• These reports have gradually established G quadruplex bindin

  2022-02-24

  

  These reports have gradually established G-quadruplex binding small molecules as promising anti-cancer therapeutic agents. Besides the stabilization of G-quadruplex structures, some of these molecules also serve as diagnostic probes and sensors for G-quadruplexes in vitro and in vivo. Of these, Thio

• One effective approach to fine tuning

  2022-02-24

  

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

• Introduction Cancer has been a significant public health

  2022-02-24

  

  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

• Historically pharmacological investigations have been

  2022-02-24

  

  Historically, pharmacological investigations have been carried out by first identifying a biological response to a ligand, and then subsequently using that ligand to identify the receptor(s) responsible for the response (Wilson et al., 1998). However, this approach needed revision with the discovery

• The physiological and pharmacological roles

  2022-02-24

  

  The physiological and pharmacological roles of GPR81 remain largely unclear because of several reasons. The low potency of lactate agonizing GPR81 in the millimolar range, together with its fast metabolic turnover, renders as a challenge in in vivo studies using lactate. Furthermore, there are no po

• br Conflicts of interest br Funding This work was supported

  2022-02-23

  

  Conflicts of interest Funding This work was supported by the National Natural Science Foundation of China (No.81670558; 81800542), and the Science & Technology Development Fund of Tianjin Education Commission for Higher Education (No.2017KJ221). Acknowledgements Introduction Free fatty

• ICH induced striatal lesion produced a reduction of EAAT exp

  2022-02-23

  

  ICH-induced striatal lesion produced a reduction of EAAT1 expression analogous to the decreased glutamate uptake at 6 h. The combined reduction of excitatory amino diacerein receptor transporters and of glutamate uptake activity might explain the well-known glutamate excitotoxicity following brain

• br GSMs Secretase cleavage of APP generates a

  2022-02-23

  

  GSMs γ-Secretase cleavage of APP generates a number of Aβ peptides [32], [137]. In most cells Aβ1–37, 38, 39, and 42 are produced at low levels (typically each represents 5–20% of total Aβ detected) and the major species generated is Aβ1–40 (typically over 50% of total Aβ). Other Aβ peptides can

• NMDARs are glutamate gated ionotropic

  2022-02-23

  

  NMDARs are glutamate-gated ionotropic receptors that are involved in excitatory neurotransmission and plasticity (Traynelis et al., 2010). There have been several reports showing that neurosteroids acting as negative modulators of NMDARs exert neuroprotective activity in both in vitro and in vivo mo

• Colorectal cancer CRC is the third most common

  2022-02-23

  

  Colorectal cancer (CRC) is the third most common cancer in men and the second in women worldwide and almost 55% of the cases occur in more developed areas of the world. In the 2012, more than 1.3 million new cases were reported, which accounts for about 10% of the total cancers worldwide (GLOBOCAN,

• uPAR promotes cell associated proteolysis by binding to uPA

  2022-02-23

  

  uPAR promotes cell-associated proteolysis by binding to uPA which locally converts plasminogen into active plasmin [10]. Ligand-engaged uPAR also acts as a potent regulator of cell migration and matrix attachment. Being a membrane receptor, uPAR needs to interact with extracellular matrix (ECM) prot

• Receptor interactions and binding mode of in hGPR were deter

  2022-02-23

  

  Receptor interactions and binding mode of in hGPR40 were determined by docking studies. The compound was docked in the rebuilt co-crystal structure of hGPR40 (PDB ID: ) using MOE for loop modeling and energy minimization and Glide for molecular docking. The docking site used for the docking simulat

• br Conflict of interest br Acknowledgments

  2022-02-23

  

  Conflict of interest Acknowledgments The research was funded by the Major Programs of Pharmaceutical research project of Jiangsu Province (Q2018044). Introduction Lipids are important regulators of cell death. In mammalian cells, both apoptotic and non-apoptotic cell death pathways can be

• Proteinase K In cardiomyocytes mechanical stress builds

  2022-02-23

  

  In cardiomyocytes mechanical stress builds up via FAs and the related costamere structures, and excessive stress can cause cardiac hypertrophy. Cardoso et al. (2016) report a comprehensive study that demonstrates the link between stress-induced FAK activation and a FAK-mediated initiation of a trans

• rta 3 Occupying at least of brain

  2022-02-23

  

  Occupying at least 50% of rta 3 volume, astroglial cells not only possess a high level of association in network through gap junctions and direct intercellular communications [28], but also are extensively exposed to extracellular fluid and contribute in shaping different types of synapses [29]. Our

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