• br Results br Discussion secretase mediated proteolysis of i

  2022-04-06

  

  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

• In addition to our results Chen

  2022-04-06

  

  In addition to our results, Chen et al. showed that administration of the GalR1 antagonist M40 improves cardiac function and attenuates cardiac remodeling in rats with heart failure [26]. These effects might be attributed to M40 suppression of galanin inhibitory effect on the vagal nerve in heart fa

• br Conclusion Discovery of an ideal orally active

  2022-04-02

  

  Conclusion Discovery of an ideal orally active antithrombotic drug has remained elusive till date. Research efforts in this direction led to the discovery of numerous coagulation enzyme inhibitors including various thrombin and FXa inhibitors. Several preclinical studies have highlighted the impo

• Additionally to their peripheral effects evidence indicate a

  2022-04-02

  

  Additionally to their peripheral effects, evidence indicate a role for ETs in the central nervous system (Mosqueda-Garcı́a et al., 1993). Indeed, using Northern blot analysis and in situ hybridization it has been shown the presence of immunoreactive ET of non-vascular origin and of neuronal location

• In studies described earlier IRL

  2022-04-02

  

  In studies described earlier, IRL-1620 was administered intravenously; however, because of its short half-life (Rubin and Levin, 1994) (about 7–8min), the dosing had to be repeated three times. Also, a dose-dependent hypotension was observed with repeated doses of IRL-1620 in rats (Leonard and Gulat

• Introduction The Antiretroviral Therapy ART

  2022-04-02

  

  Introduction The Antiretroviral Therapy (ART), in the last decade, has been providing a better treatment for the Human Immunodeficiency Virus 1 (HIV) infection, by reducing its viral load to undetectable levels and recovering the immune system. In fact, according to the last data from UNAIDS the mo

• br Conclusion br Author contributions br

  2022-04-02

  

  Conclusion Author contributions Ethics approval Competing interests Introduction VHL is a well-known tumor suppressor and works as a target recruitment subunit of an E3 ubiquitin ligase complex that recruits hydroxylated hypoxia inducible factor α (HIF-α) for proteasomal degradation u

• Different crystal structures of both HOs were reported and s

  2022-04-02

  

  Different crystal structures of both HOs were reported and showed that the three-dimensional structures of proteins (HO-1: PDB code 1N45, HO-2: PDB code 2QPP) are predominantly in an α-helical conformation, with the heme packed between two helices (distal and proximal), and present a remarkable stru

• ICLs represent of all generated DNA adducts for cisplatin

  2022-04-02

  

  ICLs represent ICL Inducers in Cancer Therapy Nitrogen mustards with aromatic substituents (chlorambucil, melphalan) or a bioactivatable phosphoramide group (cyclophosphamide) were one of the first identified DNA crosslinkers. These agents are still used in combined schemes for the therapy of chr

• Introduction Cancer has been a significant public

  2022-04-02

  

  Introduction Cancer has been a significant public health problem in the world with more patients being diagnosed every year. However, chemotherapy from non-specific cytotoxic agents that as an effective means of cancer treatment is limited by severe side effects and poor selectivity. Thus, the deve

• We started our investigation by evaluating

  2022-04-01

  

  We started our investigation by evaluating the impact of changes to the piperidine moiety of (). As demonstrated with morpholine and piperazine , attenuation of nitrogen basicity resulted in complete loss of activity, suggesting that a basic heterocyclic nitrogen is important for potent inhibition.

• K-7174 receptor The amyloid precursor protein APP is a membr

  2022-04-01

  

  The amyloid precursor protein (APP) is a membrane protein thought to be involved in plasticity, synapse formation and repair, and export of metal ions [68]. The APP present in the brain can be cleaved by three different secretases [73], [74]. Cleavage of APP first by alpha secretase and then gamma-s

• br Introduction Maintaining blood glucose within an appropri

  2022-04-01

  

  Introduction Maintaining blood glucose within an appropriate range is crucial for survival. In diabetes, those who suffer episodes of severe hypoglycemia have an increased risk of death [1], [2]. The kt 4 is especially dependent on an adequate, continuous supply of circulating glucose to fuel met

• Lidocaine Analogous to all GPCRs the GLP

  2022-04-01

  

  Analogous to all GPCRs, the GLP-1R transduces signals from the outside of the cell to the inside by allosterically converting a ligand-binding event to activation of intracellular effectors. The GLP-1R couples to several intracellular effectors and this pleiotropic coupling is physiologically releva

• Previously we have shown that ghrelin and

  2022-04-01

  

  Previously, we have shown that ghrelin and cannabinoids stimulate hypothalamic AMPK activity (Kola et al., 2005). In contrast, both the orexigenic compounds have inhibitory effects on AMPK activity in the liver and visceral fat (Kola et al., 2005). In this study, we were able to reproduce our previo

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