• The following are the supplementary data

  2021-09-09

  

  The following are the supplementary data related to this article. Transparency document Introduction Hypoxia is a pathological process that causes abnormal changes in metabolism, function and morphological structure of tissue because of insufficient oxygen supply. It's reported that hypoxia w

• Substrate affinity and specificity can be enhanced by dockin

  2021-09-09

  

  Substrate affinity and specificity can be enhanced by docking interactions, in which regions distal to the site of Stiripentol bind to grooves, pockets, or surfaces outside of the kinase catalytic cleft 1, 2, 5, 6. Like catalytic site interactions, docking interactions can involve recognition of sho

• sr9011 receptor During embryogenesis the expression of zGpr

  2021-09-08

  

  During embryogenesis, the expression of zGpr84 was found higher at the cleavage stage and decreased at both blastula and gastrula stages. It indicates that maternal zGpr84 transcripts are present at the cleavage and blastula stages, since zygotic transcripts are not produced before the gastrula stag

• Lactate induced GPR activation was confirmed

  2021-09-08

  

  Lactate-induced GPR81 activation was confirmed with a fluorimetric imaging plate reader (FLIPR) assay, in which lactate induced a [Ca2+] flux in CHO cells stably expressing Gqi5 and HA-GPR81 but not vector control (Fig. 1C). The EC50 of lactate in the FLIPR assay was 4.3±0.73mM, a value well within

• Molecular properties as well as

  2021-09-08

  

  Molecular properties as well as metabolic stability in rat and human liver microsomes for the most active nitro (), nitrile (), methylsulfone (), and sulfonamides () analogues were measured (). All these derivatives possessed excellent membrane permeability as measured in the Pampa assay and further

• The dorsal horn of the spinal cord shows

  2021-09-08

  

  The dorsal horn of the spinal cord shows a high density of Ca2+-permeable AMPA receptors, particularly in the superficial spinal laminae (laminae I and II), where primary afferents carrying nociceptive and thermoreceptive inputs terminate and synapse on spinal second-order neurons (Engelman et al.,

• br Materials and methods br Conflicts

  2021-09-08

  

  Materials and methods Conflicts of interest Some of the peptidomimetic compounds in this work are the subject of the patent application “Peptidomimetics for Imaging the Ghrelin Receptor”, WO/2016/191865 A1, December 8th, 2016. Acknowledgements Special thanks go to Rebecca McGirr (Lawson He

• br Introduction Alzheimer s disease

  2021-09-08

  

  Introduction Alzheimer's disease (AD) affects ca. 46 million people worldwide [1] and it is expected that the number will double or triple by 2030 or 2050, respectively, while no significant progress has been made in research for early diagnosis and new efficient therapies. Currently available me

• In addition to the regulation afforded by calcineurin NFAT a

  2021-09-08

  

  In addition to the regulation afforded by calcineurin/NFAT axis, it has been shown that deregulation of some microRNAs (e.g. miR-155) can induce activation of Fas/FasL-in various cell types [72]. Furthermore, Fas–FasL interactions appear to be an important mechanism for the maintenance of immune pri

• br Materials and methods br Results br

  2021-09-07

  

  Materials and methods Results Discussion The major findings of the present study are that: 1) the response to inverse agonists may be crossregulated by the activation of either Dexlansoprazole H1 or H2 receptors, 2) histamine H1 and H2 receptor inverse agonists crossdesensitize the receptor

• Oltipraz has been shown to inhibit the

  2021-09-07

  

  Oltipraz has been shown to inhibit the growth of HCC orexin receptor and is being evaluated in clinical trials as a potential anti-cancer drug for HCC (Mann et al., 2009; Piton et al., 2005; Yates and Kensler, 2007). The present observation that pre-treatment of tumorigenic liver cells with oltipra

• For further understanding of the interaction between these

  2021-09-07

  

  For further understanding of the interaction between these inhibitors and proteins (BRafV600E and HDAC1) for guiding the SAR, compound 10e, the most potent compound of this series, was chosen as a representative for docking into the BRafV600E (PDB code: 1UWJ) and HDAC1 (PDB code: 1C3R), revealing ex

• Cysteine Cys residues are frequently found to be highly

  2021-09-07

  

  Cysteine (Cys) residues are frequently found to be highly conserved within functional, regulatory, catalytic, or binding sites of proteins. Thiol or thiolate chemistry imparts active sites with unique properties like nucleophilicity, high affinity metal binding, and disulfide bond assisted multimeri

• One important aspect about GSK inhibitors is

  2021-09-07

  

  One important aspect about GSK-3 inhibitors is their effect on pluripotency of Ticlopidine HCl [4]. Many GSK-3 inhibitors are ATP-competitive and suppress both GSK-3alpha and GSK-3beta [476]. BIO was shown to suppress GSK-3 activity and promote Wnt/beta-catenin signaling. This combination of events

• Introduction Nicotinic acid niacin NA has been used in

  2021-09-07

  

  Introduction Nicotinic crm1 (niacin, NA) has been used in the treatment of dislipidemia and cardiovascular disease for almost 60years (Offermanns, 2006). Large clinical studies showed that niacin alone or in combination with LDL-lowering drugs improved cardiovascular outcomes (Canner et al., 1986,

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