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10.1002/anie.202016961 http://scihub22266oqcxt.onion/10.1002/anie.202016961 33655614!8014119!33655614     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 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 Deprecated: Implicit conversion from float 267.2 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534       Angew+Chem+Int+Ed+Engl 2021 ; 60 (18): 10423-10429 Nephropedia Template TP {{tp|p=33655614|t=2021. Targeting the Main Protease of SARS-CoV-2: From the Establishment of High Throughput Screening to the Design of Tailored Inhibitors |pdf=|usr=}}{{33655614}} gab.com Text Targeting the Main Protease of SARS-CoV-2: From the Establishment of High Throughput Screening to the Design of Tailored Inhibitors JO: Angew Chem Int Ed Engl http://www.kidney.de/pget.php?&tw=1&pmid=33655614 #FOAvip The main protease of SARS-CoV-2 (M(pro) ), the causative agent of COVID-19, constitutes a significant drug target. A new fluorogenic substrate was kinetically compared to an internally quenched fluorescent peptide and shown to be ideally suitable for high throughput screening with recombinantly expressed M(pro) . Two classes of protease inhibitors, azanitriles and pyridyl esters, were identified, optimized and subjected to in-depth biochemical characterization. Tailored peptides equipped with the unique azanitrile warhead exhibited concomitant inhibition of M(pro) and cathepsin L, a protease relevant for viral cell entry. Pyridyl indole esters were analyzed by a positional scanning. Our focused approach towards M(pro) inhibitors proved to be superior to virtual screening. With two irreversible inhibitors, azanitrile 8 (k(inac) /K(i) =37 500 m(-1) s(-1) , K(i) =24.0 nm) and pyridyl ester 17 (k(inac) /K(i) =29 100 m(-1) s(-1) , K(i) =10.0 nm), promising drug candidates for further development have been discovered. Twit Text FOAVip Targeting the Main Protease of SARS-CoV-2: From the Establishment of High Throughput Screening to the Design of Tailored Inhibitors ????Angew Chem Int Ed Engl http://www.kidney.de/pget.php?&tw=1&pmid=33655614 #FOAvip Twit Text # Free Paper on # # # # # LINK http://www.kidney.de/pget.php?&tw=1&pmid=33655614 #FOAvip English Wikipedia <ref>{{Cite pmid|33655614}}</ref> Targeting the Main Protease of SARS-CoV-2: From the Establishment of High Throughput Screening to the Design of Tailored Inhibitors #MMPMID33655614 Breidenbach J; Lemke C; Pillaiyar T; Schakel L; Al Hamwi G; Diett M; Gedschold R; Geiger N; Lopez V; Mirza S; Namasivayam V; Schiedel AC; Sylvester K; Thimm D; Vielmuth C; Phuong Vu L; Zyulina M; Bodem J; Gutschow M; Muller CE Angew Chem Int Ed Engl 2021[Apr]; 60 (18): 10423-10429 PMID33655614show ga The main protease of SARS-CoV-2 (M(pro) ), the causative agent of COVID-19, constitutes a significant drug target. A new fluorogenic substrate was kinetically compared to an internally quenched fluorescent peptide and shown to be ideally suitable for high throughput screening with recombinantly expressed M(pro) . Two classes of protease inhibitors, azanitriles and pyridyl esters, were identified, optimized and subjected to in-depth biochemical characterization. Tailored peptides equipped with the unique azanitrile warhead exhibited concomitant inhibition of M(pro) and cathepsin L, a protease relevant for viral cell entry. Pyridyl indole esters were analyzed by a positional scanning. Our focused approach towards M(pro) inhibitors proved to be superior to virtual screening. With two irreversible inhibitors, azanitrile 8 (k(inac) /K(i) =37 500 m(-1) s(-1) , K(i) =24.0 nm) and pyridyl ester 17 (k(inac) /K(i) =29 100 m(-1) s(-1) , K(i) =10.0 nm), promising drug candidates for further development have been discovered. |*COVID-19 Drug Treatment[MESH] |Antiviral Agents/chemistry/*pharmacology[MESH] |COVID-19/metabolism/virology[MESH] |Coronavirus 3C Proteases/*antagonists & inhibitors/metabolism[MESH] |Drug Design[MESH] |Drug Discovery[MESH] |HEK293 Cells[MESH] |High-Throughput Screening Assays[MESH] |Humans[MESH] |Molecular Docking Simulation[MESH] |Nitriles/chemistry/*pharmacology[MESH] |Protease Inhibitors/chemistry/*pharmacology[MESH] |Pyridines/chemistry/pharmacology[MESH] |SARS-CoV-2/*drug effects/enzymology/physiology[MESH]Targeting the Main Protease of SARS-CoV-2: From the Establishment of H(epmc).pdf DeepDyve Pubget Overpricing