The development of tankyrase inhibitors for use in breast cancer therapy. (360G-Wellcome-091050_Z_09_B)

£155,638

We propose to develop orally-bioavailable small molecule drugs that inhibit tankyrase 1 - a novel target for breast cancer therapy. Our data indicate that such drugs could be used in a synthetic lethality approach to treat cancer. A tankyrase 1 inhibitor would confront several tumour-specific characteristics and would be useful for treatment of specific breast cancer subtypes with a poor prognosis, where few treatment options exist. As part of this drug research programme, we will build on our existing in-house and proprietary knowledge to generate novel, patented candidate drugs that will be used in first in class Phase 1 clinical trials at The Royal Marsden Hospital. The programme we propose will include: 1) the further development of our existing prototype tankyrase 1 inhibitors, which we have identified following pre-selection of a compound set using an in silico based screen, 2) the delineation of a proprietary crystal structure of the active form of tankyrase 1 to guide the design of inhibitors, 3) a comprehensive medicinal chemistry programme, 4) the use of cellular assay systems and in vivo therapeutic efficacy assessments to aid the development of inhibitors and companion biomarkers and 5) high-throughput genetic and drug synergy screens that will identify companion biomarkers and direct the design of clinical trials. This programme will be underpinned by: (i) the unique in-depth knowledge of breast cancer, synthetic lethality and tankyrase 1 biology of the research team led by the Principal Applicant, (ii) the strong track-record of key members of the project team in drug research, and (iii) the strengths in structural biology and drug development available within the host Institute.

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Grant Details

Amount Awarded 155638
Applicant Surname Ashworth
Approval Committee Seeding Drug Discovery Committee
Award Date 2012-09-17T00:00:00+00:00
Financial Year 2011/12
Grant Programme: Title Seeding Drug Discovery Award
Internal ID 091050/Z/09/B
Lead Applicant Prof Alan Ashworth
Partnership Value 155638
Planned Dates: End Date 2013-01-31T00:00:00+00:00
Planned Dates: Start Date 2012-08-01T00:00:00+00:00
Recipient Org: Country United Kingdom
Region Greater London