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10.1016/j.chembiol.2021.04.020 http://scihub22266oqcxt.onion/10.1016/j.chembiol.2021.04.020 33979649!8075810!33979649     free     free     free Deprecated: Implicit conversion from float 231.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 231.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 231.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 231.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 231.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 231.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534       Cell+Chem+Biol 2021 ; 28 (6): 855-865.e9 Nephropedia Template TP {{tp|p=33979649|t=2021. Development of potent and selective inhibitors targeting the papain-like protease of SARS-CoV-2 |pdf=|usr=}}{{33979649}} gab.com Text Development of potent and selective inhibitors targeting the papain-like protease of SARS-CoV-2 JO: Cell Chem Biol http://www.kidney.de/pget.php?&tw=1&pmid=33979649 #FOAvip The COVID-19 pandemic has been disastrous to society and effective drugs are urgently needed. The papain-like protease domain (PLpro) of SARS-CoV-2 (SCoV2) is indispensable for viral replication and represents a putative target for pharmacological intervention. In this work, we describe the development of a potent and selective SCoV2 PLpro inhibitor, 19. The inhibitor not only effectively blocks substrate cleavage and immunosuppressive function imparted by PLpro, but also markedly mitigates SCoV2 replication in human cells, with a submicromolar IC(50). We further present a convenient and sensitive activity probe, 7, and complementary assays to readily evaluate SCoV2 PLpro inhibitors in vitro or in cells. In addition, we disclose the co-crystal structure of SCoV2 PLpro in complex with a prototype inhibitor, which illuminates their detailed binding mode. Overall, these findings provide promising leads and important tools for drug discovery aiming to target SCoV2 PLpro. Twit Text FOAVip Development of potent and selective inhibitors targeting the papain-like protease of SARS-CoV-2 ????Cell Chem Biol http://www.kidney.de/pget.php?&tw=1&pmid=33979649 #FOAvip Twit Text # Free Paper on # # # # # LINK http://www.kidney.de/pget.php?&tw=1&pmid=33979649 #FOAvip English Wikipedia <ref>{{Cite pmid|33979649}}</ref> Development of potent and selective inhibitors targeting the papain-like protease of SARS-CoV-2 #MMPMID33979649 Shan H; Liu J; Shen J; Dai J; Xu G; Lu K; Han C; Wang Y; Xu X; Tong Y; Xiang H; Ai Z; Zhuang G; Hu J; Zhang Z; Li Y; Pan L; Tan L Cell Chem Biol 2021[Jun]; 28 (6): 855-865.e9 PMID33979649show ga The COVID-19 pandemic has been disastrous to society and effective drugs are urgently needed. The papain-like protease domain (PLpro) of SARS-CoV-2 (SCoV2) is indispensable for viral replication and represents a putative target for pharmacological intervention. In this work, we describe the development of a potent and selective SCoV2 PLpro inhibitor, 19. The inhibitor not only effectively blocks substrate cleavage and immunosuppressive function imparted by PLpro, but also markedly mitigates SCoV2 replication in human cells, with a submicromolar IC(50). We further present a convenient and sensitive activity probe, 7, and complementary assays to readily evaluate SCoV2 PLpro inhibitors in vitro or in cells. In addition, we disclose the co-crystal structure of SCoV2 PLpro in complex with a prototype inhibitor, which illuminates their detailed binding mode. Overall, these findings provide promising leads and important tools for drug discovery aiming to target SCoV2 PLpro. |A549 Cells[MESH] |Animals[MESH] |Antiviral Agents/administration & dosage/chemistry/metabolism[MESH] |COVID-19 Drug Treatment[MESH] |COVID-19/enzymology[MESH] |Coronavirus Papain-Like Proteases/*antagonists & inhibitors/chemistry/metabolism[MESH] |Dose-Response Relationship, Drug[MESH] |Drug Delivery Systems/*methods[MESH] |Drug Development/*methods[MESH] |HEK293 Cells[MESH] |HeLa Cells[MESH] |Humans[MESH] |Mice[MESH] |Molecular Docking Simulation/methods[MESH] |Protease Inhibitors/*administration & dosage/chemistry/metabolism[MESH] |Protein Structure, Secondary[MESH] |Protein Structure, Tertiary[MESH]Development of potent and selective inhibitors targeting the papain-li(epmc).pdf DeepDyve Pubget Overpricing