PhD Scholarship Top-up student profile: Gosia Drwal


Application of computer-aided methods for the design of novel inhibitors of topoisomerases

Award:  Gosia is a recipient of a final-year PhD Scholarship Top-up (2012)

Supervisor: Dr Renate Griffith, Associate Professor of Pharmacology, School of Medical Sciences UNSW

The overall aim of Gosia’s project is to determine the molecular characterisation of the inhibition of human DNA topoisomerases I and II – both validated anticancer targets. The molecular determinants of inhibition will be expressed as pharmacophore models which can be used in virtual database screening to retrieve molecules with topoisomerase I, II, or dual inhibitory activity. The hit compounds will be tested in vitro for their enzyme inhibition as well as cytotoxic activity (both assays performed at the National Cancer Institute, USA).

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Describe the clinical link to your research

Although several topoisomerase inhibitors are currently used clinically in anticancer therapy, they exhibit problems including side-effects and drug resistance. The main aim of my project is to develop structurally novel topoisomerase inhibitors that could overcome these issues and provide starting points for the future development of anticancer agents. Furthermore, an additional objective of my research is to find novel dual topoisomerase I and II inhibitors; by targeting both enzymes with one dual inhibitor we may be able to achieve an increase in anti-tumour activity and prevent drug resistance.

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“Being part of the TCRN gives me the opportunity to meet other people working in anticancer research, to learn about different cancer therapy areas and approaches, and to exchange knowledge and ideas.”

Gosia completed her final year of PhD studies at the School of Medical Sciences, UNSW in 2013.

Further details of Gosia’s research can be found in her 2011 publication:
Drwal MN, Agama K, Wakelin LPG, Pommier Y, Griffith R (2011) Exploring DNA topoisomerase I ligand space in search of novel anticancer agents. PloS ONE 6(9): e25150. doi:10.1371/journal.pone.0025150

 

TCRN PhD Scholarship Top-up awardee Gosia Drwal