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Synthesis of novel types of nucleotide analogues as enzyme inhibitors of nucleotide metabolism with potential antiparasitic and antibacterial activity

  • Full or part time
    Dr D Hockova
  • Application Deadline
    Sunday, February 23, 2020
  • Competition Funded PhD Project (Students Worldwide)
    Competition Funded PhD Project (Students Worldwide)

Project Description

In connection with the medicinal chemistry studies of the group, the topic of the project will be rational design and synthesis of novel types of nucleotide analogues as potential inhibitors of key enzymes involved in the metabolism of nucleic acid components. Emphasis will be placed on the selectivity of inhibition resulting from subtle differences in the active sites of enzymes of individual organisms. Crystal structures and molecular docking will be used to elucidate the inhibitors binding. Prodrugs of the best inhibitors will be prepared for cell-based assays. Biological activity of the prepared compounds, mainly antiparasitic (e.g. Plasmodium falciparum, Trypanosoma brucei) and antibacterial (e.g. Mycobacterium tuberculosis, Helicobacter pylori) will be studied in collaboration.

How to apply

To apply for a PhD study at IOCB Prague, you must hold a Master’s degree (MSc) or the equivalent of the MSc in similar field (four or five year undergraduate degree). The application can be submitted before obtaining the Master’s degree, however, the applicant should obtain the degree within five months after the application deadline.

For more information visit our website “Call for PhD applications 2020”:
https://www.uochb.cz/en/phd-program

If you decided to apply, please do so online via our application form:
https://www.uochb.cz/en/call-for-phd-applications

Funding Notes

Regular monthly income of students at IOCB Prague varies depending on the faculty scholarship and supervisor's financial options.

References

Špaček, P; Keough, D. T.; Chavchich, M.; Dračínský, M.; Janeba, Z.; Naesens, L.; Edstein, M. D.; Guddat, L. W.; Hocková, D. Synthesis and Evaluation of Asymmetric Acyclic Nucleoside Bisphosphonates as Inhibitors of Plasmodium falciparum and Human Hypoxanthine-Guanine-(Xanthine) Phosphoribosyltransferase. J. Med. Chem. 2017, 60, 7539-7554.

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