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10.1074/jbc.RA117.001547 http://scihub22266oqcxt.onion/10.1074/jbc.RA117.001547 C5971468!5971468 !29615494     free     free     free Deprecated: Implicit conversion from float 233.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 233.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 233.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 233.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 233.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 233.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 267.2 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 267.2 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 267.2 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Warning: imagejpeg(C:\Inetpub\vhosts\kidney.de\httpdocs\phplern\29615494 .jpg): Failed to open stream: No such file or directory in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 117       J+Biol+Chem 2018 ; 293 (21 ): 8217-8229 Nephropedia Template TP {{tp|p=29615494 |t=2018. Small molecules that inhibit the late stage of Munc13-4-dependent secretory granule exocytosis in mast cells |pdf=|usr=}}{{29615494 }} gab.com Text Small molecules that inhibit the late stage of Munc13-4-dependent secretory granule exocytosis in mast cells JO: J Biol Chem http://www.kidney.de/pget.php?&tw=1&pmid=29615494 #FOAvip Ca(2+)-dependent secretory granule fusion with the plasma membrane is the final step for the exocytic release of inflammatory mediators, neuropeptides, and peptide hormones. Secretory cells use a similar protein machinery at late steps in the regulated secretory pathway, employing protein isoforms from the Rab, Sec1/Munc18, Munc13/CAPS, SNARE, and synaptotagmin protein families. However, no small-molecule inhibitors of secretory granule exocytosis that target these proteins are currently available but could have clinical utility. Here we utilized a high-throughput screen of a 25,000-compound library that identified 129 small-molecule inhibitors of Ca(2+)-triggered secretory granule exocytosis in RBL-2H3 mast cells. These inhibitors broadly fell into six different chemical classes, and follow-up permeable cell and liposome fusion assays identified the target for one class of these inhibitors. A family of 2-aminobenzothiazoles (termed benzothiazole exocytosis inhibitors or bexins) was found to inhibit mast cell secretory granule fusion by acting on a Ca(2+)-dependent, C2 domain-containing priming factor, Munc13-4. Our findings further indicated that bexins interfere with Munc13-4-membrane interactions and thereby inhibit Munc13-4-dependent membrane fusion. We conclude that bexins represent a class of specific secretory pathway inhibitors with potential as therapeutic agents. Twit Text FOAVip Small molecules that inhibit the late stage of Munc13-4-dependent secretory granule exocytosis in mast cells ????J Biol Chem http://www.kidney.de/pget.php?&tw=1&pmid=29615494 #FOAvip Twit Text # Free Paper on # # # # # LINK http://www.kidney.de/pget.php?&tw=1&pmid=29615494 #FOAvip English Wikipedia <ref>{{Cite pmid|29615494 }}</ref> Small molecules that inhibit the late stage of Munc13-4-dependent secretory granule exocytosis in mast cells #MMPMID29615494 Bruinsma S ; James DJ ; Quintana Serrano M ; Esquibel J ; Woo SS ; Kielar-Grevstad E ; Crummy E ; Qurashi R ; Kowalchyk JA ; Martin TFJ J Biol Chem 2018[May]; 293 (21 ): 8217-8229 PMID29615494 show ga Ca(2+)-dependent secretory granule fusion with the plasma membrane is the final step for the exocytic release of inflammatory mediators, neuropeptides, and peptide hormones. Secretory cells use a similar protein machinery at late steps in the regulated secretory pathway, employing protein isoforms from the Rab, Sec1/Munc18, Munc13/CAPS, SNARE, and synaptotagmin protein families. However, no small-molecule inhibitors of secretory granule exocytosis that target these proteins are currently available but could have clinical utility. Here we utilized a high-throughput screen of a 25,000-compound library that identified 129 small-molecule inhibitors of Ca(2+)-triggered secretory granule exocytosis in RBL-2H3 mast cells. These inhibitors broadly fell into six different chemical classes, and follow-up permeable cell and liposome fusion assays identified the target for one class of these inhibitors. A family of 2-aminobenzothiazoles (termed benzothiazole exocytosis inhibitors or bexins) was found to inhibit mast cell secretory granule fusion by acting on a Ca(2+)-dependent, C2 domain-containing priming factor, Munc13-4. Our findings further indicated that bexins interfere with Munc13-4-membrane interactions and thereby inhibit Munc13-4-dependent membrane fusion. We conclude that bexins represent a class of specific secretory pathway inhibitors with potential as therapeutic agents. |*Exocytosis [MESH] |Animals [MESH] |Cell Degranulation/*drug effects [MESH] |Leukemia, Basophilic, Acute/drug therapy/metabolism/*pathology [MESH] |Mast Cells/drug effects/*pathology [MESH] |Membrane Fusion [MESH] |Proteins/genetics/*metabolism [MESH] |Rats [MESH] |Secretory Vesicles/drug effects/*pathology [MESH] |Small Molecule Libraries/*pharmacology [MESH]Small molecules that inhibit the late stage of Munc13-4-dependent secr(epmc).pdf DeepDyve Pubget Overpricing