Use my Search Websuite to scan PubMed, PMCentral, Journal Hosts and Journal Archives, FullText. Kick-your-searchterm to multiple Engines kick-your-query now !>

A dictionary by aggregated review articles of nephrology, medicine and the life sciences Your one-stop-run pathway from word to the immediate pdf of peer-reviewed on-topic knowledge.

10.1002/anie.202105584 http://scihub22266oqcxt.onion/10.1002/anie.202105584 34097796!8456925!34097796     free     free     free Warning: file_get_contents(https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pubmed&id=34097796&cmd=llinks): Failed to open stream: HTTP request failed! HTTP/1.1 429 Too Many Requests in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 215       Angew+Chem+Int+Ed+Engl 2021 ; 60 (33): 18231-18239 Nephropedia Template TP {{tp|p=34097796|t=2021. Combining High-Throughput Synthesis and High-Throughput Protein Crystallography for Accelerated Hit Identification |pdf=|usr=}}{{34097796}} gab.com Text Combining High-Throughput Synthesis and High-Throughput Protein Crystallography for Accelerated Hit Identification JO: Angew Chem Int Ed Engl http://www.kidney.de/pget.php?&tw=1&pmid=34097796 #FOAvip Protein crystallography (PX) is widely used to drive advanced stages of drug optimization or to discover medicinal chemistry starting points by fragment soaking. However, recent progress in PX could allow for a more integrated role into early drug discovery. Here, we demonstrate for the first time the interplay of high throughput synthesis and high throughput PX. We describe a practical multicomponent reaction approach to acrylamides and -esters from diverse building blocks suitable for mmol scale synthesis on 96-well format and on a high-throughput nanoscale format in a highly automated fashion. High-throughput PX of our libraries efficiently yielded potent covalent inhibitors of the main protease of the COVID-19 causing agent, SARS-CoV-2. Our results demonstrate, that the marriage of in situ HT synthesis of (covalent) libraires and HT PX has the potential to accelerate hit finding and to provide meaningful strategies for medicinal chemistry projects. Twit Text FOAVip Combining High-Throughput Synthesis and High-Throughput Protein Crystallography for Accelerated Hit Identification ????Angew Chem Int Ed Engl http://www.kidney.de/pget.php?&tw=1&pmid=34097796 #FOAvip Twit Text # Free Paper on # # # # # LINK http://www.kidney.de/pget.php?&tw=1&pmid=34097796 #FOAvip English Wikipedia <ref>{{Cite pmid|34097796}}</ref> Combining High-Throughput Synthesis and High-Throughput Protein Crystallography for Accelerated Hit Identification #MMPMID34097796 Sutanto F; Shaabani S; Oerlemans R; Eris D; Patil P; Hadian M; Wang M; Sharpe ME; Groves MR; Domling A Angew Chem Int Ed Engl 2021[Aug]; 60 (33): 18231-18239 PMID34097796show ga Protein crystallography (PX) is widely used to drive advanced stages of drug optimization or to discover medicinal chemistry starting points by fragment soaking. However, recent progress in PX could allow for a more integrated role into early drug discovery. Here, we demonstrate for the first time the interplay of high throughput synthesis and high throughput PX. We describe a practical multicomponent reaction approach to acrylamides and -esters from diverse building blocks suitable for mmol scale synthesis on 96-well format and on a high-throughput nanoscale format in a highly automated fashion. High-throughput PX of our libraries efficiently yielded potent covalent inhibitors of the main protease of the COVID-19 causing agent, SARS-CoV-2. Our results demonstrate, that the marriage of in situ HT synthesis of (covalent) libraires and HT PX has the potential to accelerate hit finding and to provide meaningful strategies for medicinal chemistry projects. |Acrylamides/chemical synthesis/metabolism[MESH] |Acrylates/chemical synthesis/metabolism[MESH] |Catalytic Domain[MESH] |Coronavirus 3C Proteases/antagonists & inhibitors/chemistry/*metabolism[MESH] |Crystallography, X-Ray[MESH] |Cysteine Proteinase Inhibitors/chemical synthesis/*metabolism[MESH] |Drug Discovery[MESH] |High-Throughput Screening Assays[MESH] |Protein Binding[MESH] |SARS-CoV-2/chemistry[MESH]Combining High-Throughput Synthesis and High-Throughput Protein Crysta(epmc).pdf DeepDyve Pubget Overpricing