Supplementary Materials

The PDF file includes:

  • Fig. S1. Flow cytometric analysis of human lung tissue samples showing up-regulation of FAP on IPF lung fibroblasts.
  • Fig. S2. Binding of FAPL-fluorescein to HLF cells before (red dots) and after (blue dots) transfection with human FAP.
  • Fig. S3. TGFβ1 induced FAP and αSMA expression in an HLF cell line.
  • Fig. S4. FAP-targeted PI3Ki (FAPL-PI3Ki1) suppresses phosphorylation of Akt in IPF fibroblasts.
  • Fig. S5. Characterization of the time course of development of pulmonary fibrosis after intratracheal administration of bleomycin (0.75 U/kg) to mice.
  • Fig. S6. Quantitative biodistribution of FAPL_S0456 in healthy and bleomycin-treated mice.
  • Fig. S7. Quantification of optical imaging of bleomycin-induced experimental lung fibrosis in mice with a FAP-targeted NIR dye (FAPL-S0456).
  • Fig. S8. Hydroxyproline content in the lungs of bleomycin-treated mice receiving FAPL-S0456 in either the presence or absence of excess FAPL (100×).
  • Fig. S9. Analysis of pharmacokinetics and stability of FAPL-PI3Ki1.
  • Fig. S10. Evaluation of HLF survival (MTT assay).
  • Table S1. Docking and docking glide-score for the compounds docked in the active site of PI3Kγ (PDB code: 3L08) using Schrödinger Maestro software.
  • Table S2. Primer sequence.
  • Legends for data files S1 and S2

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Other Supplementary Material for this manuscript includes the following:

  • Data file S1 (Microsoft Excel format). Raw data.
  • Data file S2 (Microsoft Word format). Synthetic procedures and schemes.