• In the course of studies leading to the discovery of

  2021-12-20

  

  In the course of studies leading to the discovery of , modifications at the P3-P4 interface of these tripeptide-based inhibitors were examined with the goal of improving potency while maintaining a PK profile similar to . In this report, we summarize those studies which led to the identification of

• br Ketone body metabolism and neuronal excitability One

  2021-12-20

  

  Ketone body metabolism and neuronal excitability One of the best examples of the close connection between metabolism and neuronal excitability is illustrated by the effect of ketone bodies on epileptic seizures. One third of patients suffering from epileptic seizures do not respond to conventiona

• Our overall goal is to develop selective

  2021-12-20

  

  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

• Importance of glucokinase in glucose homeostasis and a possi

  2021-12-20

  

  Importance of glucokinase in glucose homeostasis and a possibility to change its activity using the activators define the scientific interest in the development of new allosteric activators of GK (Liu et al., 2012, Pfefferkorn et al., 2011, Waring et al., 2013, Behera et al., 2015). Activation of gl

• histamine receptor br Methods br Results br Discussion The

  2021-12-20

  

  Methods Results Discussion The measurement of intraocular pressure was made with a commercially available rebound tonometer, the Tonovet®. In our studies, Tonovet® underestimated the intraocular pressure in both animal models, being this effect more pronounced in the rat. To study the effe

• More recently Dal Peraro and coworkers carried out s CG

  2021-12-20

  

  More recently, Dal Peraro and coworkers [38] carried out 4 μs CG MD simulations of GS with six randomly placed C9915-55 peptides embedded into a synaptic plasma bilayer model. This lipid raft model was constituted by 32 different sr9009 and cholesterol (54.74%). In this study, the authors observed a

• The development of metabolic stable non peptidergic

  2021-12-20

  

  The development of metabolic stable, non-peptidergic galanin agonists could be the basis to clinical diagnosis and treatment of tumors with high levels of galanin receptor expression like gliomas and pituitary tumors. As for gliomas, penetration of the blood brain barrier by the compounds might be p

• It should be noted that the applied steered unfolding of

  2021-12-20

  

  It should be noted that the applied steered unfolding of the i-motif and G-quadruplex satisfies the conditions of Jarzynski inequality for computations of the free energy change. [41] However, in order to reproduce the free energy with an adequate quality a number of nonequilibrium unfolding transit

• br Conclusions br Conflicts of interest

  2021-12-20

  

  Conclusions Conflicts of interest Funding The research work was partially supported by National Science Center (Contract Grant Number: UMO-2015/19/B/NZ1/00332). Introduction Frusectose-1, 6-bisphosphatase (FBPase) has long been recognized as a potential therapeutic target for the treatm

• Several small molecules such as erastin and

  2021-12-20

  

  Several small molecules, such as erastin and RSL3, are reported to induce ferroptosis in both normal and cancer multidrug resistance transporter [21,22]. We confirmed that erastin-induced growth inhibition is an ideal ferroptosis model for cardiomyocytes. The erastin inhibits the growth of H9c2 cel

• Our paper also contributes to the

  2021-12-20

  

  Our paper also contributes to the large, but hitherto inconclusive literature that studies the effects of option-based compensation or convexity in compensation on corporate risk-taking policies. On the one hand, some studies document a positive relationship by showing that convexity increases lever

• Based on the above presumption activation of Sox and FAK

  2021-12-20

  

  Based on the above presumption, activation of Sox11 and FAK might be beneficial for alleviating the VILI. Previous studies have showed the relevance of Sox11 or FAK up-regulation with improvement of tissue injury. For example, over-expression of Sox11 protected and improved the tissue function or st

• The mast cell has long been

  2021-12-20

  

  The mast cell has long been recognized as central to the mediation of allergic responses not least because it is the principal repository of histamine in the body. Following activation by allergens, the mast cell can release histamine as well as generate a host of additional mediators such as cystei

• br Acknowledgments We thank Dr Kathleen Sullivan

  2021-12-18

  

  Acknowledgments We thank Dr Kathleen Sullivan of Merck Research Laboratories for providing the CHO-K1 orexin expressing an NFAT-β-lactamase reporter and the Gα subunit Gqi5, Dr. Chen Liaw (Arena Pharmaceutical), Ms. Rebecca Kaplan, Mr. Frank Xiaodong Gan for technical assistance, Dr. Andrew Howar

• Obestatin synthetized mainly in the gastrointestinal tract p

  2021-12-18

  

  Obestatin, synthetized mainly in the gastrointestinal tract, participates in the regulation of metabolic functioning at both central and peripheral levels (food intake, pancreatic activity or/and adipocytes proliferation) (Granata et al., 2008; Li et al., 2011). It is involved in the complex gut-bra

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