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www.imperial.ac.uk/medicine/about/institutes/drugdiscoverycentre/cd3/
CD3 - Cancer Drug Design and
Development GroupFocus on reversing resistance to
conventional cancer therapies
Cancer Drug Design Cancer Drug Design and Development Group (CDand Development Group (CD33) )
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
2
Focus on translation
Target PortfolioTarget Portfolio
CRUK training Programme in CRUK training Programme in Medicinal ChemistryMedicinal Chemistry
CDK7CDK7 LRH1LRH1
CDK7CDK7DNMT1DNMT1
FMSFMS
APE1APE1 HDAC4HDAC4
Other Funding Agencies:Other Funding Agencies:EPSRC, AICR, etc.EPSRC, AICR, etc.
EZH2EZH2LRH1LRH1HDAC1HDAC1 Hsp90Hsp90
GrBGrB
Lead Optimisation Target Validation/Hit Identification
CRUK Small CRUK Small Molecule Molecule
Drug Drug Discovery Discovery
ProgrammeProgramme
Key MembersKey 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
• CDK7:CDK7:•Discovery of the first selective CDK7 inhibitor BS181 Discovery of the first selective CDK7 inhibitor BS181 ((Cancer Res Cancer Res 20092009, 69, 6208, 69, 6208).).•Discovery of a spectrum selective CDK inhibitor with Discovery of a spectrum selective CDK inhibitor with strong growth inhibitory effects strong growth inhibitory effects –– BS194 (J. Med. Chem. BS194 (J. Med. Chem. 20102010, , 53, 850853, 8508).).•Validated RNA PolII P-Ser5 as a useful biomarker for Validated RNA PolII P-Ser5 as a useful biomarker for CDK7 inhibition.CDK7 inhibition.
•LRH1:LRH1:•Gained important new evidence for a major role for Gained important new evidence for a major role for LRH-1 in breast cancer progression (Breast Cancer Res LRH-1 in breast cancer progression (Breast Cancer Res Treat Treat 20102010, DOI: 10.1007/s10549-010-0994-9)., DOI: 10.1007/s10549-010-0994-9).
•Cdc25:Cdc25:•Discovery of the most potent drug-like inhibitors of this Discovery of the most potent drug-like inhibitors of this class of phosphatases known – project now achieved class of phosphatases known – project now achieved independent funding working with DDC.independent funding working with DDC.
•SIRT:SIRT:•Further defined role of isoform selectivity for known Further defined role of isoform selectivity for known SIRT inhibitiors (Mol. Can. Ther. SIRT inhibitiors (Mol. Can. Ther. 20102010, 9, 844)., 9, 844).
Key AchievementsKey Achievements