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@ARTICLE{Eberle:909095,
      author       = {Eberle, Raphael and Sevenich, Marc and Gering, Ian and
                      Scharbert, Lara and Strodel, Birgit and Santur, Karoline and
                      Mohrlüder, Jeannine and Coronado, Mônika and Willbold,
                      Dieter},
      title        = {{D}iscovery of all-{D}-peptide inhibitors of {SARS} {C}o{V}
                      2 3{C}-like protease},
      reportid     = {FZJ-2022-03008},
      year         = {2022},
      abstract     = {During the replication process of SARS-CoV-2 the main
                      protease of the virus (3-chymotrypsin-like protease
                      (3CLpro)) plays a pivotal role and is essential for the life
                      cycle of the pathogen. Numerous studies have been conducted
                      so far, which have confirmed 3CLpro as an attractive drug
                      target to combat COVID-19. We describe a novel and efficient
                      next generation sequencing (NGS) supported phage display
                      selection strategy for the identification of a set of
                      SARS-CoV-2 3CLpro targeting peptide ligands that inhibit the
                      3CL protease, in a competitive or non-competetive mode, in
                      the low µM range. From the most efficient L-peptides
                      obtained from the phage display, we designed all-D-peptides
                      based on the retro-inverso (ri) principle. They had IC50
                      values also in the low µM range, and in combination even in
                      the sub-micromolar range. The inhibition modes of these D-ri
                      peptides were the same as their respective L-peptide
                      versions. Our results demonstrate that retro-inverso
                      obtained all-D-peptides interact with high-affinity and
                      inhibit the SARS-CoV-2 3CL protease, thus reinforcing their
                      potential as therapeutic agents. The here described D-ri
                      peptides address limitations associated with current
                      L-peptide inhibitors and are promising lead compounds.
                      Further optimization regarding pharmacokinetic properties
                      will allow the development of even more potent D-peptides to
                      be used for the prevention and treatment of COVID-19.},
      cin          = {IBI-7},
      cid          = {I:(DE-Juel1)IBI-7-20200312},
      pnm          = {5241 - Molecular Information Processing in Cellular Systems
                      (POF4-524)},
      pid          = {G:(DE-HGF)POF4-5241},
      typ          = {PUB:(DE-HGF)25},
      doi          = {10.26434/chemrxiv-2022-rjdzz},
      url          = {https://juser.fz-juelich.de/record/909095},
}