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CD 3 - Cancer Drug Design and Development Group

CD 3 - Cancer Drug Design and Development Group. Focus on reversing resistance to conventional cancer therapies . www.imperial.ac.uk/medicine/about/institutes/drugdiscoverycentre/cd3/. Cancer Drug Design and Development Group (CD 3 ) .

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CD 3 - Cancer Drug Design and Development Group

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  1. CD3 - Cancer Drug Design and Development Group Focus on reversing resistance to conventional cancer therapies www.imperial.ac.uk/medicine/about/institutes/drugdiscoverycentre/cd3/

  2. Cancer Drug Design and Development Group (CD3) A cross-College Research group focused on the validation of oncology targets, and the development of leads and ultimately candidate small molecules for clinical PoC Major funding from Cancer Research UK: • CRUK training Programme in Medicinal Chemistry • CRUK Small Molecule Drug Discovery Programme Focus on translation

  3. Target Portfolio CRUK training Programme in Medicinal Chemistry Other Funding Agencies: EPSRC, AICR, etc. CDK7 APE1 HDAC4 HDAC1 DNMT1 Hsp90 GrB EZH2 LRH1 FMS CRUK Small Molecule Drug Discovery Programme CDK7 LRH1 Target Validation/Hit Identification Lead Optimisation

  4. Key Members Synthetic & Medicinal Chemistry Prof. Anthony Barrett FRS FMedSci Dr Matthew Fuchter – Also Project Manager (DDC) Dr Chris Braddock Prof. Alan Armstrong Prof. Alan Spivey Dr Albert Jaxa-Chamiec (DDC) Dr Caroline Low (DDC molecular modelling) Pharmacology and imaging Prof. Eric Aboagye Dr Cathy Tralau-Stewart (DDC) Dr Katie Chapman (DDC) Dr Richard Starkey Pharma Project Management Dr Cathy Tralau-Stewart (DDC) • Protein crystallography/structural biology • Prof. Paul Freemont • Cancer cell biology • Prof. Simak Ali • Prof. Eric Lam • Prof. Laki Buluwela • Prof. Hani Gabra • Prof. Philip Ashton-Rickardt • Dr Euan Stronach • Dr Nick Dibb • Epigenetics and pharmocodynamics • Prof. Robert Brown • Clinical development • Prof. Charles Coombes FMedSci

  5. Key Achievements • CDK7: • Discovery of the first selective CDK7 inhibitor BS181 (Cancer Res 2009, 69, 6208). • Discovery of a spectrum selective CDK inhibitor with strong growth inhibitory effects – BS194 (J. Med. Chem. 2010, 53, 8508). • Validated RNA PolII P-Ser5 as a useful biomarker for CDK7 inhibition. • LRH1: • Gained important new evidence for a major role for LRH-1 in breast cancer progression (Breast Cancer Res Treat 2010, DOI: 10.1007/s10549-010-0994-9). • Cdc25: • Discovery of the most potent drug-like inhibitors of this class of phosphatases known – project now achieved independent funding working with DDC. • SIRT: • Further defined role of isoform selectivity for known SIRT inhibitiors (Mol. Can. Ther. 2010, 9, 844).

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