FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W4205652591> ?p ?o ?g. }

• W4205652591 endingPage "128548" @default.
• W4205652591 startingPage "128548" @default.
• W4205652591 abstract "Toll-like receptors (TLRs) 7 and 8 are key targets in the development of immunomodulatory drugs for treating infectious disease, cancer, and autoimmune disorders. These receptors can adopt both agonist and antagonist binding conformations that switch the receptor signal on or off to the downstream production of cytokines. In this study, we examined the effect of simple isomeric substitutions to the C2-butyl group of two imidazoquinoline agonists and evaluated the activity of these analogs using both TLR7 and TLR8 reporter cells and cytokine induction assays. Results are presented showing the C2-isobutyl and C2-cyclopropylmethyl isomers are both mixed TLR7/8 competitive antagonists of the parent agonist [4-Amino-1-(4-(aminomethyl)benzyl)-2-butyl-7-methoxycarbonyl-1H-imidazo[4,5-c]quinoline], indicating the conformation of the dimeric receptor complex is highly sensitive to steric perturbations to the ligand binding pocket. This observation is consistent with prior work demonstrating TLR7 and TLR8 activity is directly correlated to C2-alkyl substitutions that project into a hydrophobic pocket at the dimer interface of the receptor. The close structural relationship of the agonist/antagonist pairs identified here highlights the importance of this pocket in tipping the balance between the agonist and antagonist binding states of the receptor which may have significant ramifications to the design of imidazoquinoline-based immunomodulatory agents." @default.
• W4205652591 created "2022-01-26" @default.
• W4205652591 creator A5002739271 @default.
• W4205652591 creator A5032149358 @default.
• W4205652591 creator A5033110476 @default.
• W4205652591 creator A5046692924 @default.
• W4205652591 creator A5053465014 @default.
• W4205652591 creator A5076681768 @default.
• W4205652591 creator A5078796555 @default.
• W4205652591 date "2022-03-01" @default.
• W4205652591 modified "2023-10-18" @default.
• W4205652591 title "Toll-like receptor 7 and 8 imidazoquinoline-based agonist/antagonist pairs" @default.
• W4205652591 cites W1440342876 @default.
• W4205652591 cites W1542775986 @default.
• W4205652591 cites W1965435219 @default.
• W4205652591 cites W1974046193 @default.
• W4205652591 cites W1978898713 @default.
• W4205652591 cites W1999182967 @default.
• W4205652591 cites W2005012808 @default.
• W4205652591 cites W2026506816 @default.
• W4205652591 cites W2035729149 @default.
• W4205652591 cites W2041176311 @default.
• W4205652591 cites W2052277212 @default.
• W4205652591 cites W2054680036 @default.
• W4205652591 cites W2061343703 @default.
• W4205652591 cites W2062267695 @default.
• W4205652591 cites W2071543087 @default.
• W4205652591 cites W2083029364 @default.
• W4205652591 cites W2111797481 @default.
• W4205652591 cites W2129708174 @default.
• W4205652591 cites W2146724504 @default.
• W4205652591 cites W2176745654 @default.
• W4205652591 cites W2286109529 @default.
• W4205652591 cites W2331786627 @default.
• W4205652591 cites W2610264107 @default.
• W4205652591 cites W2765445021 @default.
• W4205652591 cites W2767892990 @default.
• W4205652591 cites W2768367424 @default.
• W4205652591 cites W2904734349 @default.
• W4205652591 cites W2952393861 @default.
• W4205652591 cites W2952474097 @default.
• W4205652591 cites W2961550379 @default.
• W4205652591 cites W2985283228 @default.
• W4205652591 cites W3016627961 @default.
• W4205652591 cites W3046159581 @default.
• W4205652591 cites W3046455346 @default.
• W4205652591 cites W3092996142 @default.
• W4205652591 cites W3162795453 @default.
• W4205652591 cites W3164029425 @default.
• W4205652591 doi "https://doi.org/10.1016/j.bmcl.2022.128548" @default.
• W4205652591 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/35051578" @default.
• W4205652591 hasPublicationYear "2022" @default.
• W4205652591 type Work @default.
• W4205652591 citedByCount "4" @default.
• W4205652591 countsByYear W42056525912022 @default.
• W4205652591 countsByYear W42056525912023 @default.
• W4205652591 crossrefType "journal-article" @default.
• W4205652591 hasAuthorship W4205652591A5002739271 @default.
• W4205652591 hasAuthorship W4205652591A5032149358 @default.
• W4205652591 hasAuthorship W4205652591A5033110476 @default.
• W4205652591 hasAuthorship W4205652591A5046692924 @default.
• W4205652591 hasAuthorship W4205652591A5053465014 @default.
• W4205652591 hasAuthorship W4205652591A5076681768 @default.
• W4205652591 hasAuthorship W4205652591A5078796555 @default.
• W4205652591 hasConcept C116569031 @default.
• W4205652591 hasConcept C170493617 @default.
• W4205652591 hasConcept C185592680 @default.
• W4205652591 hasConcept C2776885963 @default.
• W4205652591 hasConcept C2778122271 @default.
• W4205652591 hasConcept C2778938600 @default.
• W4205652591 hasConcept C55493867 @default.
• W4205652591 hasConcept C58732023 @default.
• W4205652591 hasConcept C71240020 @default.
• W4205652591 hasConcept C86803240 @default.
• W4205652591 hasConcept C86811712 @default.
• W4205652591 hasConcept C98274493 @default.
• W4205652591 hasConceptScore W4205652591C116569031 @default.
• W4205652591 hasConceptScore W4205652591C170493617 @default.
• W4205652591 hasConceptScore W4205652591C185592680 @default.
• W4205652591 hasConceptScore W4205652591C2776885963 @default.
• W4205652591 hasConceptScore W4205652591C2778122271 @default.
• W4205652591 hasConceptScore W4205652591C2778938600 @default.
• W4205652591 hasConceptScore W4205652591C55493867 @default.
• W4205652591 hasConceptScore W4205652591C58732023 @default.
• W4205652591 hasConceptScore W4205652591C71240020 @default.
• W4205652591 hasConceptScore W4205652591C86803240 @default.
• W4205652591 hasConceptScore W4205652591C86811712 @default.
• W4205652591 hasConceptScore W4205652591C98274493 @default.
• W4205652591 hasLocation W42056525911 @default.
• W4205652591 hasLocation W42056525912 @default.
• W4205652591 hasOpenAccess W4205652591 @default.
• W4205652591 hasPrimaryLocation W42056525911 @default.
• W4205652591 hasRelatedWork W1780338288 @default.
• W4205652591 hasRelatedWork W1968497068 @default.
• W4205652591 hasRelatedWork W2001759023 @default.
• W4205652591 hasRelatedWork W2009397774 @default.
• W4205652591 hasRelatedWork W2017764792 @default.
• W4205652591 hasRelatedWork W2033874747 @default.

• next