FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2949202626> ?p ?o ?g. }

• W2949202626 endingPage "6162" @default.
• W2949202626 startingPage "6146" @default.
• W2949202626 abstract "Targeted covalent inhibitors (TCIs) have attracted growing attention from the pharmaceutical industry in recent decades because they have potential advantages in terms of efficacy, selectivity, and safety. TCIs have recently evolved into a new version with reversibility that can be systematically modulated. This feature may diminish the risk of haptenization and help optimize the drug–target residence time as needed. The enteroviral 3C protease (3Cpro) is a valuable therapeutic target, but the development of 3Cpro inhibitors is far from satisfactory. Therefore, we aimed to apply a reversible TCI approach to the design of novel 3Cpro inhibitors. The introduction of various substituents onto the α-carbon of classical Michael acceptors yielded inhibitors bearing several classes of warheads. Using steady-state kinetics and biomolecular mass spectrometry, we confirmed the mode of reversible covalent inhibition and elucidated the mechanism by which the potency and reversibility were affected by electronic and steric factors. This research produced several potent inhibitors with good selectivity and suitable reversibility; moreover, it validated the reversible TCI approach in the field of viral infection, suggesting broader applications in the design of reversible covalent inhibitors for other proteases." @default.
• W2949202626 created "2019-06-27" @default.
• W2949202626 creator A5016806784 @default.
• W2949202626 creator A5024365809 @default.
• W2949202626 creator A5047649241 @default.
• W2949202626 creator A5053920011 @default.
• W2949202626 creator A5054957857 @default.
• W2949202626 creator A5067064015 @default.
• W2949202626 creator A5074499208 @default.
• W2949202626 creator A5075439180 @default.
• W2949202626 creator A5076582791 @default.
• W2949202626 date "2019-06-11" @default.
• W2949202626 modified "2023-10-13" @default.
• W2949202626 title "Application of Dually Activated Michael Acceptor to the Rational Design of Reversible Covalent Inhibitor for Enterovirus 71 3C Protease" @default.
• W2949202626 cites W1970988101 @default.
• W2949202626 cites W1998948439 @default.
• W2949202626 cites W2010993054 @default.
• W2949202626 cites W2031799240 @default.
• W2949202626 cites W2048072131 @default.
• W2949202626 cites W2051620175 @default.
• W2949202626 cites W2077424659 @default.
• W2949202626 cites W2088307139 @default.
• W2949202626 cites W2093217911 @default.
• W2949202626 cites W2134612577 @default.
• W2949202626 cites W2153977062 @default.
• W2949202626 cites W2237489673 @default.
• W2949202626 cites W2282075251 @default.
• W2949202626 cites W2317424391 @default.
• W2949202626 cites W2326100802 @default.
• W2949202626 cites W2395363162 @default.
• W2949202626 cites W248383993 @default.
• W2949202626 cites W2516283456 @default.
• W2949202626 cites W2517550655 @default.
• W2949202626 cites W2531391789 @default.
• W2949202626 cites W2553303154 @default.
• W2949202626 cites W2571523815 @default.
• W2949202626 cites W2623565822 @default.
• W2949202626 cites W2796108867 @default.
• W2949202626 cites W2898502203 @default.
• W2949202626 cites W3189337309 @default.
• W2949202626 cites W4247370221 @default.
• W2949202626 cites W4376595609 @default.
• W2949202626 doi "https://doi.org/10.1021/acs.jmedchem.9b00387" @default.
• W2949202626 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/31184893" @default.
• W2949202626 hasPublicationYear "2019" @default.
• W2949202626 type Work @default.
• W2949202626 sameAs 2949202626 @default.
• W2949202626 citedByCount "17" @default.
• W2949202626 countsByYear W29492026262020 @default.
• W2949202626 countsByYear W29492026262021 @default.
• W2949202626 countsByYear W29492026262022 @default.
• W2949202626 countsByYear W29492026262023 @default.
• W2949202626 crossrefType "journal-article" @default.
• W2949202626 hasAuthorship W2949202626A5016806784 @default.
• W2949202626 hasAuthorship W2949202626A5024365809 @default.
• W2949202626 hasAuthorship W2949202626A5047649241 @default.
• W2949202626 hasAuthorship W2949202626A5053920011 @default.
• W2949202626 hasAuthorship W2949202626A5054957857 @default.
• W2949202626 hasAuthorship W2949202626A5067064015 @default.
• W2949202626 hasAuthorship W2949202626A5074499208 @default.
• W2949202626 hasAuthorship W2949202626A5075439180 @default.
• W2949202626 hasAuthorship W2949202626A5076582791 @default.
• W2949202626 hasConcept C118792377 @default.
• W2949202626 hasConcept C161790260 @default.
• W2949202626 hasConcept C171250308 @default.
• W2949202626 hasConcept C178790620 @default.
• W2949202626 hasConcept C180577832 @default.
• W2949202626 hasConcept C181199279 @default.
• W2949202626 hasConcept C182220744 @default.
• W2949202626 hasConcept C185592680 @default.
• W2949202626 hasConcept C192562407 @default.
• W2949202626 hasConcept C201194858 @default.
• W2949202626 hasConcept C21951064 @default.
• W2949202626 hasConcept C53105671 @default.
• W2949202626 hasConcept C55493867 @default.
• W2949202626 hasConcept C70721500 @default.
• W2949202626 hasConcept C71240020 @default.
• W2949202626 hasConcept C74187038 @default.
• W2949202626 hasConcept C86803240 @default.
• W2949202626 hasConceptScore W2949202626C118792377 @default.
• W2949202626 hasConceptScore W2949202626C161790260 @default.
• W2949202626 hasConceptScore W2949202626C171250308 @default.
• W2949202626 hasConceptScore W2949202626C178790620 @default.
• W2949202626 hasConceptScore W2949202626C180577832 @default.
• W2949202626 hasConceptScore W2949202626C181199279 @default.
• W2949202626 hasConceptScore W2949202626C182220744 @default.
• W2949202626 hasConceptScore W2949202626C185592680 @default.
• W2949202626 hasConceptScore W2949202626C192562407 @default.
• W2949202626 hasConceptScore W2949202626C201194858 @default.
• W2949202626 hasConceptScore W2949202626C21951064 @default.
• W2949202626 hasConceptScore W2949202626C53105671 @default.
• W2949202626 hasConceptScore W2949202626C55493867 @default.
• W2949202626 hasConceptScore W2949202626C70721500 @default.
• W2949202626 hasConceptScore W2949202626C71240020 @default.
• W2949202626 hasConceptScore W2949202626C74187038 @default.
• W2949202626 hasConceptScore W2949202626C86803240 @default.
• W2949202626 hasFunder F4320321001 @default.
• W2949202626 hasFunder F4320321540 @default.

• next