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10.1007/s00424-014-1488-0 http://scihub22266oqcxt.onion/10.1007/s00424-014-1488-0 24633576!ä!24633576 Deprecated: Implicit conversion from float 209.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 209.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 209.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534       Pflugers+Arch 2014 ; 466 (12): 2177-89 Nephropedia Template TP {{tp|p=24633576|t=2014. Activation of TRPM7 channels by small molecules under physiological conditions |pdf=|usr=}}{{24633576}} gab.com Text Activation of TRPM7 channels by small molecules under physiological conditions JO: Pflugers Arch http://www.kidney.de/pget.php?&tw=1&pmid=24633576 #FOAvip Transient receptor potential cation channel, subfamily M, member 7 (TRPM7) is a cation channel covalently linked to a protein kinase domain. TRPM7 is ubiquitously expressed and regulates key cellular processes such as Mg(2+) homeostasis, motility, and proliferation. TRPM7 is involved in anoxic neuronal death, cardiac fibrosis, and tumor growth. The goal of this work was to identify small molecule activators of the TRPM7 channel and investigate their mechanism of action. We used an aequorin bioluminescence-based assay to screen for activators of the TRPM7 channel. Valid candidates were further characterized using patch clamp electrophysiology. We identified 20 drug-like compounds with various structural backbones that can activate the TRPM7 channel. Among them, the delta opioid antagonist naltriben was studied in greater detail. Naltriben's action was selective among the TRP channels tested. Naltriben activates TRPM7 currents without prior depletion of intracellular Mg(2+) even under conditions of low PIP2. Moreover, naltriben interfered with the effect of the TRPM7 inhibitor NS8593. Finally, our experiments with TRPM7 variants carrying mutations in the pore, TRP, and kinase domains indicate that the site of TRPM7 activation by this small-molecule ligand is most likely located in or near the TRP domain. In conclusion, we identified the first organic small-molecule activators of TRPM7 channels, thus providing new experimental tools to study TRPM7 function in native cellular environments. Twit Text FOAVip Activation of TRPM7 channels by small molecules under physiological conditions ????Pflugers Arch http://www.kidney.de/pget.php?&tw=1&pmid=24633576 #FOAvip Twit Text # Free Paper on # # # # # LINK http://www.kidney.de/pget.php?&tw=1&pmid=24633576 #FOAvip English Wikipedia <ref>{{Cite pmid|24633576}}</ref> Activation of TRPM7 channels by small molecules under physiological conditions #MMPMID24633576 Hofmann T; Schafer S; Linseisen M; Sytik L; Gudermann T; Chubanov V Pflugers Arch 2014[Dec]; 466 (12): 2177-89 PMID24633576show ga Transient receptor potential cation channel, subfamily M, member 7 (TRPM7) is a cation channel covalently linked to a protein kinase domain. TRPM7 is ubiquitously expressed and regulates key cellular processes such as Mg(2+) homeostasis, motility, and proliferation. TRPM7 is involved in anoxic neuronal death, cardiac fibrosis, and tumor growth. The goal of this work was to identify small molecule activators of the TRPM7 channel and investigate their mechanism of action. We used an aequorin bioluminescence-based assay to screen for activators of the TRPM7 channel. Valid candidates were further characterized using patch clamp electrophysiology. We identified 20 drug-like compounds with various structural backbones that can activate the TRPM7 channel. Among them, the delta opioid antagonist naltriben was studied in greater detail. Naltriben's action was selective among the TRP channels tested. Naltriben activates TRPM7 currents without prior depletion of intracellular Mg(2+) even under conditions of low PIP2. Moreover, naltriben interfered with the effect of the TRPM7 inhibitor NS8593. Finally, our experiments with TRPM7 variants carrying mutations in the pore, TRP, and kinase domains indicate that the site of TRPM7 activation by this small-molecule ligand is most likely located in or near the TRP domain. In conclusion, we identified the first organic small-molecule activators of TRPM7 channels, thus providing new experimental tools to study TRPM7 function in native cellular environments. |Action Potentials[MESH] |Animals[MESH] |HEK293 Cells[MESH] |Humans[MESH] |Magnesium/metabolism[MESH] |Mice[MESH] |Naltrexone/analogs & derivatives/pharmacology[MESH] |Phosphatidylinositol 4,5-Diphosphate/metabolism[MESH] |Small Molecule Libraries/chemistry/*pharmacology[MESH]Activation of TRPM7 channels by small molecules under physiological co(epmc).pdf DeepDyve Pubget Overpricing