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10.1038/ncomms11384 http://scihub22266oqcxt.onion/10.1038/ncomms11384 C4853478!4853478 !27122193     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 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 Warning: imagejpeg(C:\Inetpub\vhosts\kidney.de\httpdocs\phplern\27122193 .jpg): Failed to open stream: No such file or directory in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 117       Nat+Commun 2016 ; 7 (ä): 11384 Nephropedia Template TP {{tp|p=27122193 |t=2016. Polycomb repressive complex 2 structure with inhibitor reveals a mechanism of activation and drug resistance |pdf=|usr=}}{{27122193 }} gab.com Text Polycomb repressive complex 2 structure with inhibitor reveals a mechanism of activation and drug resistance JO: Nat Commun http://www.kidney.de/pget.php?&tw=1&pmid=27122193 #FOAvip Polycomb repressive complex 2 (PRC2) mediates gene silencing through chromatin reorganization by methylation of histone H3 lysine 27 (H3K27). Overexpression of the complex and point mutations in the individual subunits of PRC2 have been shown to contribute to tumorigenesis. Several inhibitors of the PRC2 activity have shown efficacy in EZH2-mutated lymphomas and are currently in clinical development, although the molecular basis of inhibitor recognition remains unknown. Here we report the crystal structures of the inhibitor-bound wild-type and Y641N PRC2. The structures illuminate an important role played by a stretch of 17 residues in the N-terminal region of EZH2, we call the activation loop, in the stimulation of the enzyme activity, inhibitor recognition and the potential development of the mutation-mediated drug resistance. The work presented here provides new avenues for the design and development of next-generation PRC2 inhibitors through establishment of a structure-based drug design platform. Twit Text FOAVip Polycomb repressive complex 2 structure with inhibitor reveals a mechanism of activation and drug resistance ????Nat Commun http://www.kidney.de/pget.php?&tw=1&pmid=27122193 #FOAvip Twit Text # Free Paper on # # # # # LINK http://www.kidney.de/pget.php?&tw=1&pmid=27122193 #FOAvip English Wikipedia <ref>{{Cite pmid|27122193 }}</ref> Polycomb repressive complex 2 structure with inhibitor reveals a mechanism of activation and drug resistance #MMPMID27122193 Brooun A ; Gajiwala KS ; Deng YL ; Liu W ; Bolaņos B ; Bingham P ; He YA ; Diehl W ; Grable N ; Kung PP ; Sutton S ; Maegley KA ; Yu X ; Stewart AE Nat Commun 2016[Apr]; 7 (ä): 11384 PMID27122193 show ga Polycomb repressive complex 2 (PRC2) mediates gene silencing through chromatin reorganization by methylation of histone H3 lysine 27 (H3K27). Overexpression of the complex and point mutations in the individual subunits of PRC2 have been shown to contribute to tumorigenesis. Several inhibitors of the PRC2 activity have shown efficacy in EZH2-mutated lymphomas and are currently in clinical development, although the molecular basis of inhibitor recognition remains unknown. Here we report the crystal structures of the inhibitor-bound wild-type and Y641N PRC2. The structures illuminate an important role played by a stretch of 17 residues in the N-terminal region of EZH2, we call the activation loop, in the stimulation of the enzyme activity, inhibitor recognition and the potential development of the mutation-mediated drug resistance. The work presented here provides new avenues for the design and development of next-generation PRC2 inhibitors through establishment of a structure-based drug design platform. |Antineoplastic Agents/*chemistry [MESH] |Drug Resistance, Neoplasm [MESH] |Enhancer of Zeste Homolog 2 Protein/chemistry/genetics/metabolism [MESH] |Enzyme Inhibitors/*chemistry [MESH] |Humans [MESH] |Models, Molecular [MESH] |Mutation [MESH] |Neoplasms/genetics/metabolism [MESH]Polycomb repressive complex 2 structure with inhibitor reveals a mecha(epmc).pdf DeepDyve Pubget Overpricing