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@ARTICLE{ribar:430316,
      author       = {Šribar, Dora and Grabowski, Maria and Murgueitio, Manuela
                      S. and Bermudez, Marcel and Weindl, Günther and Wolber,
                      Gerhard},
      title        = {{I}dentification and characterization of a novel chemotype
                      for human {TLR}8 inhibitors},
      journal      = {European journal of medicinal chemistry},
      volume       = {179},
      issn         = {0223-5234},
      address      = {Amsterdam [u.a.]},
      publisher    = {Elsevier10887},
      reportid     = {PUBDB-2020-00008},
      pages        = {744-752},
      year         = {2019},
      note         = {© Elsevier Masson SAS. ; Final published version in
                      progress; Post referee fulltext in progress; Embargo 12
                      months from publication},
      abstract     = {The endosomal Toll-like receptor 8 (TLR8) recognizes
                      single-stranded RNA and initiates early inflammatory
                      responses. Despite the importance of endosomal TLRs for
                      human host defense against microbial pathogens, extensive
                      activation may contribute to autoimmune and inflammatory
                      diseases. In contrast to the recent progress made in the
                      development of modulators of plasma membrane-bound TLRs,
                      little is known about endosomal TLR modulation and very few
                      TLR8 inhibitors have been reported. In this study, we
                      discovered and validated novel small-molecule TLR8
                      inhibitors. Fourteen potential TLR8 modulators were
                      experimentally validated in HEK293T cells stably
                      overexpressing human TLR8 and THP-1 macrophages. Five
                      compounds inhibited TLR8-mediated signaling, representing a
                      hit rate of $36\%.$ The three most potent compounds neither
                      cause cellular toxicity nor inhibition of TLR signaling
                      induced by other receptor subtypes. Conclusively, we
                      experimentally confirm novel and selective, pyrimidine-based
                      TLR8 inhibitors with low cytotoxicity that are relevant
                      candidates for lead optimization and further mechanistic
                      studies.},
      cin          = {EMBL-User},
      ddc          = {610},
      cid          = {I:(DE-H253)EMBL-User-20120814},
      pnm          = {6G3 - PETRA III (POF3-622)},
      pid          = {G:(DE-HGF)POF3-6G3},
      experiment   = {EXP:(DE-H253)P-P14-20150101},
      typ          = {PUB:(DE-HGF)16},
      pubmed       = {pmid:31284084},
      UT           = {WOS:000486133100055},
      doi          = {10.1016/j.ejmech.2019.06.084},
      url          = {https://bib-pubdb1.desy.de/record/430316},
}