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Lead Optimisation of Novel Androgen Receptor Small.. (FBMC2010MDG)
Lead Optimisation of Novel Androgen Receptor Small Molecule Modulators - Improving Treatment of Prostate Cancer
(FBMC2010MDG)
Date du début: 1 mars 2011,
Date de fin: 28 févr. 2013
PROJET
TERMINÉ
"One of the traditional approaches for the treatment of prostate cancer is the administration of steroid-derived Androgen Receptor (AR) antagonists. These treatments show significant side effects due to their high dosing requirements. In a novel intervention approach Molecular Design Group (Trinity College Dublin), has used a variety of computational drug discovery techniques to analyse a recently identified, non-steroid AR protein binding site, termed the activation function 2 (AF2) site. The goal of this proposal is to perform lead optimisation for the development of new drugs that combat prostate cancer in a different way, circumventing the observed resistance.The project will be implemented at Trinity College Dublin (TCD), Ireland's leading research University, supervised by Dr David Lloyd and Dr Darren Fayne, from Molecular Design Group (TCD), on the computational methodologies, Prof Mary Meegan, from the School of Pharmacy and Pharmaceuticals Studies (TCD), on the synthetic methodologies and Prof Clive Williams, from the School of Biochemistry and Immunology (TCD) on the biological assays. The responsibilities of the experienced researcher, Dr. Fernando Blanco, within the project will focus on the rational computational design and synthesis of new potential pharmaceuticals, receiving multidisciplinary training combining computational strategies, synthesis and biological assays, as well as other fundamental aspects (managing and administering of a research programme) related to strengthen the abilities of the Dr. Blanco to become a leading independent researcher in the field.The completion of the present project is a major step in the research career of Dr. Blanco to successfully reach a position of professional maturity. In addition, the development of new small molecules to treat prostate cancer and have an impact upon translational research that will lead to clinical applications for cancer treatments is a central priority in Europe."
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