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10.1016/j.str.2020.10.007 http://scihub22266oqcxt.onion/10.1016/j.str.2020.10.007 33152262!7584437!33152262     free     free     free Deprecated: Implicit conversion from float 219.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 219.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 219.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 219.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 219.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 219.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534       Structure 2020 ; 28 (12): 1313-1320.e3 Nephropedia Template TP {{tp|p=33152262|t=2020. Malleability of the SARS-CoV-2 3CL M(pro) Active-Site Cavity Facilitates Binding of Clinical Antivirals |pdf=|usr=}}{{33152262}} gab.com Text Malleability of the SARS-CoV-2 3CL M(pro) Active-Site Cavity Facilitates Binding of Clinical Antivirals JO: Structure http://www.kidney.de/pget.php?&tw=1&pmid=33152262 #FOAvip The COVID-19 pandemic caused by SARS-CoV-2 requires rapid development of specific therapeutics and vaccines. The main protease of SARS-CoV-2, 3CL M(pro), is an established drug target for the design of inhibitors to stop the virus replication. Repurposing existing clinical drugs can offer a faster route to treatments. Here, we report on the binding mode and inhibition properties of several inhibitors using room temperature X-ray crystallography and in vitro enzyme kinetics. The enzyme active-site cavity reveals a high degree of malleability, allowing aldehyde leupeptin and hepatitis C clinical protease inhibitors (telaprevir, narlaprevir, and boceprevir) to bind and inhibit SARS-CoV-2 3CL M(pro). Narlaprevir, boceprevir, and telaprevir are low-micromolar inhibitors, whereas the binding affinity of leupeptin is substantially weaker. Repurposing hepatitis C clinical drugs as COVID-19 treatments may be a useful option to pursue. The observed malleability of the enzyme active-site cavity should be considered for the successful design of specific protease inhibitors. Twit Text FOAVip Malleability of the SARS-CoV-2 3CL M(pro) Active-Site Cavity Facilitates Binding of Clinical Antivirals ????Structure http://www.kidney.de/pget.php?&tw=1&pmid=33152262 #FOAvip Twit Text # Free Paper on # # # # # LINK http://www.kidney.de/pget.php?&tw=1&pmid=33152262 #FOAvip English Wikipedia <ref>{{Cite pmid|33152262}}</ref> Malleability of the SARS-CoV-2 3CL M(pro) Active-Site Cavity Facilitates Binding of Clinical Antivirals #MMPMID33152262 Kneller DW; Galanie S; Phillips G; O'Neill HM; Coates L; Kovalevsky A Structure 2020[Dec]; 28 (12): 1313-1320.e3 PMID33152262show ga The COVID-19 pandemic caused by SARS-CoV-2 requires rapid development of specific therapeutics and vaccines. The main protease of SARS-CoV-2, 3CL M(pro), is an established drug target for the design of inhibitors to stop the virus replication. Repurposing existing clinical drugs can offer a faster route to treatments. Here, we report on the binding mode and inhibition properties of several inhibitors using room temperature X-ray crystallography and in vitro enzyme kinetics. The enzyme active-site cavity reveals a high degree of malleability, allowing aldehyde leupeptin and hepatitis C clinical protease inhibitors (telaprevir, narlaprevir, and boceprevir) to bind and inhibit SARS-CoV-2 3CL M(pro). Narlaprevir, boceprevir, and telaprevir are low-micromolar inhibitors, whereas the binding affinity of leupeptin is substantially weaker. Repurposing hepatitis C clinical drugs as COVID-19 treatments may be a useful option to pursue. The observed malleability of the enzyme active-site cavity should be considered for the successful design of specific protease inhibitors. |*Antiviral Agents/pharmacology[MESH] |*Betacoronavirus/metabolism[MESH] |*COVID-19[MESH] |*Coronavirus Infections/drug therapy[MESH] |Catalytic Domain[MESH] |Crystallography, X-Ray[MESH] |Cysteine Endopeptidases/metabolism[MESH] |Humans[MESH] |Pandemics[MESH] |Protease Inhibitors/pharmacology[MESH] |SARS-CoV-2[MESH] |Temperature[MESH]Malleability of the SARS-CoV-2 3CL M(pro) Active-Site Cavity Facilitat(epmc).pdf DeepDyve Pubget Overpricing