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
Host: Vrije Universiteit Amsterdam

I- Project proposal:

Aim:
The project aims for the design, synthesis and photochemistry of novel photoswitchable ligands for the CXCR4 and ACKR3 chemokine receptors.

Methodology:
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.

Planned secondments:

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.

 Key publications:

  1. Hauwert et al., J. Am. Chem. Soc. 2018, 140, 4232
  2. Hauwert et al., Angew. Chem. Intl. Ed. 2019, 58, 4531
  3. Gómez-Santacana et al., Angew. Chem. Intl. Ed. 2018, 57, 11608
  4. Gómez-Santacana et al., Beilstein Arch. 2019, doi:10.3762/bxiv.2019.69.v1

For more information:

Prof. Dr. Rob Leurs – r.leurs@vu.nl

Prof. Dr. Iwan de Esch – i.de.esch@vu.nl

Dr. Maikel Wijtmans – m.wijtmans@vu.nl

 

Application:

Apply here

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My project will be focused on the role of #CXCR4/ACKR3/GRK2 -governed networks in cancer cell migration and metastasis.

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I am here to continue the series in which all #ESRs are presenting themselves. I am Viviana Marolda and I am in my first year of PhD. I am #ESR13, originally from Italy, and currently, I am working as a PhD student in @CBMSO_CSIC_UAM, at Universidad Autonoma de Madrid.

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I am @DehanComez. I am taking over the Oncornet account for a while to start a series of all #ESRs writing about themselves and their projects. I am #ESR5, originally from Turkey and right now I am working as a PhD student in @COMPARE_UoBUoN , @UniofNottingham , UK.

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ONCORNET2.0 is the successor to #ONCORNET. You can see some of the work of ESRs from the first ONCORNET in this special issue of @MolPharmJournal from 2019, with reviews on #CXCR4 and #ACKR3 structure and function: https://molpharm.aspetjournals.org/content/96/6

Hi everyone – we’re on Twitter! ONCORNET2.0 is a #MarieCurie ITN of 16 ESRs across Europe studying #chemokine #GPCRs #CXCR4 and #ACKR3 in cancer. Our projects cover molecular dynamics, medchem, #pharmacology through to translational work. Follow us for updates from our ESRs!

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Public service announcement: our Marie-Curie ITN @ONCORNET1 is on Twitter! The 16 wonderful #ECRs working on the project will soon be Tweeting about #GPCR #chemokine #ECR life and #pharmacology

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Contact details

Please contact us at:
info@oncornet.eu

ONCORNET Coordinator
VU University Amsterdam
The Netherlands