• CgtA is involved in stringent response

  2022-03-07

  

  CgtA is involved in stringent response and it interacts with SpoT to maintain optimal (p)ppGpp/ppGpp quotient in bacteria. Depletion of CgtA results in increased ppGpp levels [8]. CgtA is also important for cellular development [12] and involved in synchronization of DNA replication initiation and c

• A few of the islet specific proteins identified

  2022-03-07

  

  A few of the islet-specific proteins identified in the present study have previously been described in various contexts of pancreatic islets, i.e. PTPRN, SCG5, SCGN, SNAP25 and SNED1, validating the search algorithm applied and supporting the notion that also the novel proteins identified are indeed

• br Results and discussion br Conclusion

  2022-03-07

  

  Results and discussion Conclusion In summary, starting from our previous lead CGP41251 1, we replaced the 5-nitropyrimidine core with pyrimidopyrimidine to obtain a series of novel compounds as drug candidates of GPR119 agonist for treatment of type 2 diabetes. Some derivatives showed good ago

• In patients with type diabetes glucagon receptor antagonism

  2022-03-04

  

  In patients with type 2 diabetes glucagon receptor antagonism led lowered fasting glucose however not postprandial glucose levels [9], which may reflect that glucagon may not be of particular importance for the diabetic hyperglycemia upon a meal. Current glucagon receptor antagonists have however be

• Gastric inhibitory polypeptide a hormone belonging to the

  2022-03-04

  

  Gastric inhibitory polypeptide, a hormone belonging to the glucagon-secretin family of peptides, exhibits protection against the neurodegeneration and also stimulates neurogenesis in adult rats in a paracrine manner (Gault and Holscher, 2008, Nyberg et al., 2005, Usdin et al., 1993). The expression

• br Presenilins and Wnt catenin signalling Several groups hav

  2022-03-04

  

  Presenilins and Wnt/β-catenin signalling Several groups have provided substantial data indicating that PS1 acts as a negative modulator of the transcriptional activity of the β-catenin/Tcf-4 complex (Fig. 4) [120], [121], [122]. β-Catenin is a multifunctional protein that was first described as a

• br FXR FGF in the

  2022-03-04

  

  FXR–FGF15/19 in the control of BAs synthesis The nuclear receptor FXR is the master regulator of BAs homeostasis, modulating their synthesis, Pyridostatin and uptake [15]. FXR decreases BA de novo hepatic biosynthesis by reducing the expression of CYP7A1. At the canalicular membrane, newly-synth

• cgrp antagonist One effective approach to fine tuning the li

  2022-03-04

  

  One effective approach to fine-tuning the lipophilicity profile of FFA1 agonists is to ‘decorate’ the 3-phenylpropahoic cgrp antagonist scaffold with polar heterocyclic moieties. Alternatively, this scaffold could be replaced with heterocyclic isosteres (as in Takeda’s compounds 1,2 and 3 as well a

• Through the analysis of various synthetic GPR

  2022-03-04

  

  Through the analysis of various synthetic GPR40 agonists as reported in literature, we found that a number of these compounds contained a phenylpropanoic Telaprevir synthesis motif which was inspired from naturally occurring medium to long chain fatty acids. For instance, in the early period of dis

• MMV s distinct mode of inhibition addresses key

  2022-03-04

  

  MMV019313's distinct mode of inhibition addresses key impediments in the development of PfFPPS/GGPPS inhibitors as antimalarial drugs. First, it is the first non-bisphosphonate inhibitor of Plasmodium FPPS/GGPPS with drug-like physicochemical properties satisfying the “Rule of 5” (Van Voorhis et al.

• In conclusion a series of new carboxamido aryl

  2022-03-04

  

  In conclusion, a series of new 3-carboxamido-5-aryl-isoxazoles was designed, synthesized and screened for their inhibitory potency against FAAH. Their cytotoxicity was determined and their lipophilicity was calculated. Compounds bearing a 3-substituted biphenyl moiety with high Log values displayed

• In tumor cells HK II induction

  2022-03-03

  

  In tumor cells HK-II induction is mediated by Akt/mTOR pathway [6], [11]. HK-II dynamically shuttles between the mitochondria and cytoplasm under different metabolic conditions. In cardiomyocytes, Akt enhances HK-II binding to mitochondria, setting the heart at a state resistant to ischemic injury [

• Hepatitis C virus HCV is a frequent cause of infectious

  2022-03-03

  

  Hepatitis C virus (HCV) is a frequent cause of infectious chronic hepatitis. Unlike hepatitis A and B, there is no vaccine to prevent hepatitis C infection yet. According to WHO, around 200 million people are infected with HCV worldwide [1], in addition to three to four million newly infected patien

• br Niacin has long been used for

  2022-03-03

  

  Niacin () () has long been used for the treatment of lipid disorders and for the prevention of cardiovascular disease, the leading cause of death in the U.S., as a result of its ability to raise high-density lipoprotein (HDL) levels. Recent mechanistic investigations have shown that niacin may exe

• One difficulty in studying gp

  2022-03-03

  

  One difficulty in studying gp120 is that it binds to more than one receptor. Understanding how (-)-epicatechin receptor respond to gp120 is complex because of this promiscuity. In an attempt to establish the contribution of CXCR4 in the antagonistic effect of gp120 on morphine-induced antinocicepti

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