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@ARTICLE{Capener:307547,
      author       = {J. L. Capener and M. P. Schwalm and J. D. Vasta and A.
                      Michaud and K. A. Teske and W. M. Marsiglia and K. V. M.
                      Huber and A. C. Dar and S. Knapp$^*$ and A. D. Axtman and M.
                      B. Robers},
      title        = {{A}dvances in {BRET} probes for intracellular target
                      engagement studies.},
      journal      = {Nature chemical biology},
      volume       = {nn},
      issn         = {1552-4450},
      address      = {Basingstoke},
      publisher    = {Nature Publishing Group},
      reportid     = {DKFZ-2026-00044},
      pages        = {nn},
      year         = {2026},
      note         = {#DKTKZFB9# / epub},
      abstract     = {Assessing drug-target engagement in living cells is
                      essential for verifying the activity of pharmacological
                      agents. Traditional binding assays often overlook key
                      factors such as permeability, intracellular distribution and
                      complex formation that influence target occupancy in cells.
                      Bioluminescence resonance energy transfer (BRET)-based
                      probes enable direct, quantitative assessment of
                      small-molecule binding to proteins in live, intact cells.
                      BRET provides sensitive detection of target engagement
                      across a wide range of target classes, including
                      less-tractable proteins in membrane compartments. Compared
                      to other existing methods, BRET offers quantification of
                      drug occupancy at steady state and open system regimens.
                      Recent innovations in this platform have expanded its
                      utility beyond occupancy confirmation to include
                      applications in polypharmacology and mechanism-of-action
                      studies. Here, we provide an updated perspective on BRET
                      target engagement assays as versatile tools for chemical
                      biology and early-stage drug discovery.},
      subtyp        = {Review Article},
      cin          = {FM01},
      ddc          = {570},
      cid          = {I:(DE-He78)FM01-20160331},
      pnm          = {899 - ohne Topic (POF4-899)},
      pid          = {G:(DE-HGF)POF4-899},
      typ          = {PUB:(DE-HGF)16},
      pubmed       = {pmid:41495225},
      doi          = {10.1038/s41589-025-02103-y},
      url          = {https://inrepo02.dkfz.de/record/307547},
}