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至今,GenScript的服務(wù)及產(chǎn)品已被Cell, Nature, Science, PNAS等1300多家生物醫(yī)藥類雜志引用近萬(wàn)次,處于行業(yè)領(lǐng)先水平。NIH、哈佛、耶魯、斯坦福、普林斯頓、杜克大學(xué)等約400家全球著名機(jī)構(gòu)使用GenScript的基因合成、多肽服務(wù)、抗體服務(wù)和蛋白服務(wù)等成功地發(fā)表科研成果,再次證明GenScript 有能力幫助業(yè)內(nèi)科學(xué)家Make research easy.

Fragment-based screening targeting an open form of the SARS-CoV-2 main protease binding pocket

Acta Crystallogr D Struct Biol. 2024-01; 
Chia Ying Huang, Alexander Metz, Roland Lange, Nadia Artico, Céline Potot, Julien Hazemann, Manon Müller, Marina Dos Santos, Alain Chambovey, Daniel Ritz, Deniz Eris, Solange Meyer, Geoffroy Bourquin, May Sharpe, Aengus Mac Sweeney
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Proteins, Expression, Isolation and Analysis … sites (GenScript) and transformed into E. coli BL21(DE3) cells. The protein was expressed … The hexahistidine SUMO-3CLpro fusion protein was purified by immobilized metal affinity … Get A Quote

摘要

To identify starting points for therapeutics targeting SARS-CoV-2, the Paul Scherrer Institute and Idorsia decided to collaboratively perform an X-ray crystallographic fragment screen against its main protease. Fragment-based screening was carried out using crystals with a pronounced open conformation of the substrate-binding pocket. Of 631 soaked fragments, a total of 29 hits bound either in the active site (24 hits), a remote binding pocket (three hits) or at crystal-packing interfaces (two hits). Notably, two fragments with a pose that was sterically incompatible with a more occluded crystal form were identified. Two isatin-based electrophilic fragments bound covalently to the catalytic cysteine residue. The... More

關(guān)鍵詞

3CLpro, SARS-CoV-2, X-ray crystallography, covalent binders, fragment screening, surface plasmon resonance
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