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Synthesis of selective FKBP51 ligands

Synthesis of Macrocycles with functionalized linker units as selective FKBP51 ligands

This project comprises the rational design and synthesis of natural product-derived macrocycles as improved subtype-selective ligands for FKBP51, a validated drug for depression, obesity and chronic pain.

First, the students will synthesize a common core unit following internally established routes. Second, they will synthesize optically pure building blocks, which are then used to elaborate the core unit in a combinatorial fashion. All synthesized compounds will be characterized by NMR, MS and HPLC, their in vitro binding affinities will be determined in biochemical fluorescence polarization and nanoBRET assays, and for advanced compounds the binding mode will be established by X-ray crystallography of FKBP51 complexes.

This Project is supervised by Prof. Felix Hausch.

  • Experience in organic synthesis and analytics (NMR, HPLC, MS)
  • Bauder et al. J. Med. Chem. 2021, 64, 3320−3349 Voll et al. Angew.Chem.Int.Ed.2021,60,13257 –1326

Additional Information

Capacity One to Three IREP Students
Project available for Spring, Summer and Fall 2024
Credits 18 ECTS
Available via Remote No