Since obesity appears to impact leptin and adiponectin
2024-06-18
Since obesity appears to impact leptin and adiponectin levels in opposite manners, several studies have suggested that the serum adiponectin/leptin ratio may be a key parameter in indicating the relative risk of postmenopausal breast cancer (Ollberding et al, 2013, Cleary et al, 2009). Therapeutic s
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In summary these data show that
2024-06-18
In summary, these data show that agonist exposure induces internalization and reduction in cell surface HA-mAPJ expression that occurs relatively rapidly during agonist exposure and recovers more slowly after agonist removal. Moreover the ppERK response of mAPJ-HEK293 cells to [Pyr1]apelin-13 desens
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Various antiangiogenic drugs have been analyzed
2024-06-18
Various antiangiogenic drugs have been analyzed over the last few years; noteworthy, bevacizumab, a monoclonal antibody against VEGF-A, alone or in combination with cytotoxic agents showed interesting results in terms of radiographic response rates and progression-free survival in initial phase 2 st
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Kidney contributes importantly to the long term blood pressu
2024-06-18
Kidney contributes importantly to the long-term blood pressure control via regulating sodium homeostasis. Renal proximal tubule (RPT) is one of the most critical segments for sodium reabsorption within kidney and therefore involved in blood pressure adjustment. This process is regulated by numerous
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A unique finding in this study is
2024-06-18
A unique finding in this study is that 12/15-LO influences CREB phosphorylation in the murine brain. While previous reports have found that knockout of 5-lipoxygenase, a related enzyme that also uses arachidonic Pifithrin-α for substrate, can regulate CREB phosphoryation in the context of Alzheimer
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