Photoactivatable ligand tools for CXCR4 and ACKR3
Early stage researcher 1 (ESR1) project
Supervision: Prof. Dr. Rob Leurs, Prof. Dr. Iwan de Esch, Dr. Maikel Wijtmans
I- Project proposal:
The project aims for the design, synthesis and photochemistry of novel photoswitchable ligands for the CXCR4 and ACKR3 chemokine receptors.
This project will entail the design, synthesis and photochemical characterization of photoswitchable small-molecule CXCR4 and ACKR3 ligands. A wide variety of chemical transformations, synthetic equipment and photochemical techniques will be employed to generate and analyze the ligands. The design of any new ligands can be supported by computer-aided drug design studies where necessary. In vitro and in vivo pharmacological assays on the ligands will be conducted by fellow ESR7.
Heptares - the candidate will use modelling for characterizing the binding site of developed tools in CXCR4 X-ray structure and ACKR3 models.
University Hospital Jena – the candidate will work on in vitro characterization of photoswitchable compounds using single cell microscopy methodology.
II - Requirement candidate:
Required diploma: A MSc degree in Chemistry (or related field) with a specialization in Synthetic Organic Chemistry and/or Synthetic Medicinal Chemistry.
Required expertise: Experience in the design and synthesis of biologically active compounds is a necessity. The candidate has a strong background (theoretical and practical) in synthetic organic chemistry or synthetic medicinal chemistry.
Recommended expertise: Expertise in photochemistry is a strong pre. Expertise in medicinal chemistry on GPCRs is a pre.
- Hauwert et al., J. Am. Chem. Soc. 2018, 140, 4232
- Hauwert et al., Angew. Chem. Intl. Ed. 2019, 58, 4531
- Gómez-Santacana et al., Angew. Chem. Intl. Ed. 2018, 57, 11608
- Gómez-Santacana et al., Beilstein Arch. 2019, doi:10.3762/bxiv.2019.69.v1
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