FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2012075902> ?p ?o ?g. }

• W2012075902 endingPage "334" @default.
• W2012075902 startingPage "326" @default.
• W2012075902 abstract "Rheumatoid arthritis (RA) is an autoimmune disease mediated by T-lymphocytes and associated with the human leukocyte antigen-death receptor 4 (HLA-DR4). The HLA-DR4 protein selectively interacts with the antigenic peptides on the cell surface and presents them to the T cell receptor (TCR) on CD4+ T cells. The HLA-DR4-antigen−TCR complex initiates the autoimmune response and eventually causes the chronic inflammation within patients bodies. To inhibit HLA-DR4-restricted T cell activation, an ideal approach is to discover non-T cell stimulating substrates that specifically bind to HLA-DR4. In this paper, a comprehensive structure-based design strategy involved de novo design approach, pharmacophore search, and dock method was presented and applied to “simplify” the known binding peptide ligand of HLA-DR4 and identified specific small-molecule inhibitors for HLA-DR4. The designed three-step strategy successfully identified five nonpeptide ligands with novel scaffolds from a chemical library containing 4 × 106 commercially available compounds within a tolerable computing time. The identified five chemicals, BAS-0219606, T0506-2494, 6436645, 3S-71981, and KM 11073, are all non-T cell stimulators and are able to significantly inhibit HLA-DR4-restricted T cell activation induced by type II collagen (CII) 263-272 peptide. IC50 for the best two potentials, BAS-0219606 and T0506-2494, was 31 and 17 μM, respectively, which is equivalent or better than the known peptide ligands. It is hopeful that they can be used as effective therapeutic means for further treatment of RA patients. In addition, the comprehensive strategy presented in this paper exhibited itself to be an effective flow line from peptide ligands to small-molecule inhibitors and will have applications to other targets." @default.
• W2012075902 created "2016-06-24" @default.
• W2012075902 creator A5034995105 @default.
• W2012075902 creator A5049692186 @default.
• W2012075902 creator A5053884196 @default.
• W2012075902 creator A5064049271 @default.
• W2012075902 creator A5079738340 @default.
• W2012075902 date "2011-02-02" @default.
• W2012075902 modified "2023-09-25" @default.
• W2012075902 title "Identification of Small-Molecule Inhibitors against Human Leukocyte Antigen-Death Receptor 4 (HLA-DR4) Through a Comprehensive Strategy" @default.
• W2012075902 cites W1503151765 @default.
• W2012075902 cites W1556420978 @default.
• W2012075902 cites W1562694314 @default.
• W2012075902 cites W1592950931 @default.
• W2012075902 cites W187920822 @default.
• W2012075902 cites W1964958542 @default.
• W2012075902 cites W1965377917 @default.
• W2012075902 cites W1967666989 @default.
• W2012075902 cites W1974173455 @default.
• W2012075902 cites W1982358601 @default.
• W2012075902 cites W2003607390 @default.
• W2012075902 cites W2003984456 @default.
• W2012075902 cites W2011230643 @default.
• W2012075902 cites W2023251537 @default.
• W2012075902 cites W2027329184 @default.
• W2012075902 cites W2027446384 @default.
• W2012075902 cites W2037111659 @default.
• W2012075902 cites W2037368532 @default.
• W2012075902 cites W2051005022 @default.
• W2012075902 cites W2053482692 @default.
• W2012075902 cites W2059247897 @default.
• W2012075902 cites W2074438676 @default.
• W2012075902 cites W2088067960 @default.
• W2012075902 cites W2091531721 @default.
• W2012075902 cites W2095025073 @default.
• W2012075902 cites W2096582408 @default.
• W2012075902 cites W2104823138 @default.
• W2012075902 cites W2118600639 @default.
• W2012075902 cites W2125649971 @default.
• W2012075902 cites W2136561782 @default.
• W2012075902 cites W2138058910 @default.
• W2012075902 cites W2158534713 @default.
• W2012075902 cites W2158637536 @default.
• W2012075902 cites W2164224372 @default.
• W2012075902 cites W2409346245 @default.
• W2012075902 cites W295940176 @default.
• W2012075902 cites W4236032807 @default.
• W2012075902 cites W4241888002 @default.
• W2012075902 doi "https://doi.org/10.1021/ci100444c" @default.
• W2012075902 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/21284404" @default.
• W2012075902 hasPublicationYear "2011" @default.
• W2012075902 type Work @default.
• W2012075902 sameAs 2012075902 @default.
• W2012075902 citedByCount "11" @default.
• W2012075902 countsByYear W20120759022014 @default.
• W2012075902 countsByYear W20120759022015 @default.
• W2012075902 countsByYear W20120759022016 @default.
• W2012075902 countsByYear W20120759022017 @default.
• W2012075902 countsByYear W20120759022018 @default.
• W2012075902 countsByYear W20120759022019 @default.
• W2012075902 countsByYear W20120759022020 @default.
• W2012075902 crossrefType "journal-article" @default.
• W2012075902 hasAuthorship W2012075902A5034995105 @default.
• W2012075902 hasAuthorship W2012075902A5049692186 @default.
• W2012075902 hasAuthorship W2012075902A5053884196 @default.
• W2012075902 hasAuthorship W2012075902A5064049271 @default.
• W2012075902 hasAuthorship W2012075902A5079738340 @default.
• W2012075902 hasConcept C147483822 @default.
• W2012075902 hasConcept C170493617 @default.
• W2012075902 hasConcept C185592680 @default.
• W2012075902 hasConcept C188280979 @default.
• W2012075902 hasConcept C19317047 @default.
• W2012075902 hasConcept C203014093 @default.
• W2012075902 hasConcept C2776090121 @default.
• W2012075902 hasConcept C2777575956 @default.
• W2012075902 hasConcept C2779281246 @default.
• W2012075902 hasConcept C55493867 @default.
• W2012075902 hasConcept C56173144 @default.
• W2012075902 hasConcept C86803240 @default.
• W2012075902 hasConcept C8891405 @default.
• W2012075902 hasConceptScore W2012075902C147483822 @default.
• W2012075902 hasConceptScore W2012075902C170493617 @default.
• W2012075902 hasConceptScore W2012075902C185592680 @default.
• W2012075902 hasConceptScore W2012075902C188280979 @default.
• W2012075902 hasConceptScore W2012075902C19317047 @default.
• W2012075902 hasConceptScore W2012075902C203014093 @default.
• W2012075902 hasConceptScore W2012075902C2776090121 @default.
• W2012075902 hasConceptScore W2012075902C2777575956 @default.
• W2012075902 hasConceptScore W2012075902C2779281246 @default.
• W2012075902 hasConceptScore W2012075902C55493867 @default.
• W2012075902 hasConceptScore W2012075902C56173144 @default.
• W2012075902 hasConceptScore W2012075902C86803240 @default.
• W2012075902 hasConceptScore W2012075902C8891405 @default.
• W2012075902 hasIssue "2" @default.
• W2012075902 hasLocation W20120759021 @default.
• W2012075902 hasLocation W20120759022 @default.
• W2012075902 hasOpenAccess W2012075902 @default.
• W2012075902 hasPrimaryLocation W20120759021 @default.

• next