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@ARTICLE{Amrhein:276862,
      author       = {J. A. Amrhein and G. Wang$^*$ and B.-T. Berger and L. M.
                      Berger and A. D. Kalampaliki and A. Krämer$^*$ and S.
                      Knapp$^*$ and T. Hanke},
      title        = {{D}esign and {S}ynthesis of {P}yrazole-{B}ased
                      {M}acrocyclic {K}inase {I}nhibitors {T}argeting {BMPR}2.},
      journal      = {ACS medicinal chemistry letters},
      volume       = {14},
      number       = {6},
      issn         = {1948-5875},
      address      = {Washington, DC},
      publisher    = {ACS},
      reportid     = {DKFZ-2023-01174},
      pages        = {833 - 840},
      year         = {2023},
      abstract     = {Bone morphogenetic protein (BMP) signaling is mediated by
                      transmembrane protein kinases that form heterotetramers
                      consisting of type-I and type-II receptors. Upon BMP
                      binding, the constitutively active type-II receptors
                      activate specific type-I receptors by transphosphorylation,
                      resulting in the phosphorylation of SMAD effector proteins.
                      Drug discovery in the receptor tyrosine kinase-like (TKL)
                      family has largely focused on type-I receptors, with few
                      inhibitors that have been published targeting type-II
                      receptors. BMPR2 is involved in several diseases, most
                      notably pulmonary arterial hypertension, but also
                      contributes to Alzheimer's disease and cancer. Here, we
                      report that macrocyclization of the promiscuous inhibitor 1,
                      based on a 3-amino-1H-pyrazole hinge binding moiety, led to
                      a selective and potent BMPR2 inhibitor 8a.},
      subtyp        = {Letter},
      cin          = {FM01},
      ddc          = {610},
      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:37312836},
      pmc          = {pmc:PMC10258821},
      doi          = {10.1021/acsmedchemlett.3c00127},
      url          = {https://inrepo02.dkfz.de/record/276862},
}