• 4 methylumbelliferone receptor Compared with the tetrazole d

  2022-02-11

  

  Compared with the tetrazole derivative , the potency of analogs – was 3- to 17-fold improved. Of the range of heterocycles prepared, 1,2,4-thiadiazol-5(4)-one and 1,3,4-oxadiazol-2(3)-one showed the best potencies of 0.52μM and 0.61μM, respectively. Introduction of a second hydrogen bond donor, su

• br Mutagenesis and Receptor Modeling Studies br

  2022-02-11

  

  Mutagenesis and Receptor-Modeling Studies Signal Transduction and Receptor Desensitization Therapeutic Potential of HCA Receptor Ligands Although all members of the HCA receptor family are potentially interesting drug targets, only HCA2 is currently exploited as such. Therefore, this sectio

• The GPR receptor is also emerging as

  2022-02-11

  

  The GPR55 receptor is also emerging as an important therapeutic target. GPR55−/− mice possess no overt phenotype, but were protected in models of inflammatory and neuropathic pain (Staton et al., 2008). Staton et al. (2008) reported that no GPR55 mRNA could be detected by RT-PCR in the animals. Also

• The hypothesis that genes involved in

  2022-02-11

  

  The hypothesis that genes involved in type 2 diabetes evolved under changing selective pressures and may carry the signature of natural selection motivated us to describe patterns of sequence variation at CAPN10 and GPR35 in human populations. An initial population genetics study reported an unusual

• br Opportunities The ever expanding diabetes market is one o

  2022-02-11

  

  Opportunities The ever-expanding diabetes market is one of the driving forces for the development of new antidiabetes drugs. Diabetes mellitus influenced an estimated 371 million humans during 2012 worldwide, and this figure is projected to increase in every country. According to International Di

• br Several reports have shown an anti proliferative

  2022-02-11

  

  Several reports have shown an anti-proliferative effect of type I IFNs on CD4+ T bcrp inhibitor activated in vitro either upon anti-CD3 antibody treatment [28,29] or upon cognate antigen stimulation [29]. However, the in vivo setting is a lot more complex, since the final outcome is the net effec

• In summary we have developed an efficient

  2022-02-11

  

  In summary, we have developed an efficient synthetic route to the required urea-isostere containing hydroxamic acid-based inhibitor . The target molecule, , was found to retain the inhibitory potency of the corresponding carbo-analog against glyoxalase-I while possessing resistance to cleavage by γ

• br Conflict of interest br Funding br Acknowledgements

  2022-02-11

  

  Conflict of interest Funding Acknowledgements Introduction to SLC6 transporters The solute carrier (SLC) 6 family of membrane proteins perform the Na+-coupled symport of amino acids and amino cysteine protease inhibitors derivatives into cells throughout the body. Disrupting neurotransm

• br Recent insights into EAAT structure function aspects The

  2022-02-11

  

  Recent insights into EAAT structure/function aspects The EAATs are secondary-active transporters coupling the movement of one Glu with the symport of three Na+ and one proton and the counter-transport of one K+ [3, 4]. The transporters are trimeric assemblies of protomers that function independen

• The mammalian AMPA receptor protein family comprises four

  2022-02-11

  

  The mammalian AMPA receptor protein family comprises four subunits, termed GluR-A through GluR-D (or GluR1 through GluR4), which form hetero-tetrameric receptor complexes Dingledine et al. 1999, Rosenmund et al. 1998. These subunits possess distinctive intracellular C-terminal domains that can be gr

• Acarbose and voglibose the classic

  2022-02-11

  

  Acarbose and voglibose, the classic α-glucosidase inhibitors, were clinically used to inhibit α-glucosidase activity for the treatment of type 2 diabetes. However, the intake of these drugs may cause some undesirable gastrointestinal side effects and weight gain (Xu et al., 2015). The synthetic drug

• Together our data are consistent

  2022-02-10

  

  Together, our data are consistent with the idea that the antidepressant-like effect of a low dose of galanin administration in the DRN would be mediated by the activation of local GAL2. To support this hypothesis, we set an additional experiment to evaluate whether the antidepressant-like effect of

• Myelination by oligodendrocytes is required for saltatory ne

  2022-02-10

  

  Myelination by oligodendrocytes is required for saltatory nerve impulse conduction and proper CNS function (Bercury and Macklin, 2015). Defects in myelination and remyelination impair saltatory nerve conduction and functional connectivity leading to cognitive, behavioral, and motor deficits in neuro

• br Introduction Erythropoietin EPO is a glycoprotein

  2022-02-10

  

  Introduction Erythropoietin (EPO) is a glycoprotein hormone and the principal stimulator of erythropoiesis (Jelkmann, 2011). EPO promotes the proliferation and differentiation of red blood cells, which is important for oxygen transport. Low EPO levels in blood cause anemia; however, excessive lev

• The H autoreceptors distributed mainly in the CNS act as

  2022-02-10

  

  The H3 autoreceptors distributed mainly in the CNS act as a negative feedback on histamine synthesis and release from histaminergic neurons. Histamine is involved in many physiological functions such as sleep-wake regulation, circadian and feeding rhythm, thermal regulation, locomotion, learning, co

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