• Our overall goal is to develop selective

  2022-03-18

  

  Our overall goal is to develop selective compounds for low-affinity/high-capacity transporters inhibitors (i.e. OCT1–3 and PMAT), and provide the field with much needed, specific pharmacological tools to study these transporters. In our initial efforts, we synthesized halogen substituted analogs and

• Here we studied GLUT targeted

  2022-03-17

  

  Here, we studied GLUT1-targeted nanomedicines as a new strategy directed to overcome vascular barrier, enhancing delivery and efficacy in solid tumors. These nanomedicines were prepared by controlled installation of glucose on polymeric micelles incorporating the antitumor agent cisplatin, which is

• The most ubiquitous serine threonine phosphatases such

  2022-03-17

  

  The most ubiquitous serine/threonine phosphatases, such as PP1, PP2A, and PP2B are known to contribute to the majority of phosphatase activity in the heart [4]. Dysregulation of these and other PPs have been found in numerous CVDs, including heart failure (HF), and may play a critical role in reduce

• How changes in APP processing by secretase

  2022-03-17

  

  How changes in APP processing by γ-secretase lead to AD is still not well understood. Deposition of amyloid beta (Aβ) peptide fragments of the amyloid precursor protein (APP) in amyloid plaques and hyperphosphorylated tau in neurofibrillary tangles are the cellular hallmarks of AD (O’Brien and Wong,

• br Results br Discussion secretase

  2022-03-17

  

  Results Discussion γ-secretase-mediated proteolysis of integral membrane proteins is required for diverse biological processes (Lal and Caplan, 2011). One γ-secretase target of particular interest is Notch, as recent work has shown Notch activity to be increased in obesity and associated metab

• br Galanin in depression A

  2022-03-17

  

  Galanin in depression A major impediment in depression research is the lack of validated animals´ models. Animals not only lack consciousness of self, self-reflection and consideration of others but also hallmarks of the disorder such as depressed mood, low self-esteem or suicidal intent are hard

• br Competing interests br Authors

  2022-03-17

  

  Competing interests Authors contributions Transparency document Introduction Non-alcoholic fatty liver disease (NAFLD) is a spectrum of liver diseases ranging from simple steatosis to non-alcoholic steatohepatitis (NASH), which may further progress to liver cirrhosis and liver carcinoma

• br Materials and methods br

  2022-03-17

  

  Materials and methods Results Discussion Several studies highlighted an improvement of glycaemic control in diabetic patients receiving sunitinib, while the underlying mechanism remained still elusive [3], [4], [5], [6], [8]. The present study gives evidence that sunitinib directly and spec

• The Ala to Leu substitution would reduce

  2022-03-17

  

  The Ala116 to Leu110 substitution would reduce the size of the active-site cavity disfavoring the production of longer allylic compounds as a result of steric hindrance, according to the observations of Poulter and co-workers [29], [30]. However, this explanation appears to be unlikely since several

• Computational approaches such as docking

  2022-03-17

  

  Computational approaches such as docking and classical molecular dynamics (MD) are now commonly used to study the structure and dynamics of proteins as well as associated protein-ligand interactions [12]. A fundamental requirement of MD in order to accurately determine the behavior of a protein over

• Mitochondrial binding by HK prevents

  2022-03-17

  

  Mitochondrial binding by HK prevents mortality by inhibiting pro-apoptotic factor (Bcl-2 family)-mediated opening of the mitochondrial permeability transition pore (mPTP) (Arora and Pedersen, 1988, Calmettes et al., 2016, Kodde et al., 2007, Pedersen et al., 2002, Rosano, 2011, Schindler and Foley,

• Treatment and control for IBD are

  2022-03-17

  

  Treatment and control for IBD are targeted to identify and eliminate the cause if possible, decrease intestinal inflammation, reduce diarrhea and vomiting, improve appetite, and promote weight gain. Methods include dietary manipulation with or without concurrent medical therapy such as corticosteroi

• Biochemical and genetic studies indicate that the endosomal

  2022-03-17

  

  Biochemical and genetic studies indicate that the endosomal sorting complex required for transport (ESCRT) machinery is crucial for Hh exovesicle packaging and morphogen gradient function 39., 43., 44.. In vertebrates, ESCRT proteins promote the release of Shh exovesicles to maintain progenitor cell

• Let Therefore where F X denotes the rate

  2022-03-16

  

  Let Therefore,where F(X) denotes the rate of production of new people who get infected and V(x) represents the motion of individuals in compartments, which gives us Now, the derivative of F and V calculated at an equilibrium point E0 gives matrices f and v of order 6 × 6 defined aswhere Thus, th

• It is known that changes in cGMP

  2022-03-16

  

  It is known that changes in cGMP levels are positively correlated with plant adaptation to environmental stresses. It seems that a novel group of moonlighting kinases with GC activity is particularly involved in response to biotic stress. It was shown that danger-associated molecular pattern (DAMPs)

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